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TSA (Trichostatin A)

中文名稱：曲古抑菌素A

TSA (Trichostatin A) 是一種HDAC抑制劑，無細(xì)胞試驗中IC50為1.8 nM左右。

TSA (Trichostatin A) Chemical Structure

TSA (Trichostatin A) Chemical Structure

CAS: 58880-19-6

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 3595.41 現(xiàn)貨
2mg 1613.43 現(xiàn)貨
5mg 3030.3 現(xiàn)貨
100mg 22686.3 現(xiàn)貨
更大包裝 有超大折扣

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TSA (Trichostatin A)相關(guān)產(chǎn)品

相關(guān)信號通路圖

HDAC Signaling Pathways

HDAC信號通路圖

細(xì)胞實(shí)驗數(shù)據(jù)示例

細(xì)胞系 實(shí)驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
U87 GBM Growth Inhibition Assay 100/300/500 nM 72 h reduces mean cell number by 31, 54, and 58?% 24464841
U87 GBM Function Assay 100/500 Nm 48 h Induces Senescence-Like Alterations in Nuclear Morphology 24464841
RPE Growth Inhibition Assay 0.2/0.4/0.8/1 μM 24/48/72 h inhibits the proliferation by cell cycle arrest 24456602
HT29? Growth Inhibition Assay 180 nM 72 h IC50 of 180 nM 24368265
hMSCs Function Assay 6.25 nM 24 h stabilizes Histone Acetylation and the Expression of Pluripotent Genes 24312356
Huh7? Function Assay 0.1/0.5/1.0 μM 24h suppresses YTHDC2 gene expression 24269672
SKOV3 Growth Inhibition Assay 0.05-2 μM 10/24/48 h mediates growth arrest in a concentration- and time-dependent manner 24223801
A2780 Growth Inhibition Assay 0.05-2 μM 10/24/48 h mediates growth arrest in a concentration- and time-dependent manner 24223801
SRA01/04? Growth Inhibition Assay 0.2 μM 48 h suppresses cell proliferation through suppressing the PI3K/Akt, p38MAPK and ERK1/2 signaling pathways 24157878
HLEB3 Growth Inhibition Assay 0.2 μM 48 h suppresses cell proliferation through suppressing the PI3K/Akt, p38MAPK and ERK1/2 signaling pathways 24157878
SRA01/04? Growth Inhibition Assay 0.4/0.8 μM 48 h induces cell apoptosis 24157878
HLEB3 Growth Inhibition Assay 0.4/0.8 μM 48 h induces cell apoptosis 24157878
HCT116 Growth Inhibition Assay 0.2 μM 12 h enhances cell apoptosis induced by radiation 24122231
CA46 Growth Inhibition Assay 3/6/12/24/48 nM 48 h inhibits the cell proliferation at 24 and 48 nM? 24064951
PMNs Function Assay 30 nM 48 h inhibits efferocytosis, HDAC activity and Rac activity 23988617
H1299 Growth Inhibition Assay 1?μM? 24/48/72 h increases cell death after 24h 23916609
A549 Growth Inhibition Assay 0.25/0.5/1 μM 24/48/72 h inhibits the cell growth in concentration and time-dependent manner 23867991
H1299 Growth Inhibition Assay 0.25/0.5/1 μM 24/48/72 h inhibits the cell growth in concentration and time-dependent manner 23867991
A549 Apoptosis Assay 0.5/1 μM 48 h induces cell apoptosis 23867991
H1299 Apoptosis Assay 0.5/1 μM 48 h induces cell apoptosis 23867991
SUM149PT Growth Inhibition Assay 2/7.5/10 μM 48 h induces cell death at 2 μM insensitively 23792638
SUM190PT Growth Inhibition Assay 50/100/250 nM 48 h induces cell death at 50 nM sensitively 23792638
HCT1 Growth Inhibition Assay 0.2/1.0/5.0 μM 12/24/36/48 h induces cell death in concentration- and time-dependent manner 23770000
Lovo Growth Inhibition Assay 0.2/1.0/5.0 μM 12/24/36/48 h induces cell death in concentration- and time-dependent manner 23770000
Huh7 Growth Inhibition Assay 1 μM 24 h reduces about 20% viability? 23643933
AGS Growth Inhibition Assay 0.015-1 μM 72 h induces cell death concentration dependently 23745024
ECC1 Function Assay 500 nM 5 d induces L1CAM?expression co-treatment with 5-AzaC 23530769
HEC1A Function Assay 500 nM 5 d induces L1CAM?expression co-treatment with 5-AzaC 23530769
EN1 Function Assay 500 nM 5 d induces L1CAM?expression co-treatment with 5-AzaC 23530769
MFE296 Function Assay 500 nM 5 d induces L1CAM?expression co-treatment with 5-AzaC 23530769
HASMCs Function Assay 0-500 nM 6 d down-regulates the expression of HADC and cell viability 23518467
U373 Function Assay 0.25/0.5/1 μM 24 h increases PR-B expression co-treatment with 5AzadC 23474171
ARN8? Function Assay 0.05-2 μM 24 h reduces the induction of p53-dependent genes by Nutlin-3 23470540
MCF7 Function Assay 0.05-2 μM 24 h reduces the induction of p53-dependent genes by Nutlin-3 23470540
H1299? Function Assay 0.33–1?μM 24/48 h increases E-cadherin protein levels dose dependently 23461975
H1299 Function Assay 0.5 μM 48 h inhibits the migratory potential combine with silibinin 23461975
H1299 Function Assay 0.5 μM 48 h inhibits the invasiveness? combine with silibinin 23461975
MG-63? Growth Inhibition Assay 0.3 μM 12-96 h inhibits the cell growth co-treatment with metformin 23451817
LM8 Growth Inhibition Assay 0.3 μM 12-96 h inhibits the cell growth co-treatment with metformin 23451817
K562 Function Assay 0.5 μM 24 h decreases the enzyme activity of HDACs co-treatment with curcumin 23430957
HEL Function Assay 0.5 μM 24 h decreases the enzyme activity of HDACs co-treatment with curcumin 23430957
HL60 Apoptosis Assay 1 μM 24 h induces?cell death 23400519
KG1 Apoptosis Assay 1 μM 24 h induces?cell death 23400519
Kazumi Apoptosis Assay 1 μM 24 h induces?cell death 23400519
K562 Apoptosis Assay 1 μM 24 h induces?cell death 23400519
THP1 Apoptosis Assay 1 μM 24 h induces?cell death 23400519
SH-SY5Y Function Assay 250 nM 16 h changes expression pattern of genes involved in cholesterol synthesis, uptake and efflux 23326422
HEK293 Function Assay 1 μM? 18 h? inhibits the kalirin-7-mediated recruitment of synphilin-1 aggregates into aggresomes 23284848
HTK Function Assay 400 nM 72 h inhibits TGF-β–Induced Myofibroblast Differentiation 23284002
HTK Function Assay 100-800nM 72 h blocks TGF-β–Induced ROS and H2O2?Accumulation 23284002
Caco-2? Function Assay 1 μM? 24 h decreases SERT protein expression 23195070
HeLa Growth Inhibition Assay 100 nM 24 h IC50 of 100nM 23165748
HeLa Growth Inhibition Assay 40 nM 48 h IC50 of 40nM 23165748
HeLa Growth Inhibition Assay 20 nM 72 h IC50 of 20nM 23165748
HeLa Growth Inhibition Assay 10/30/50 nM 72 h increases the number of MMP (ΔΨm) loss cells dose dependently 23165748
ACP03 Growth Inhibition Assay 250/350/500nM 24h decreases cell viability of approximately 70?% at 250?nM 24668547
ACP02 Growth Inhibition Assay 250/350/500nM 24h decreases cell viability of approximately 70?% at 250?nM 24668547
HeLa Function Assay 1mM 0.5h abolishes the total HDAC activity 24707474
HMEC-1? Function Assay 300nM 24h increases expression of?VEGFR3?mRNA 24710631
HeLa? Growth Inhibition Assay 2μM 48h decreases cell viability about 25% 24846135
LNCaP Growth Inhibition Assay 100-1000nM 24h IC50 of 300nM 24854658
PC3 Growth Inhibition Assay 100-1000nM 24h IC50 of 300nM 24854658
CNE2 Growth Inhibition Assay 100-600nM 24/48/72h inhibits the proliferation in a time- and dose-dependent manner 24969901
HeLa Function Assay 250nM 16h increases CYP1A1 mRNA expression? 25116688
A549 Growth Inhibition Assay 0.01-0.9μM 72h IC50 of 0.06μM 25169491
SKOV-3 Growth Inhibition Assay 0.01-0.9μM 72h IC50 of 0.32μM 25169491
A549 Growth Inhibition Assay 0.1-1μM 48h IC50 of 0.28μM 25169491
SKOV-3 Growth Inhibition Assay 0.1-1μM 48h IC50 of 0.7μM 25169491
A549 Growth Inhibition Assay 1-10μM 24h IC50 of 3.2μM 25169491
SKOV-3 Growth Inhibition Assay 1-10μM 24h IC50 of 5.6μM 25169491
MCF7 Growth Inhibition Assay 0-600nM 24h IC50 of 75nM 25192721
MDA-MB-231 Growth Inhibition Assay 0-600nM 24h IC50 of 100nM 25192721
A431 Function Assay 50nM 2/6/12/24h activates p21 and inhibits ATF3 expression 25371069
A431 Apoptosis Assay 2/10/50/100nM 48h inhibits the cell growth 25371069
PC3? Function Assay 0.1μM 48h induces increase of HDAC1 and HDAC2 on Slug genes promoter 25434997
SW480? Function Assay 0.1μM 48h induces increase of HDAC1 and HDAC2 on Slug genes promoter 25434997
PC3? Function Assay 0.1μM 48h attenuates invasion and migration 25434997
PC3? Function Assay 0.1μM 48h reverses EMT 25434997
SW480? Function Assay 0.1μM 48h attenuates invasion and migration 25434997
SW480? Function Assay 0.1μM 48h reverses EMT 25434997
MEFs Function Assay 5μM 16h increases the EPEC attachment, Tir delivery and the efficiency of pedestal formation 25482634
TE13 Apoptosis Assay 0.3μM 24h inhibits the cell proliferation 25579665
TE13 Function Assay 0.3μM 24h up-regulates RASSF5A level 25579665
HEK 293 Function Assay 0.7μM 24h enhances ENaC acetylation and increases ENaC abundance in the total cell lysate and at the cell surface 25787079
MDA-MB-231 Growth Inhibition Assay 25-400 nM 48 h IC50 of 263.2nM? 23055198
MCF-7? Growth Inhibition Assay 25-400 nM 48 h IC50 of 220.4nM 23055198
ECC-1? Growth Inhibition Assay 100 nM 24 h increases the proportion of apoptotic nuclei to 35% 23028803
HEC-1A Growth Inhibition Assay 100 nM 24 h increases the proportion of apoptotic nuclei to 39% 23028803
NHAC-kn Growth Inhibition Assay 10/100/500 nM 12 h IC50 of 500nM 23017871
A549 Growth Inhibition Assay 250 nM 6-72 h causes a greater inhibitory effect combine with TXT or erlotinib 22994780
MG-63 Growth Inhibition Assay 300 nM 12 h inhibits the cell growth to 86% 22799338
MG-63 Growth Inhibition Assay 300 nM 24 h inhibits the cell growth to 67% 22799338
MG-63 Growth Inhibition Assay 300 nM 48 h inhibits the cell growth to 56% 22799338
HL60? Growth Inhibition Assay 150-350 nM 24 h increases cell apoptosis?when concentrations higher than 250 nM 22753739
U937 Growth Inhibition Assay 150-350 nM 24 h increases cell apoptosis?when concentrations higher than 250 nM 22753739
SCC-6 Growth Inhibition Assay 200-3200 nM 12/24/48 h inhibits the proliferation of SCC-6 cells in a dose- and time-dependent manner 22552321
U87? Growth Inhibition Assay 100-300 ng 24 h inhibits the cell growth to 72% at 200ng 22270849
K562 Function Assay 1 μM 12 h enhances the expression of RUNX3 induced by 5-aza-CdR 22179198
Reh Function Assay 0.3/1 μM 12 h enhances the expression of RUNX3 induced by 5-aza-CdR 22179198
GM15850 Function assay 0.1 uM 12 hrs Inhibition of HDAC in human GM15850 cells assessed as increase in total acetylated histone level at 0.1 uM after 12 hrs by Western blot analysis 16921367
HeLa Function assay 1 uM 24 hrs Induction of p16 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting 17643111
HeLa Function assay 1 uM 24 hrs Induction of p27 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting 17643111
HeLa Function assay 1 uM 24 hrs Induction of p21 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting 17643111
NCI-H661 Function assay 300 nM 6 hrs Inhibition of HDAC in human NCI-H661 cells assessed as induction of histone H4 acetylation at 300 nM after 6 hrs by Western blot analysis 19385600
NCI-H661 Function assay 300 nM 6 hrs Inhibition of HDAC in human NCI-H661 cells assessed as induction of alpha-tubulin acetylation at 300 nM after 6 hrs by Western blot analysis 19385600
HL60 Function assay 20 ug/ml 24 hrs Inhibition of HDAC in human HL60 cells assessed as increase in histone H3 acetylation at 20 ug/ml after 24 hrs by Western blot analysis 19534471
MCF7 Function assay 0.1 uM 16 hrs Inhibition of SIRT2 in human MCF7 cells assessed as tubulin hyperacetylation at 0.1 uM after 16 hrs by Western blot 20030343
HeLa Function assay 1 uM 10 mins Inhibition of HDAC in human HeLa cells at 1 uM after 10 mins by fluorometric assay 21055848
MCF7 Function assay 0.5 uM 24 hrs Inhibition of Class 1 histone deacetylase in human MCF7 cells assessed as up-regulation of p21 protein level at 0.5 uM after 24 hrs by Western blot analysis 22280363
MCF7 Function assay 0.5 uM 24 hrs Inhibition of HDAC6 in human MCF7 cells assessed as change in tubulin acetylation level at 0.5 uM after 24 hrs by Western blot analysis 22280363
MCF7 Function assay 0.5 uM 24 hrs Inhibition of HDAC1 in human MCF7 cells assessed as up-regulation of acetylated histone H3 protein level at 0.5 uM after 24 hrs by Western blot analysis 22280363
PC12 Function assay 10 uM 48 hrs Inhibition of HDAC6 in rat PC12 cells assessed as acetylation of histone H3 at 10 uM after 48 hrs by Western blotting analysis 23905680
PC12 Function assay 10 uM 48 hrs Inhibition of HDAC6 in rat PC12 cells assessed as induction of alpha-tubulin acetylation at 10 uM after 48 hrs by Western blotting analysis 23905680
PC12 Function assay 10 uM 5 days Induction of neurite outgrowth in rat PC12 cells at 10 uM after 5 days 23905680
SH-SY5Y Function assay 10 uM 5 days Induction of neurite outgrowth in human SH-SY5Y cells at 10 uM after 5 days 23905680
A549 Antiproliferative assay 0.4 uM 24 hrs Antiproliferative activity against human A549 cells assessed as shrunken and sharp shape at 0.4 uM after 24 hrs by phase contrast microscopy 25884112
C127-LT Function assay 200 nM 24 hrs Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 200 nM after 24 hrs by fluorescence microscopy 26996372
HeLa nuclear Function assay 10 to 25 uM 30 mins Competitive inhibition of HDAC in human HeLa nuclear cells at 10 to 25 uM using Boc-acetyl-lysine-AMC as substrate after 30 mins by Lineweaver-Burk plot analysis 26996372
HeLa Function assay 2 uM 24 hrs Inhibition of HDAC1 in human HeLa cells assessed as hyperacetylation of histone H3 at 2 uM incubated for 24 hrs by Western blot analysis 27060764
HeLaS3 Function assay 10 uM 16 hrs Inhibition of HDAC in human HeLaS3 cells assessed as increase in histone H3K9 acetylation at 10 uM treated for 16 hrs followed by compound washout and measured up to 24 hrs by immunoblot analysis 30258535
A549 Function assay 0.1 uM Inhibition of SIRT2 in A549 cells assessed as ability to induce hyperacetylation of tubulin by Western blot analysis at 0.1 uM 17149860
ST14A Function assay 75 nM Induction of REST/NRSF-coupled repression of luciferase tagged rat RE1/NRSE BDNF promoter activity expressed in ST14A cells at 75 nM assessed as increase in luciferase activity 17565993
HEK293 Function assay 600 nM Increase in GRP78 protein level in HEK293 cells at 600 nM by immunoblot 17566732
HEK293 Function assay 600 nM Increase in protein disulfide isomerase level in HEK293 cells at 600 nM by immunoblot 17566732
primary bronchial epithelial cell Function assay 0.1 uM Inhibition of HDAC7 in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 0.1 uM 19966789
HeLaS3 Function assay 10 uM Inhibition of HDAC in human HeLaS3 cells assessed as increase in histone H3K9 acetylation at 10 uM measured immediately by immunoblot analysis 30258535
Mv1Lu Function assay 18 hrs Induction of wild-type p21 promoter activation in mink Mv1Lu cells after 18 hrs by luciferase assay relative to basal level, EC1000 = 0.19 μM. 17881232
HeLa Function assay 24 hrs Induction of p21 expression in human HeLa cells after 24 hrs, EC1000 = 0.0115 μM. 18397826
Mv1Lu Function assay 24 hrs Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay, EC1000 = 0.02 μM. 24997578
HL60 Antiproliferative assay 24 hrs Antiproliferative activity against human HL60 cells after 24 hrs by MTT assay, GI50 = 0.59 μM. 29454918
MDA-MB-435 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-435 cells after 24 hrs by MTT assay, GI50 = 1.78 μM. 29454918
H661 Antiproliferative assay 48 hrs Antiproliferative activity against H661 cells after 48 hrs by XTT assay, IC50 = 0.085 μM. 17624773
H661 Antiproliferative assay 48 hrs Antiproliferative activity against H661 cells after 48 hrs, IC50 = 0.085 μM. 17897824
NCI-H661 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H661 cells after 48 hrs by XTT assay, IC50 = 0.1 μM. 19385600
HCT116 Cytotoxicity assay 3 days Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.8 μM. 20452226
HCT116 Growth inhibition assay 48 hrs Growth inhibition of human HCT116 cells after 48 hrs by SRB assay, IC50 = 0.043 μM. 21073160
H460 Growth inhibition assay 48 hrs Growth inhibition of human H460 cells after 48 hrs by SRB assay, IC50 = 0.1 μM. 21073160
DMS53 Cytotoxicity assay 2 days Cytostatic activity against human DMS53 cells assessed as inhibition of cell proliferation after 2 days by MTT assay, IC50 = 0.025 μM. 21504214
HeLa Function assay 20 mins Inhibition of HDAC in human HeLa cells using Ac-Arg-Gly-Lys(Ac)-AMC as fluorescent substrate after 20 mins by fluorescence assay, IC50 = 0.003 μM. 21621883
Sf9 Function assay 1 hr Inhibition of N terminal hexahistidine-tagged human HDAC8 expressed in Sf9 cells after 1 hr by fluorescence assay, IC50 = 0.96 μM. 21723733
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 1.7 μM. 22465091
BE(2)-C Antiproliferative assay 72 hrs Antiproliferative activity against human BE(2)-C cells after 72 hrs by Alamar blue assay, IC50 = 0.05 μM. 22932316
Sf9 Function assay 2 hrs Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 0.0012 μM. 23009203
Sf9 Function assay 2 hrs Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 0.005 μM. 23009203
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against cisplatin resistant human A2780 cells after 72 hrs by MTT assay, IC50 = 0.22 μM. 23252603
A2780 Function assay 18 hrs Inhibition of HDAC in cisplatin resistant human A2780 cells after 18 hrs by fluorescence assay, IC50 = 0.25 μM. 23252603
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, IC50 = 0.29 μM. 23252603
A2780 Function assay 18 hrs Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay, IC50 = 0.43 μM. 23252603
MOLT4 Cytotoxicity assay 72 hrs Cytotoxicity against human MOLT4 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.03 μM. 24960627
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.05 μM. 24960627
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.06 μM. 24960627
HL60 Cytotoxicity assay 72 hrs Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.08 μM. 24960627
BGC823 Cytotoxicity assay 72 hrs Cytotoxicity against human BGC823 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.08 μM. 24960627
HuH7 Cytotoxicity assay 72 hrs Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.1 μM. 24960627
U937 Cytotoxicity assay 72 hrs Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.1 μM. 24960627
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.11 μM. 24960627
NCI-H1975 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.21 μM. 24960627
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 0.41 μM. 24960627
HEK293 Cytotoxicity assay 96 hrs Cytotoxicity against human HEK293 cells after 96 hrs by MTT assay, IC50 = 0.16 μM. 25556102
LO2 Cytotoxicity assay 96 hrs Cytotoxicity against human LO2 cells after 96 hrs by MTT assay, IC50 = 0.21 μM. 25556102
HeLa Cytotoxicity assay 96 hrs Cytotoxicity against human HeLa cells after 96 hrs by MTT assay, IC50 = 0.85 μM. 25556102
HepG2 Cytotoxicity assay 96 hrs Cytotoxicity against human HepG2 cells after 96 hrs by MTT assay, IC50 = 0.96 μM. 25556102
U2OS Cytotoxicity assay 96 hrs Cytotoxicity against human U2OS cells after 96 hrs by MTT assay, IC50 = 14.93 μM. 25556102
Sf9 Function assay 90 mins Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate incubated for 90 mins by fluorescence assay, IC50 = 0.001716 μM. 27060764
Sf21 Function assay 60 mins Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay, IC50 = 0.006574 μM. 27060764
insect cell Function assay 60 mins Inhibition of full length human recombinant C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay, IC50 = 0.01051 μM. 27060764
insect cell Function assay 60 mins Inhibition of full length human recombinant C-terminal His-tagged HDAC3 (1 to 428 residues)/human recombinant N-terminal GST-tagged NCOR2 expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay, IC50 = 0.01107 μM. 27060764
insect cell Function assay 60 mins Inhibition of human recombinant C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay, IC50 = 0.3074 μM. 27060764
SHSY5Y Function assay 8 hrs Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0078 μM. 27650925
SHSY5Y Function assay 8 hrs Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0091 μM. 27650925
Sf9 Function assay 4 hrs Inhibition of human recombinant GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using MOCPAC as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0157 μM. 27650925
insect cell Function assay 4 hrs Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using BATCP as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.016 μM. 27650925
SHSY5Y Function assay 8 hrs Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0188 μM. 27650925
HEK293T Function assay 30 mins Inhibition of recombinant human HDAC1 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins in presence of DTT by fluorescence assay, IC50 = 0.019 μM. 29519604
HEK293T Function assay 30 mins Inhibition of recombinant mouse HDAC6 expressed in HEK293T cells co-expressing mouse HDA2 using Ac-KGLGK(Ac)-MCA as substrate after 30 mins in presence of DTT by fluorescence assay, IC50 = 0.028 μM. 29519604
Sf9 Function assay 90 mins Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus-infected Sf9 insect cells using RHKK(Ac)AMC as substrate after 90 mins by fluorimeter, Ki = 0.00058 μM. 29589441
Sf21 Function assay 60 mins Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus-infected Sf21 insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter, Ki = 0.00064 μM. 29589441
insect cell Function assay 60 mins Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged recombinant human NCOR2 (395 to 489 residues) expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter, Ki = 0.00084 μM. 29589441
insect cell Function assay 60 mins Inhibition of full length recombinant human C-terminal GST-tagged HDAC2 expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter, Ki = 0.00355 μM. 29589441
insect cell Function assay 60 mins Inhibition of recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in baculovirus-infected insect cells using RHK(Ac)K(Ac)AMC as substrate after 60 mins by fluorimeter, Ki = 0.145 μM. 29589441
HEK293 STF Function assay 24 hrs Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay 19022675
HN13 Function assay 24 hrs Inhibition of HDAC in human HN13 cells assessed as reduction in histone H3 Lys9 acetylation incubated for 24 hrs by immunofluorescence assay 29031066
HCT 116 Antiproliferative assay In vitro antiproliferative activity against human colon cancer HCT 116 cells determined by MMT assay, EC50 = 1 μM. 11597413
T24 Function assay Concentration of compound required for acetylation of histone-4 in human T24 cancer cells, EC50 = 1 μM. 11597413
T24 Function assay Inhibition of acetylation of histone-4 in human T-24 cancer cells, EC50 = 1 μM. 14613312
T24 Function assay Inhibition of acetylation of histone-4 in human T-24 cancer cells, EC50 = 4 μM. 14613312
T24 Function assay Induction of alpha tubulin acetylation in human T24 cells, EC50 = 0.01 μM. 19111466
T24 Function assay Induction of histone H3 acetylation in human T24 cells, EC50 = 0.01 μM. 19111466
HepG2 Function assay Up-regulation of transcriptional activity of human CLA-1 promoter region -1055 to -62bp transfected in HepG2 cells by luciferase reporter gene assay, EC50 = 0.38 μM. 25556102
HeLa Function assay Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA, EC50 = 0.0052 μM. 26611919
K562 Function assay Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells., IC50 = 0.0046 μM. 10425110
A20 Function assay In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells, IC50 = 0.002 μM. 11960489
K 562 Function assay Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells, IC50 = 0.0034 μM. 14592473
friend cell Function assay Inhibitory concentration against friend cells proliferation, IC50 = 0.04 μM. 14613312
SNU-16 Function assay Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells, IC50 = 0.05329 μM. 14667227
melanoma B16/BL6 Function assay Inhibitory activity against histone deacetylases (HDAC1) prepared from mouse melanoma B16/BL6 cells, IC50 = 0.019 μM. 15109626
melanoma B16/BL6 Function assay Inhibitory activity against histone deacetylase (HDAC4) prepared from mouse melanoma B16/BL6 cells, IC50 = 0.02 μM. 15109626
melanoma B16/BL6 Function assay Inhibitory activity against histone deacetylase 6 prepared from mouse melanoma B16/BL6 cells, IC50 = 0.028 μM. 15109626
melanoma B16/BL6 Function assay Inhibitory activity against histone deacetylase 8 prepared from mouse melanoma B16/BL6 cells, IC50 = 0.04 μM. 15109626
293T Function assay Inhibition of human histone deacetylase 4 prepared from 293T cells, IC50 = 0.02 μM. 15454224
293T Function assay Inhibition of human histone deacetylase 1 prepared from 293T cells, IC50 = 0.02 μM. 15454224
293T Function assay Inhibition of human histone deacetylase 6 prepared from 293T cells, IC50 = 0.02 μM. 15454224
293T Function assay Inhibition of human histone deacetylase 8 prepared from 293T cells, IC50 = 0.04 μM. 15454224
HeLa Function assay Inhibitory concentration against human histone deacetylase (HDAC) from HeLa cells with substrate 5a, IC50 = 0.0545 μM. 15456267
HCT116 Antiproliferative assay Antiproliferative activity against HCT116 cells, IC50 = 0.0013 μM. 16904890
H1299 Antiproliferative assay Antiproliferative activity against H1299 cells, IC50 = 0.1 μM. 16904890
H661 Antiproliferative assay Antiproliferative activity against H661 cells, IC50 = 0.3 μM. 16904890
WiDr Growth inhibition assay Inhibition of SAP130 mediated cell growth in human WiDr cells, IC50 = 0.5776 μM. 17643112
U251 Function assay Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay, IC50 = 0.6112 μM. 17643112
293T Function assay Inhibition of human HDAC1 expressed in 293T cells, IC50 = 0.0019 μM. 17881232
293T Function assay Inhibition of human HDAC4 expressed in 293T cells, IC50 = 0.002 μM. 17881232
293T Function assay Inhibition of mouse HDAC6 expressed in 293T cells, IC50 = 0.0028 μM. 17881232
293T Function assay Inhibition of HDAC1 expressed in 293T cells, IC50 = 0.19 μM. 17900911
293T Function assay Inhibition of HDAC4 expressed in 293T cells, IC50 = 0.2 μM. 17900911
293T Function assay Inhibition of HDAC6 expressed in 293T cells, IC50 = 0.28 μM. 17900911
NIH3T3 Function assay Inhibition of human recombinant HDAC1 expressed in NIH3T3 cells, IC50 = 0.021 μM. 17929798
human 293 Function assay Inhibition of human recombinant HDAC4 expressed in 293 cells, IC50 = 0.034 μM. 17929798
mouse 293 Function assay Inhibition of mouse recombinant HDAC6 expressed in 293 cells, IC50 = 0.081 μM. 17929798
SKBR3 Antiproliferative assay Antiproliferative activity against human SKBR3 cells, IC50 = 0.02 μM. 18247554
MM96L Function assay Inhibition of human MM96L cells, IC50 = 0.03 μM. 18247554
SNU16 Function assay Inhibition of HDAC from human SNU16 cells, IC50 = 0.053 μM. 18247554
A549 Antiproliferative assay Antiproliferative activity against human A549 cells, IC50 = 0.08 μM. 18247554
MKN45 Antiproliferative assay Antiproliferative activity against human MKN45 cells, IC50 = 0.1 μM. 18247554
SQ20B Function assay Inhibition of human SQ20B cells, IC50 = 0.2 μM. 18247554
neonatal foreskin fibroblasts Growth inhibition assay Growth inhibition of human neonatal foreskin fibroblasts cells, IC50 = 0.2 μM. 18247554
HeLa Function assay Inhibition of HDAC from human HeLa cells, IC50 = 0.3 μM. 18247554
MM96L/NFF Function assay Selectivity index, ratio of IC50 for human MM96L cells to IC50 for human NFF cells, IC50 = 6.7 μM. 18247554
293T Function assay Inhibition of human HDAC1 expressed in 293T cells, IC50 = 0.0366 μM. 18397826
293T Function assay Inhibition of human HDAC4 expressed in 293T cells, IC50 = 0.0629 μM. 18397826
293T Function assay Inhibition of human HDAC6 expressed in 293T cells, IC50 = 0.0833 μM. 18397826
HeLa Function assay Inhibition of human HDAC in HeLa cells by flour de lys assay, IC50 = 0.005 μM. 18397827
S2 Function assay Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells, IC50 = 0.0006 μM. 19317450
NIH3T3 Function assay Inhibition of HDAC1 in human NIH3T3 cells by radiometric histone deacetylation assay, IC50 = 0.006 μM. 19457659
HeLa Function assay Inhibition of HDAC from human HeLa cells by fluorogenic enzyme assay, IC50 = 0.3 μM. 19457659
ML1 Antitumor assay Antitumor activity against mouse ML1 cells, IC50 = 0.25 μM. 19534534
Sf9 Function assay Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.0009 μM. 23905680
Sf9 Function assay Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.005 μM. 23905680
Sf9 Function assay Inhibition of human recombinant HDAC2 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.005 μM. 23905680
Sf9 Function assay Inhibition of human recombinant HDAC10 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.009 μM. 23905680
Sf9 Function assay Inhibition of human recombinant HDAC11 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.0173 μM. 23905680
Sf9 Function assay Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate, IC50 = 0.129 μM. 23905680
insect cell Function assay Inhibition of human recombinant N-terminal His-tagged HDAC11 (1 to 347 residues) expressed in insect cells/baculovirus expression system using RHK-K(Ac)-AMC as substrate by fluorescence assay, IC50 = 0.01137 μM. 27060764
NFF Cytotoxicity assay Cytotoxicity against human NFF cells, IC50 = 0.2 μM. 30245402
insect cell Function assay Inhibition of N-terminal GST-tagged recombinant human HDAC6 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay, IC50 = 0.0085 μM. 30365892
Sf21 Function assay Inhibition of C-terminal FLAG-His-tagged full length recombinant human HDAC1 expressed in Sf21 insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay, IC50 = 0.0094 μM. 30365892
insect cell Function assay Inhibition of recombinant human HDAC3/NCOR2 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay, IC50 = 0.0127 μM. 30365892
insect cell Function assay Inhibition of C-terminal GST-tagged recombinant human HDAC2 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay, IC50 = 0.0267 μM. 30365892
insect cell Function assay Inhibition of C-terminal His-tagged recombinant human HDAC8 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay, IC50 = 0.609 μM. 30365892
A20 Function assay Binding affinity towards HDAC1 (Histone deacetylase 1) in mouse A20 cells, expressed as binding constant (pKi), Ki = 0.001072 μM. 11960489
Hela Function assay Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay, Ki = 0.504 μM. 19520580
insect cell Function assay Inhibition of recombinant human HDAC10 expressed in baculovirus-infected insect cells using fluorogenic peptide RHKKAc as substrate by fluorimeter, Ki = 0.00476 μM. 29589441
insect cell Function assay Inhibition of recombinant human N-terminal His-tagged HDAC11 (1 to 347 residues) expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate by fluorimeter, Ki = 0.401 μM. 29589441
HCT116 Function assay Inhibition of human HDAC1 assessed as histone hyperacetylation in human HCT116 cells by Western blot 18054239
HCT116 Function assay Inhibition of human HDAC6 assessed as tubulin hyperacetylation in human HCT116 cells by Western blot 18054239
HeLa Function assay Inhibition of HDAC6 in human HeLa cells assessed as tubulin acetylation incubated for overnight by immunofluorescence microscopic analysis 26611919
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生物活性

產(chǎn)品描述 TSA (Trichostatin A) 是一種HDAC抑制劑，無細(xì)胞試驗中IC50為1.8 nM左右。
靶點(diǎn)
HDAC [1]
(Cell-free assay)
~1.8 nM
體外研究(In Vitro)
體外研究活性 Trichostatin A 抑制八種乳腺癌細(xì)胞系，包括MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, 和 SK-BR-3增殖，平均IC50為124.4 nM (范圍為26.4-308.1 nM),作用于表達(dá)ERα的細(xì)胞系比作用于表達(dá) ERα陰性的細(xì)胞系更有效。Trichostatin A作用于全部乳腺癌細(xì)胞系，抑制HDAC活性，平均IC50為 2.4 nM (范圍為0.6-2.6 nM), 產(chǎn)生顯著的組蛋白 H4高度乙?；?。[1]與 Trapoxin (TPX) 和 Chlamydocin 有效抑制HDAC1 或 HDAC4而不是 HDAC6不同，Trichostatin A 抑制這些HDACs，且抑制程度相似， IC50 分別為6 nM, 38 nM, 和8.6 nM。[2] Trichostatin A (100 ng/mL) 作用于MIA PaCa-2細(xì)胞，通過招募p300和 PCAF進(jìn)入Sp1-NF-Y HDAC復(fù)合體，而誘導(dǎo)轉(zhuǎn)化生長因子βⅡ型受體(TβRII) 表達(dá)，復(fù)合體與TβRII 啟動子的DNA片段結(jié)合，伴隨著Sp1乙?；遗c復(fù)合體相關(guān)的HDAC數(shù)理全部降低。[4]
激酶實(shí)驗 體外HDAC活性
從每種乳腺癌細(xì)胞系(MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51,或 SK-BR-3)中準(zhǔn)備全部細(xì)胞提取物。在溶于0.1% (v/v)乙醇的不同濃度Trichostatin A存在時，或者使用0.1% (v/v)乙醇作為對照, 20 μL 細(xì)胞粗提取物(~2.5 ×105 個細(xì)胞)與 1 μL ~1.5 × 106 cpm [3H]乙酰標(biāo)記的組蛋白 H4 肽底物(第2-20位NH2-末端殘基) 在25oC下溫育60分鐘。使用50 μL 1 M HCl/0.16 M 乙酸對每組 200-μL 反應(yīng)進(jìn)行淬火，然后使用600 μL 乙酸乙酯進(jìn)行抽提，通過閃爍計數(shù)器測量釋放的[3H]乙酸。使用非線性回歸曲線擬合抑制數(shù)據(jù)，繪制合適的劑量反應(yīng)曲線，而測定IC50。
細(xì)胞實(shí)驗 細(xì)胞系 MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, 和 SK-BR-3
濃度 溶于無水酒精,終濃度為~10 μM
孵育時間 96小時
方法 使用不同濃度Trichostatin A處理細(xì)胞96小時。處理后,使用sulforhodamine B 比色分析測定細(xì)胞增殖。通過臺酚藍(lán)染色排除法測定細(xì)胞活力。
實(shí)驗圖片 檢測方法 檢測指標(biāo) 實(shí)驗圖片 PMID
Western blot EGFR / STAT3 Cyclin D1 / CDK6 / CDK4 / p-RB / RB MMP-1 / MMP-3 / MMP-13 / TIMP-1 Acetyl-H3 (Lys27) / H3 (96C10) / Acetyl-H4(Lys8) / H4(L64C1) α-H3Ac / α-H4Ac / α-H3K9Ac / α-H3K9 S10 / α-H3K4 me / α-H3K4 me2 / α-H3K9 me2 31289542
Immunofluorescence α-C/EBPβ / α-HP1α α-HDAC1 α-tubulin / acetylated histone 3 21122806
Growth inhibition assay Cell viability (A549 cells) Cell viability (MDA-MB-231 cells) Cell viability (PC3 cells) 27571418
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Administration of Trichostatin A 按 0.5 mg/kg 劑量處理N-甲基-N-亞硝基脲致癌物誘發(fā)的大鼠乳腺癌模型，持續(xù)處理4周，具有有效的抗癌活性，即使按按高達(dá)5 mg/kg劑量處理也沒有任何可測量到的毒性。[1]Trichostatin A 按10 mg/kg 劑量單獨(dú)腹腔注射給藥非轉(zhuǎn)基因和脊髓性肌萎縮癥（SMA）模型鼠，導(dǎo)致乙?；?H3 和 H4組蛋白水平提高，也導(dǎo)致活運(yùn)動神經(jīng)元(SMN) 基因表達(dá)稍微提高。Trichostatin A 每天按10 mg/kg劑量處理SMA模型鼠，促進(jìn)存活, 減輕體重下降,且增強(qiáng)運(yùn)動行為。[5]
動物實(shí)驗 Animal Models 攜帶NMU誘導(dǎo)的腫瘤的近交系(Ludwig/Wistar/Olac)處女鼠
Dosages ~5 mg/kg/day
Administration 皮下注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05355363 Recruiting
Colorectal Cancer|Colon Adenoma
Centre hospitalier de l''Université de Montréal (CHUM)
 February 27 2023 Not Applicable
NCT05414890 Recruiting
NMO Spectrum Disorder|NMDA-R Encephalitis|Diagnostic Self Evaluation|Immune System Diseases|Nervous System Diseases|Autoimmune Diseases of the Nervous System|Autoimmune Diseases
Beijing Tiantan Hospital|Tianjin Medical University General Hospital
 June 30 2022 --
NCT05271955 Not yet recruiting
Autism Spectrum Disorder
Assistance Publique - H?pitaux de Paris|University Hospital Montpellier
 June 15 2022 Not Applicable
NCT04606771 Active not recruiting
Non-Small Cell Lung Cancer
AstraZeneca
 September 28 2020 Phase 2
NCT03877510 Completed
Parkinson Disease
Impax Laboratories LLC
 April 3 2019 Phase 3

化學(xué)信息&溶解度

分子量 302.4 分子式

C17H22N2O3
CAS號 58880-19-6 SDF Download TSA (Trichostatin A) SDF
Smiles CC(C=C(C)C=CC(=O)NO)C(=O)C1=CC=C(C=C1)N(C)C
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 60 mg/mL ( (198.41 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實(shí)驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實(shí)驗信息（考慮到實(shí)驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 1:
I would like to obtain the enantiomers of TSA, as separate chemicals: R-TSA and S-TSA. Do you have any ideas?

回答：
Our S1045 Trichostatin A (TSA) is R enantiomer.

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