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Staurosporine (STS)

別名: AM-2282，Antibiotic AM-2282 中文名稱：星形孢菌素

Staurosporine (STS)是一種有效的PKC抑制劑，在無細(xì)胞試驗(yàn)中作用于PKCα，PKCγ 和PKCη，IC50分別為2 nM，5 nM 和 4 nM，對(duì)PKCδ(20 nM)和PKCε(73 nM)作用較弱，對(duì)PKCζ (1086 nM)的活性很低。同時(shí) 對(duì)其他的激酶PKA, PKG, S6K, CaMKII, 等也顯示抑制活性。Phase 3。

Staurosporine (STS) Chemical Structure

Staurosporine (STS) Chemical Structure

CAS: 62996-74-1

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 1777.23 現(xiàn)貨
2mg 794.43 現(xiàn)貨
5mg 1466.01 現(xiàn)貨
25mg 4398.03 現(xiàn)貨
1g 54946.71 現(xiàn)貨
更大包裝 有超大折扣

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常與Staurosporine (STS)一起在實(shí)驗(yàn)中被使用的化合物

5-FU (5-Fluorouracil)

Staurosporine和5-FU聯(lián)合使用對(duì)Lovo B2細(xì)胞的凋亡誘導(dǎo)作用高2倍。

Sigmond J, et al. Nucleosides Nucleotides Nucleic Acids. 2004 Oct;23(8-9):1503-6.

Oxaliplatin

Staurosporine和Oxaliplatin的使用導(dǎo)致DAPI+細(xì)胞在人非小細(xì)胞肺癌A549細(xì)胞中積累。

Sauvat A, et al. Oncotarget. 2015 Apr 20;6(11):9467-75.

Prostaglandin E2 (PGE2)

Staurosporine和Prostaglandin E2處理增強(qiáng)了人CD34+的轉(zhuǎn)導(dǎo)，增加了人短期NSG再生細(xì)胞的轉(zhuǎn)導(dǎo)。

Lewis G, et al. Mol Ther Methods Clin Dev. 2018 Apr 5;9:313-322.

Retinoic acid (Tretinoin)

Staurosporine和Retinoic acid聯(lián)用可誘導(dǎo)NB4-R1/NB4-R2細(xì)胞的粒細(xì)胞分化并抑制其增殖。

Ge DZ, et al. Sci Rep. 2014 Apr 28;4:4821.

Z-VAD-FMK

Z-VAD-FMK抑制Staurosporine誘導(dǎo)的SJG2/MT330細(xì)胞死亡。

Wang R, et al. Biochem Biophys Res Commun. 2016 Sep 9;478(1):128-134.

Staurosporine (STS)相關(guān)產(chǎn)品

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
HepG2 cells Cytotoxicity assay 100 uM 3 days Cytotoxicity against human HepG2 cells at 100 uM after 3 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.018 μM. 28993106
Sf21 cells Function assay 30 uM Inhibition of human CHK2 kinase expressed in insect Sf21 cells using phospho-CREBtide as substrate at 30 uM, IC50 = 0.027 μM. 21334796
Sf21 cells Function assay 30 uM Inhibition of human recombinant IKK-alpha expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.039 μM. 21334796
Sf21 cells Function assay 30 uM Inhibition of human recombinant IKK-beta expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.49 μM. 21334796
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0024 μM. 18484775
Sf9 cells Function assay 20 mins Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 100 umol/L ATP, IC50 = 0.51 μM. 17315853
Sf9 cells Function assay 1 min Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 100 umol/L ATP, IC50 = 0.27 μM. 17315853
Sf9 cells Function assay 20 mins Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 10 umol/L ATP, IC50 = 0.083 μM. 17315853
Sf9 cells Function assay 1 min Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 10 umol/L ATP, IC50 = 0.036 μM. 17315853
Sf9 cells Function assay 20 mins Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 1 umol/L ATP, IC50 = 0.015 μM. 17315853
Sf9 cells Function assay 1 min Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 1 umol/L ATP, IC50 = 0.005 μM. 17315853
human PBMC Function assay 24 h Suppression of IL2 production in human PBMC after 24 hrs by ELISA, IC50=16 nM. 18585046
MDA-MB-231 cells Cytotoxicity assay 72 h Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0071 μM. 18484775
HT29 cells Cytotoxicity assay 72 h Cytotoxicity against human HT29 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0109 μM. 18484775
HT-29 cells Apoptosis assay 2 h Induction of apoptosis in human HT-29 cells assessed as change in mitochondrial transmembrane potential after 2 hrs by JC1 staining based fluorescence assay, ED50 = 0.0026 μM. 19422206
HUE cells Function assay 90 mins Inhibition of VEGFR2 in HUE cells assessed as inhibition of VEGF-induced autophosphorylation treated for 90 mins before VEGF challenge by ELISA, IC50 = 0.07 μM. 20170163
Sf9 cells Function assay 60 mins Inhibition of human recombinant GST-fused NIK expressed in Sf9 cells after 60 mins by radiometric protein kinase assay, IC50 = 2.3 μM. 20580552
HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM. 21388191
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM. 21388191
HT-29 cells Function assay 2 h Effect on mitochondrial membrane potential in human HT-29 cells after 2 hrs using JC-1 staining by fluorescence assay, IC50 = 0.002 μM. 21428375
HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM. 21488655
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM. 21488655
SF268 cells Cytotoxicity assay 48 h Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50 = 0.044 μM. 21513294
CHOK1 cells Cytotoxicity assay 48 h Cytotoxicity against human CHOK1 cells after 48 hrs by SRB assay, GI50 = 0.13 μM. 21513294
H460 cells Cytotoxicity assay 48 h Cytotoxicity against human H460 cells after 48 hrs by SRB assay, GI50 = 3.6 μM. 21513294
HT-29 cells Cytotoxicity assay 48 h Cytotoxicity against human HT-29 cells after 48 hrs by SRB assay, GI50 = 3.6 μM. 21513294
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 11 μM. 21513294
SW1116 cells Function assay 24 h Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.32 μM. 21962523
HT-29 cells Apoptosis assay 2 h Induction of apoptosis in human HT-29 cells assessed reduction of mitochondrial membrane potential after 2 hrs by using JC1 staining by fluorescence cell-based assay, ED50 = 0.0026 μM. 21973101
LoVo cells Antiproliferative activity assay 48 to 72 h Antiproliferative activity against human LoVo cells after 48 to 72 hrs by MTT assay, IC50 = 0.001 μM. 22182929
ST486 cells Antiproliferative activity assay 48 to 72 h Antiproliferative activity against human ST486 cells after 48 to 72 hrs by MTT assay, IC50 = 0.007 μM. 22182929
DLD1 cells Antiproliferative activity assay 48 to 72 h Antiproliferative activity against human DLD1 cells after 48 to 72 hrs by MTT assay, IC50 = 0.009 μM. 22182929
B16F10 cells Antiproliferative activity assay 48 h Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 2.82 μM. 22503364
MCF7 cells Antiproliferative activity assay 48 h Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 3.07 μM. 22503364
A431 cells Cytotoxicity assay 24 h Cytotoxicity against human A431 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.07 μM. 22541051
MCF7 cells Cytotoxicity assay 24 h Cytotoxicity against human MCF7 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.18 μM. 22541051
BJ cells Cytotoxicity assay 72 h Cytotoxicity against human BJ cells after 72 hrs by Calcein AM assay, IC50 = 0.002 μM. 22921081
CEM cells Cytotoxicity assay 72 h Cytotoxicity against human CEM cells after 72 hrs by Calcein AM assay, IC50 = 0.023 μM. 22921081
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by Calcein AM assay, IC50 = 0.064 μM. 22921081
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by Calcein AM assay, IC50 = 0.175 μM. 22921081
HepG2 cells Function assay 24 h Inhibition of telomerase in human HepG2 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.14 μM. 23018096
SW1116 cells Antiproliferative activity assay 48 h Antiproliferative activity against human SW1116 cells after 48 hrs by MTT method, IC50 = 4.95 μM. 23018096
HepG2 cells Antiproliferative activity assay 48 h Antiproliferative activity against human HepG2 cells after 48 hrs by MTT method, IC50 = 6.73 μM. 23018096
BGC823 cells Antiproliferative activity assay 48 h Antiproliferative activity against human BGC823 cells after 48 hrs by MTT method, IC50 = 6.83 μM. 23018096
HeLa cells Antiproliferative activity assay 48 h Antiproliferative activity against human HeLa cells after 48 hrs by MTT method, IC50 = 9.12 μM. 23018096
HepG2 cells Function assay 48 h Inhibition of telomerase in human HepG2 cells after 48 hrs by TRAP-PCR-ELISA, IC50 = 8.3 μM. 23279864
SW1116 cells Function assay 24 h Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.18 μM. 24286761
KE-97 cells Cytotoxicity assay 72 h Cytotoxicity against human KE-97 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.13 μM. 24328283
Jurkat cells Cytotoxicity assay 72 h Cytotoxicity against human Jurkat cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.14 μM. 24328283
HuH7 cells Cytotoxicity assay 72 h Cytotoxicity against human HuH7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.23 μM. 24328283
BGC823 cells Cytotoxicity assay 72 h Cytotoxicity against human BGC823 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.38 μM. 24328283
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.52 μM. 24328283
NIH/3T3 cells Cytotoxicity assay 96 h Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
A2780 cells Cytotoxicity assay 96 h Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
HT-29 cells Cytotoxicity assay 96 h Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
8505C cells Cytotoxicity assay 96 h Cytotoxicity against human 8505C cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
518A2 cells Cytotoxicity assay 96 h Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
MCF7 cells Cytotoxicity assay 96 h Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 0.4 μM. 24361521
A549 cells Cytotoxicity assay 96 h Cytotoxicity against human A549 cells after 96 hrs by SRB assay, IC50 = 0.6 μM. 24361521
HEK293 cells Cytotoxicity assay 72 h Cytotoxicity against HEK293 cells after 72 hrs by CellTiterGlo assay, IC50 = 0.056 μM. 24763262
HeLa cells Antiproliferative activity assay 24 to 48 h Antiproliferative activity against human HeLa cells after 24 to 48 hrs by CCK-8 assay, IC50 = 2.72 μM. 24792811
A549 cells Antiproliferative activity assay 24 to 48 h Antiproliferative activity against human A549 cells after 24 to 48 hrs by CCK-8 assay, IC50 = 3.05 μM. 24792811
A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 25825934
HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.025 μM. 25825934
PC3 cells Cytotoxicity assay 48 h Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 0.031 μM. 25825934
MGC-803 cells Function assay 24 h Inhibition of telomerase in human MGC-803 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.97 μM. 26900656
Sf9 insect cells Function assay 10 mins Inhibition of N-terminal GST tagged recombinant full-length human CHK1 expressed in baculovirus Sf9 insect cells after 10 mins by luminescent ADP-Glo assay, IC50 = 0.0012 μM. 27089211
Sf21 cells Function assay 60 mins Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method, IC50 = 0.002 μM. 27137359
Neuro2a cells Cytotoxicity assay 72 h Cytotoxicity against mouse Neuro2a cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0113 μM. 28152427
MDA-MB-231 cells Function assay 16 h Inhibition of retinoblastoma protein phosphorylation in human MDA-MB-231 cells after 16 hrs by Hoechst 33342 staining based fluorescence assay, IC50 = 0.066 μM. 28431342
Sf9 insect cells Function assay 20 mins Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50 = 0.00029 μM. 28482151
HEK293 cells Cytotoxicity assay 72 h Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay, CC50 = 0.00354 μM. 28624701
BT549 cells Cytotoxicity assay 24 h Cytotoxic activity against human BT549 cells incubated for 24 hrs by MTT assay, IC50 = 0.08 μM. 28705432
MDA-MB-468 cells Cytotoxicity assay 24 h Cytotoxic activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay, IC50 = 0.15 μM. 28705432
MDA-MB-231 cells Cytotoxicity assay 24 h Cytotoxic activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay, IC50 = 0.24 μM. 28705432
Vero cells Cytotoxicity assay 2 days Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 2 days by cell-titer-glo luminescent assay, TC50 = 0.0024 μM. 28763645
L929 cells Antiproliferative activity assay 5 days Antiproliferative activity against mouse L929 cells after 5 days by WST-1 assay, IC50 = 0.2 μM. 28956915
KB-3-1 cells Antiproliferative activity assay 5 days Antiproliferative activity against human KB-3-1 cells after 5 days by WST-1 assay, IC50 = 0.2 μM. 28956915
MCF7 cells Antiproliferative activity assay 5 days Antiproliferative activity against human MCF7 cells after 5 days by WST-1 assay, IC50 = 1.8 μM. 28956915
FS4-LTM cells Antiproliferative activity assay 24 h Antiproliferative activity against human FS4-LTM cells after 24 hrs by WST-1 assay, IC50 = 2.8 μM. 28956915
Vero cells Cytotoxicity assay 2 days Cytotoxicity against African green monkey Vero cells after 2 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.0024 μM. 28993106
NIH/3T3 cells Cytotoxicity assay 96 h Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, EC50 = 0.008 μM. 29197730
518A2 cells Cytotoxicity assay 96 h Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, EC50 = 0.03 μM. 29197730
A549 cells Cytotoxicity assay 96 h Cytotoxicity against human A549 cells after 96 hrs by SRB assay, EC50 = 0.04 μM. 29197730
MCF7 cells Cytotoxicity assay 96 h Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, EC50 = 0.1 μM. 29197730
A2780 cells Cytotoxicity assay 96 h Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, EC50 = 0.12 μM. 29197730
HT-29 cells Cytotoxicity assay 96 h Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, EC50 = 0.15 μM. 29197730
insect cells Function assay 30 mins Inhibition of recombinant human PDGFRbeta expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 30 mins by LANCE method, IC50 = 0.00076 μM. 29549836
Sf9 insect cells Function assay 60 mins Inhibition of recombinant human KDR expressed in Sf9 insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.0021 μM. 29549836
insect cells Function assay 10 mins Inhibition of recombinant human Src expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 10 mins by LANCE method, IC50 = 0.005 μM. 29549836
insect cells Function assay 15 mins Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM. 29549836
insect cells Function assay 15 mins Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM. 29549836
Sf9 insect cells Function assay 15 mins Inhibition of recombinant human Flt1 expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 15 mins by LANCE method, IC50 = 0.035 μM. 29549836
Sf21 insect cells Function assay 15 mins Inhibition of recombinant human Aurora-A expressed in Sf21 insect cells using Ulight-RRRSLLE as substrate after 15 mins by LANCE method, IC50 = 0.039 μM. 29549836
insect cells Function assay 60 mins Inhibition of recombinant human AKT1 expressed in insect cells using CREBtide as substrate after 60 mins by LANCE method, IC50 = 0.056 μM. 29549836
Sf9 insect cells Function assay 60 mins Inhibition of recombinant human FAK expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.062 μM. 29549836
insect cells Function assay 60 mins Inhibition of recombinant human ABL expressed in insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.29 μM. 29549836
insect cells Function assay 60 mins Inhibition of recombinant human c-MET expressed in insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.31 μM. 29549836
PC3 cells Cytotoxicity assay 72 h Cytotoxicity against human PC3 cells after 72 hrs by SRB assay, IC50 = 0.039 μM. 29558119
Sf9 cells Function assay 45 mins Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.047 μM. 29902719
Sf9 cells Function assay 45 mins Inhibition of recombinant human N-terminal GST-tagged HER2 (679 to 1255 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.0608 μM. 29902719
HT-29 cells Function assay 3 h Inhibition of mitochondrial membrane potential in human HT-29 cells after 3 hrs by JC-1 staining based fluorescence assay, IC50 = 0.02 μM. 30057155
HCT116 cells Cytotoxicity assay 48 h Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.03 μM. 30106291
Huh7.5 cells Cytotoxicity assay 48 h Cytotoxicity against human Huh7.5 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.6 μM. 30106291
K562 cells Cytotoxicity assay 48 h Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 1.7 μM. 30106291
LO2 cells Cytotoxicity assay 48 h Cytotoxicity against human LO2 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 9.5 μM. 30106291
U937 cells Cytotoxicity assay Cytotoxicity against human U937 cells, IC50 = 2 μM. 17088067
Sf21 cells Function assay Inhibition of JAK3 expressed in Sf21 cells, IC50 = 0.006 μM. 17088059
FL5.12-Akt1 cells Function assay Activity against GSK3 phosphorylation in FL5.12-Akt1 cells, EC50 = 0.46 μM. 16413780
MiaPaCa-2 cells Antiproliferative activity assay Antiproliferative activity against human MiaPaCa-2 cells, IC50 = 0.37 μM. 16413780
FL5.12-Akt1 cells Function assay Activity against GSK3 in FL5.12-Akt1 cells, EC50 = 0.46 μM. 16403626
MiaPaCa-2 cells Antiproliferative activity assay Antiproliferative activity against MiaPaCa-2 cells by MTT assay, IC50 = 0.37 μM. 16403626
FL5.12-Akt1 cells Antiproliferative activity assay Antiproliferative activity against FL5.12-Akt1 cells by MTT assay, IC50 = 0.29 μM. 16403626
P19 cells Function assay Inhibition of Casein kinase 1 in P19 cells, IC50 = 1.4 μM. 15771419
P19 cells Function assay Inhibition of Insulin receptor kinase in P19 cells, IC50 = 0.2 μM. 15771419
HEK293 cells Function assay Inhibition of IL-8 release by HEK293 cells expressing PKC-beta2, IC50 = 0.077 μM. 15771419
P19 cells Function assay Inhibition of Vascular endothelial growth factor receptor in P19 cells, IC50 = 0.014 μM. 15771419
P19 cells Function assay Inhibition of Cyclin-dependent kinase 1 in P19 cells, IC50 = 0.008 μM. 15771419
P19 cells Function assay Inhibition of Calcium/calmodulin-dependent protein kinase type II in P19 cells, IC50 = 0.006 μM. 15771419
P19 cells Function assay Inhibition of Protein Kinase A in P19 cells, IC50 = 0.004 μM. 15771419
P19 cells Function assay Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM. 15771419
P19 cells Function assay Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM. 15771419
HEK293 cells Function assay Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA, IC50 = 0.077 μM. 12941331
DLD-1 cells Antiproliferative activity assay Antiproliferative activity against human colon cancer cell line (DLD-1 cells) using MTT assay, IC50 = 0.009 μM. 11591505
ST-486 cells Antiproliferative activity assay Antiproliferative activity against burkit lymphoma cell line (ST-486 cells) using MTT assay, IC50 = 0.007 μM. 11591505
umbilical vein endothelial cells Antiproliferative activity assay Antiproliferative activity against human umbilical vein endothelial cells (HUVECs) using MTT assay, IC50 = 0.004 μM. 11591505
LoVo cells Antiproliferative activity assay Antiproliferative activity against human colon cancer cell line (LoVo cells) using MTT assay, IC50 = 0.001 μM. 11591505
Sf9 insect cells Function assay Inhibition of protein kinase C(1:1mixture of PKC alpha & beta) expressed in Sf9 insect cells, IC50 = 0.02 μM. 9873605
endothelial cells Function assay Effective dose against plasminogen activator activity stimulated by phorbol ester in endothelial cells, ED50 = 7.5 μM. 8709095
human colon carcinoma cell line HCT116 Function assay Concentration required for growth inhibition of human colon carcinoma cell line HCT116, IC50=6 nM. 15537345
MCF7 cells Function assay Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, Ki = 0.005 μM. 18656369
MCF7 cells Function assay Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, IC50 = 2 μM. 18656369
Sf9 cells Function assay Inhibition of human Syk expressed in Sf9 cells, IC50 = 0.003 μM. 18823784
Sf9 cells Function assay Inhibition of human ZAP70 expressed in Sf9 cells, IC50 = 0.053 μM. 18823784
insect cells Function assay Inhibition of human recombinant Pim1 expressed in insect cells by HTRF, IC50 = 0.01 μM. 19179076
insect Sf21 cells Function assay Inhibition of JAK3 expressed in insect Sf21 cells assessed as inhibition of biotinylated substrate phosphorylation, IC50 = 0.006 μM. 19427203
Jurkat cells Antiproliferative activity assay Antiproliferative activity against JAK3 expressing IL2-stimulated human Jurkat cells, IC50 = 0.071 μM. 19427203
Jurkat cells Antiproliferative activity assay Antiproliferative activity against JAK3 expressing human resting Jurkat cells, IC50 = 0.311 μM. 19427203
HT-29 cells Function assay Inhibition of mitochondrial membrane potential in human HT-29 cells using JC1 dye staining by fluorescence plate reader assay, IC50 = 0.0025 μM. 21513293
HCT116 cells Function assay Inhibition of TNIK-mediated TCF4/beta-casein transcription in human HCT116 cells by beta-lactamase reporter gene assay, IC50 = 0.039 μM. 23232060
V79 MZ cells Function assay Inhibition of human aldosterone synthase expressed in V79 MZ cells assessed as inhibition of aldosterone synthesis, IC50 = 0.011 μM. 24422519
HepG2 cells Cytotoxicity assay Cytotoxicity against human HepG2 cells, EC50 = 2 μM. 25316317
Raji cells Cytotoxicity assay Cytotoxicity against human Raji cells, EC50 = 2 μM. 25316317
BJ cells Cytotoxicity assay Cytotoxicity against human BJ cells, EC50 = 2 μM. 25316317
HEK293 cells Cytotoxicity assay Cytotoxicity against HEK293 cells, EC50 = 2 μM. 25316317
PC3 cells Cytotoxicity assay Cytotoxicity against human PC3 cells by sulforhodamine B assay, IC50 = 0.017 μM. 29389122
HCT116 cells Cytotoxicity assay Cytotoxicity against human HCT116 cells by sulforhodamine B assay, IC50 = 0.055 μM. 29389122
Sf9 cells Function assay Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM. 30067358
Sf9 cells Function assay Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM. 30067358
Sf9 cells Function assay Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM. 30067358
Sf9 cells Function assay Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM. 30067358
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生物活性

產(chǎn)品描述 Staurosporine (STS)是一種有效的PKC抑制劑，在無細(xì)胞試驗(yàn)中作用于PKCα，PKCγ 和PKCη，IC50分別為2 nM，5 nM 和 4 nM，對(duì)PKCδ(20 nM)和PKCε(73 nM)作用較弱，對(duì)PKCζ (1086 nM)的活性很低。同時(shí) 對(duì)其他的激酶PKA, PKG, S6K, CaMKII, 等也顯示抑制活性。Phase 3。
靶點(diǎn)
PKCα [1]
(Cell-free assay)		 c-Fgr [2]
(Cell-free assay)		 phosphorylase kinase [2]
(Cell-free assay)		 PKCη [1]
(Cell-free assay)		 PKCγ [1]
(Cell-free assay)		 點(diǎn)擊更多
2 nM 2 nM 3 nM 4 nM 5 nM
體外研究(In Vitro)
體外研究活性 Staurosporine 也強(qiáng)抑制HeLa S3細(xì)胞，IC50為4 nM。[1]Staurosporine 也抑制多種其他蛋白激酶，包括PKA, PKG, 磷酸激酶, S6 激酶, 肌球蛋白輕鏈激酶(MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, 和Syk ， IC50分別為 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, 和 16 nM。[3] Staurosporine (1 μM) 誘導(dǎo) PC12細(xì)胞90%以上凋亡,這種作用可被過量表達(dá)的Bcl-2抑制,或者zVAD-fmk, cycloheximide (10 μM) 及actinomycin D (5 μM)處理也可抑制。相應(yīng)地, Staurosporine處理，誘導(dǎo)細(xì)胞內(nèi)游離鈣水平 [Ca2+]i快速且持久的提升，線粒體活性氧（ROS）的積累,及 隨后的線粒體功能障礙。[4]通過caspase-8激活和Bid 分裂，功能性caspase-3的表達(dá)可增強(qiáng)Staurosporine誘導(dǎo)MCF7細(xì)胞死亡。[5] 1 μM Staurosporine處理，只部分抑制IL-3刺激的Bcl2 磷酸化，而完全阻斷PKC調(diào)節(jié)的 Bcl2磷酸化。[6] Staurosporine 誘導(dǎo)人類包皮成纖維細(xì)胞AG-1518凋亡,根據(jù)溶酶體組織蛋白酶D調(diào)節(jié)的 細(xì)胞色素 c釋放和 caspase 激活。[7] 除了激活傳統(tǒng)線粒體凋亡通路, Staurosporine觸發(fā)一種新型內(nèi)在凋亡通路, 依賴Apaf-1存在時(shí)對(duì)caspase-9的激活。[8]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 PC12
濃度 溶于DMSO,終濃度為1 μM
孵育時(shí)間 ~32 小時(shí)
方法 使用Staurosporine處理細(xì)胞32小時(shí)。細(xì)胞在4%多聚甲醛中混合，然后使用DNA結(jié)合染料Hoechst 33342染色。在熒光照明下觀察細(xì)胞，測(cè)定凋亡細(xì)胞百分?jǐn)?shù)。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p-Akt / Akt / PARP /Cleaved PARP FAK / RIP Ambra1 24174874
Growth inhibition assay Cell viability 25215174
Immunofluorescence Tubulin / Actin Phalloidin / Type II collagen Pyk2 Annexin cleaved-caspase 3 FAK 4.47 25215174
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 在局部貧血前，使用Staurosporine(0.1-10 ng)預(yù)處理局部貧血沙鼠和大鼠模型，可防止神經(jīng)元損傷，這種作用存在劑量依賴性，說明CAl錐體細(xì)胞死亡涉及PKC。[2]
動(dòng)物實(shí)驗(yàn) Animal Models 短暫局部貧血的雄性Mongolian沙鼠或雄性 Wistar大鼠
Dosages ~10 ng
Administration 定向處理到海馬雙邊CA1子域
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05209347 Withdrawn
Ankle Fractures|Post-traumatic Osteoarthritis|Osteoarthritis Ankle
University of Iowa
 December 2024 Not Applicable
NCT05956990 Not yet recruiting
Colorectal Cancer Survivor|Rehabilitation|Quality of Life
Qu Shen|The First Affiliated Hospital of Xiamen University|Xiamen University
 July 1 2024 Not Applicable
NCT05957289 Not yet recruiting
Rehabilitation|Colorectal Cancer Survivor|Quality of Life|Pilot Study
Qu Shen|The First Affiliated Hospital of Xiamen University|Xiamen University
 June 1 2024 Not Applicable
NCT06245135 Not yet recruiting
Mobility Limitation
University of Toronto|University Health Network Toronto|March of Dimes Canada|Heart and Stroke Foundation of Canada|University of Alberta|University of Manitoba|Bruyere Research Institute
 June 2024 Not Applicable
NCT06374108 Not yet recruiting
Multiple Sclerosis
University of Aarhus|Aarhus University Hospital|University of Copenhagen
 May 1 2024 Not Applicable

化學(xué)信息&溶解度

分子量 466.53 分子式

C28H26N4O3
CAS號(hào) 62996-74-1 SDF Download Staurosporine (STS) SDF
Smiles CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 46 mg/mL ( (98.6 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(qǐng)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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