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Azacitidine (5-Azacytidine)

別名: 5-AzaC,Ladakamycin, AZA,5-Aza, CC-486,NSC 102816,5-Azacytidine 中文名稱：氮胞苷, 5-氮胞苷

Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) 是胞苷的核苷類似物，通過捕獲DNA甲基轉(zhuǎn)移酶，特異性抑制DNA甲基化。Azacitidine可誘導(dǎo)線粒體凋亡與自噬。

Azacitidine (5-Azacytidine) Chemical Structure

Azacitidine (5-Azacytidine) Chemical Structure

CAS: 320-67-2

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1057.59 現(xiàn)貨
10mg 548.73 現(xiàn)貨
50mg 788.76 現(xiàn)貨
200mg 2212.28 現(xiàn)貨
1g 5487.3 現(xiàn)貨
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常與Azacitidine (5-Azacytidine)一起在實(shí)驗(yàn)中被使用的化合物

Venetoclax (ABT-199)

Azacitidine和Venetoclax聯(lián)合治療可顯著降低從急性髓系白血病(AML)患者分離的白血病細(xì)胞中的OXPHOS水平。

Pollyea DA, et al. Nat Med. 2018 Dec;24(12):1859-1866.

Decitabine

Azacitidine和Decitabine在基因組重排過程中誘導(dǎo)序列元件去甲基化，導(dǎo)致外接合體細(xì)胞中重復(fù)元件增加。

Bracht JR, et al. Genome Biol. 2012 Oct 17;13(10):R99.

Linifanib (ABT-869)

Azacitidine和Linifanib組成的cocktail可將成纖維細(xì)胞轉(zhuǎn)化為上皮樣細(xì)胞，并激活OCT4。

Abbey D, et al. Cell Regen. 2022 Aug 3;11(1):27.

UNC0379

Azacitidine抑制PC9/ER和HCC827/ER細(xì)胞的細(xì)胞生長，而UNC0379對這兩種細(xì)胞系的細(xì)胞生長沒有顯著影響。

Wang L, et al. Cell Death Dis. 2018 Jan 26;9(2):129.

Azacitidine (5-Azacytidine)相關(guān)產(chǎn)品

相關(guān)信號通路圖

DNA Methyltransferase Signaling Pathways

DNA Methyltransferase信號通路圖

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 孵育時間 活性描述 文獻(xiàn)信息
OCM1 Function Assay 0.5/1 μM 48 h causes global DNA hypomethylation at L-1 repeat loci 25146981
92.1 Cell Viability Assay 0.5/1 μM 5 d decreases radiation-induced cell viability inhibition 25146981
OCM1 Cell Viability Assay 0.5/1 μM 5 d decreases radiation-induced cell viability inhibition 25146981
OMM1 Function Assay 0.5/1 μM 48 h decreases invasion dose dependently? 25146981
Mel 290 Function Assay 0.5/1 μM 48 h decreases invasion dose dependently? 25146981
OCM3 Function Assay 0.5/1 μM 48 h decreases invasion dose dependently? 25146981
Mel 290 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
Mel 285 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
OMM1 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
OCM1 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
92.1 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
OCM3 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
Mel 290 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
Mel 285 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
OMM1 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
OCM1 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
92.1 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
OCM3 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
CP70 Function Assay 5 μM? 7 d weakens the level of methylation 25299694
A2780 Function Assay 5 μM? 7 d weakens the level of methylation 25299694
CP70 Function Assay 5 μM? 7 d increases DNA methylation level 25299694
A2780 Function Assay 5 μM? 7 d increases DNA methylation level 25299694
MV4-11 Function Assay 5 μM 72 h significantly upregulates ZNF382 expression 25319049
HL-60 Function Assay 5 μM 72 h significantly upregulates ZNF382 expression 25319049
MSCs Function Assay 10 μM 24 h promotes the commitment of MSCs to myocardial differentiation 25351395
HRPE Function Assay 5/10?μM 48 h down-regulates of VEGF, IL-1β, and MMP2 dose-dependently 25352747
HREC Function Assay 5/10?μM 48 h down-regulates of VEGF, ICAM-1 (not protein level in HRPE cells), IL-1β dose-dependently 25352747
HRPE Function Assay 5/10?μM 48 h induces PEDF in a dose-dependent manner 25352747
HREC Function Assay 5/10?μM 48 h induces PEDF in a dose-dependent manner 25352747
MKN45 Function Assay 5?μM 72 h decreases the mRNA expression of PRL-3 significantly 25475733
SGC-7901 Function Assay 5?μM 72 h decreases the mRNA expression of PRL-3 significantly 25475733
MKN28 Function Assay 5?μM 72 h decreases the mRNA expression of PRL-3 significantly 25475733
BGC-823 Function Assay 5?μM 72 h decreases the mRNA expression of PRL-3 significantly 25475733
MKN45 Function Assay 5?μM 72 h decreases the PRL-3 protein level signifcantly 25475733
SGC-7901 Function Assay 5?μM 72 h decreases the PRL-3 protein level signifcantly 25475733
MKN28 Function Assay 5?μM 72 h decreases the PRL-3 protein level signifcantly 25475733
BGC-823 Function Assay 5?μM 72 h decreases the PRL-3 protein level signifcantly 25475733
MCF7 Growth Inhibition Assay 0.3 μM? 4 d decreases the cell growth 24.8% combined with GSK126 25477340
PC3 Growth Inhibition Assay 0.2 μM? 4 d decreases the cell growth to 20.3% combined with GSK126 25477340
MCF7 Function Assay 0.3 μM? 4 d increases the gene expression of IGFBP7, SFRP1 and SLC6A15 combined with GSK126 25477340
PC3 Function Assay 0.2 μM? 4 d increases the gene expression of IGFBP7, SFRP1 and SLC6A15 combined with GSK126 25477340
A253 Function Assay 10 μM 0-4 d reduces the 5-methylcytosine content 25485536
A253 Function Assay 10 μM 72 h increases the expression level of the M3R in both membrane and cytosolic preparations 25485536
A253 Function Assay 10 μM 0-4 d increases the mRNA expression level of the M3R?after 24 h 25485536
Ketr-3 Function Assay 10 μM 72 h induces the ADAMTS18 gene expression 25569086
CaKI-2 Function Assay 10 μM 72 h induces the ADAMTS18 gene expression 25569086
A498 Function Assay 10 μM 72 h induces the ADAMTS18 gene expression 25569086
MDA-MB-231? Function Assay 1/2.5/5 μM 24/48 h increases the expression of miRNA-124 at the concerntration of 5 μM 25817229
MCF-7 Function Assay 1/2.5/5 μM 24/48 h increases PARP cleavage? 25817229
MDA-MB-231 Function Assay 1/2.5/5 μM 24/48 h induces significant PARP cleavage after 48 h 25817229
MDA-MB-231 Function Assay 1/2.5/5 μM 48 h increases the levels of E-cadherin mRNA at the concerntration of 2.5?μMfor 48?h 25817229
MDA-MB-231 Function Assay 1/2.5/5 μM 48 h decreases the PTPN12 expression at the concerntration of 5?μM 48?h 25817229
Jurkat? Function Assay 3.5?μM 48 h increases?PTPL1?mRNA expression 26133246
Raji? Function Assay 15?μM 48 h increases?PTPL1?mRNA expression 26133246
CA46 Function Assay 20?μM 48 h increases?PTPL1?mRNA expression 26133246
Jurkat? Growth Inhibition Assay 0.1-50 μM 12-72 h inhibits cell growth in a dose dependent manner 26133246
Raji? Growth Inhibition Assay 0.1-50 μM 12-72 h inhibits cell growth in a dose dependent manner 26133246
OCM3 Function Assay 0.5/1 μM 48 h causes global DNA hypomethylation at L-1 repeat loci 25146981
92.1 Function Assay 0.5/1 μM 48 h causes global DNA hypomethylation at L-1 repeat loci 25146981
IMR32 Function Assay 3 μM 72 h induces?p19-INK4d?expression?significantly 25104850
IMR5-75 Function Assay 3 μM 72 h induces?p19-INK4d?expression?significantly 25104850
Be(2)-C Function Assay 3 μM 72 h induces?p19-INK4d?expression?significantly 25104850
Bxpc-3 Growth Inhibition Assay 5/10 μM 24/48/72 h inhibits the proliferation of Bxpc-3 cells in time- and concentration-dependent manners 25061731
Bxpc-3 Apoptosis Assay 5/10 μM 24/48/72 h induces apoptosis in time- and concerntration manners 25061731
Bxpc-3 Function Assay 5/10 μM 24/48/72 h decreases β-catenin expression after 24 h 25061731
Bxpc-3 Function Assay 5/10 μM 24/48/72 h decreases cyclinD1 expression at the concerntration of 10 μM 25061731
Bxpc-3 Function Assay 5/10 μM 24/48/72 h down-regulateS c-myc mRNA expression in time- and concentration-dependent manners 25061731
HL-60 Growth Inhibition Assay 1.0 μM 48 h significantly inhibits HL-60 cell growth? 25051119
HL-60 Function Assay 1.0 μM 48 h increases p21WAF1/CIP1?and caspase-3 expression? 25051119
HL-60 Function Assay 1.0 μM 48 h decreases Bcl-xL expression?significantly 25051119
HuTu-80? Function Assay 1/5/10 μM 48/72 h increases the expression of human NPC1L1 mRNA in a dose-dependent manner 24904062
Caco2? Function Assay 10 μM 48 h increases NPC1L1 expression 24904062
HepG2? Function Assay 0-25 μM 24 h decreases subtilisin/kexin type 9 (PCSK9) protein levels dose dependently 24855646
HepG2? Function Assay 0-25 μM 24 h increases low density lipoprotein receptor (LDLR) gene expression? 24855646
HepG2? Function Assay 10 μm? 0-24 h decreases?PCSK9?and?HMGCR?expression and increases LDLR expression after 6 h 24855646
HepG2? Function Assay 10 μm 24 h promotes cytosolic neutral lipid accumulation independently of exogenous lipoproteins 24855646
HepG2? Function Assay 10 μm 24 h prevents SREBP processing 24855646
HC45? Function Assay 5μM? 4 d reduces the methylation levels of WIF1, P16, CXCL14, NKX2–3, CDH1, LAMA1, and CTNNB1 24762809
CNDT2? Function Assay 5μM? 4 d reduces the methylation levels of WIF1, P16, CXCL14, NKX2–3, CDH1, LAMA1, and CTNNB1 24762809
CNDT2? Function Assay 5μM? 4 d increases gene expression of?WIF1, P16, CDH1,?LAMA1,?and?CTNNB1 24762809
T-cells Growth Inhibition Assay 5/20 μM 0-48 h inhibits cell growth in a dose dependent manner 24757283
CD3+ T-cells Function Assay 5/20 μM 48 h upregulates p15 expression 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h upregulates p15 expression 24757283
CD8+ T-cells Function Assay 5/20 μM 48 h upregulates p15 expression 24757283
CD3+ T-cells Function Assay 5/20 μM 48 h upregulates the expression of FOXP3 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h upregulates the expression of FOXP3 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h reduces TBET1?mRNA expression 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h upregulates the expression of?RORγt? 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h inhibits memory T-cells 24757283
CD8+ T-cells Function Assay 5/20 μM 48 h inhibits memory T-cells 24757283
CD3+ T-cells Function Assay 5 μM 48 h reduces long-term memory cell phenotype 24757283
U937 Apoptosis Assay 10 μM 72 h induces apoptosis significantly 24680865
HL-60 Apoptosis Assay 10 μM 72 h induces apoptosis significantly 24680865
MCF7 Function Assay 5 μM 48 h? displays selective toxicity toward suspended MCF-7 cells 24633350
MCF7 Function Assay 10 μM 24 h? induces the cleavage of caspase 7 and PARP? 24633350
MCF7 Function Assay 0–0.5 μM? 7 d inhibits the growth MCF-7 tumorspheres in suspension cultures? 24633350
MCF7 Function Assay 0.5 μM? 14 d reduces the size of MCF-7 colonies embedded in soft agar 24633350
MCF7 Function Assay 0.05–20 μM 1 d reduces the clonal survival of MCF-7 cells in monolayer cultures 24633350
T47D? Function Assay 0.5 μM 4 d inhibits tumorsphere formation 24633350
MCF7 Function Assay 0.5–10 μM 48 h? inhibits the gap closure in the wound healing assay 24633350
MCF7 Function Assay 0/10 μM 24 h inhibits the activity of MMP9 24633350
MDA-MB-231? Function Assay 0.5–10 μM 36 h inhibits the migration 24633350
U373-MAGI Antiviral assay 25 to 400 uM 2 to 72 hrs Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in gag level at 25 to 400 uM after 2 to 72 hrs by qPCR method 27117260
U373-MAGI Antiviral assay 25 to 400 uM 2 to 72 hrs Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in U5-gag level at 25 to 400 uM after 2 to 72 hrs by qPCR method 27117260
MCF7 Function assay 15 uM 72 hrs Inhibition of UHRF1 in human MCF7 cells assessed as decrease in methylation at RAR beta exon at 15 uM after 72 hrs by methylation specific-PCR method 27049577
SKM1-S Apoptosis assay 1 uM Induction of apoptosis in human SKM1-S cells assessed as caspase 3 cleavage at 1 uM by Western blot method 28094938
SKM1-S Antiproliferative assay 48 hrs Antiproliferative activity against human SKM1-S cells after 48 hrs by XTT assay, IC50 = 0.5 μM. 28094938
SKM1-S Antiproliferative assay 48 hrs Antiproliferative activity against human SKM1-S cells after 48 hrs by DAPI-staining-based flow cytometric method, EC50 = 0.51 μM. 28094938
A427 Antiproliferative assay 96 hrs Antiproliferative activity against human A427 cells after 96 hrs by crystal violet assay, IC50 = 0.63 μM. 18434163
KYSE70 Antiproliferative assay 96 hrs Antiproliferative activity against human KYSE70 cells after 96 hrs by crystal violet assay, IC50 = 1.59 μM. 18434163
5637 Antiproliferative assay 96 hrs Antiproliferative activity against human 5637 cells after 96 hrs by crystal violet assay, IC50 = 1.73 μM. 18434163
HT-29 Antiproliferative assay 96 hrs Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay, IC50 = 3.8 μM. 2778449
P388 Antiproliferative assay 48 hrs Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay, IC50 = 5 μM. 2778449
MCF7 Antiproliferative assay 96 hrs Antiproliferative activity against human MCF7 cells after 96 hrs by crystal violet assay, IC50 = 6.78 μM. 18434163
L1210 Cytotoxicity assay Cytotoxicity against mouse L1210 cells assessed as cessation of growth 69026
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
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生物活性

產(chǎn)品描述 Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) 是胞苷的核苷類似物，通過捕獲DNA甲基轉(zhuǎn)移酶，特異性抑制DNA甲基化。Azacitidine可誘導(dǎo)線粒體凋亡與自噬。
靶點(diǎn)
DNA methyltransferase [1]
(Cell-free assay)
體外研究(In Vitro)
體外研究活性

Azacitidine廣泛地被用于證明特定基因區(qū)域的甲基化損失與相關(guān)基因的激活之間的相關(guān)性。Azacitidine進(jìn)入到DNA后，非競爭性抑制DNA甲基化，在新復(fù)制的DNA中抑制胞嘧啶甲基化，而對休息不分裂的細(xì)胞沒有抑制作用。[1] Azacitidine誘導(dǎo)血友病紅細(xì)胞白血病細(xì)胞C3H10T1/2的分化，且誘導(dǎo)肌管形成。[2]Azacitidine作用于正常的真核細(xì)胞和癌細(xì)胞中，可激活核苷三磷酸，并進(jìn)入DNA和RNA，抑制DNA，RNA和蛋白合成，最終導(dǎo)致細(xì)胞死亡。Azacitidine也抑制嘌呤代謝產(chǎn)物滲透到大分子中。Azacitidine抑制 L1210 細(xì)胞生長，IC50為 0.019 μg/mL [3]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 白血病 L1210細(xì)胞
濃度 0.15 μg/mL
孵育時間 3 天
方法

5 mL L1210 細(xì)胞(5×103cells/mL) 與藥物在37°C下溫育3天。使用Model A Coulter血球計(jì)數(shù)儀測定細(xì)胞數(shù)，沒有測定兩次，持續(xù)測定3天。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot DNMT1

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