research use only
Cat.No.S1782
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase |
|---|---|
| Other DNA Methyltransferase Inhibitors | RG108 SGI-1027 Zebularine (NSC 309132) Gamma-Oryzanol GSK3685032 CM272 Bobcat339 β-thujaplicin GSK-3484862 DC-05 |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| Raji | Growth Inhibition Assay | 0.1-50 μM | 12-72 h | inhibits cell growth in a dose dependent manner | 26133246 | |
| Jurkat | Growth Inhibition Assay | 0.1-50 μM | 12-72 h | inhibits cell growth in a dose dependent manner | 26133246 | |
| CA46 | Function Assay | 20 µM | 48 h | increases PTPL1 mRNA expression | 26133246 | |
| Raji | Function Assay | 15 µM | 48 h | increases PTPL1 mRNA expression | 26133246 | |
| Jurkat | Function Assay | 3.5 µM | 48 h | increases PTPL1 mRNA expression | 26133246 | |
| 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 | |
| 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 | 24/48 h | induces significant PARP cleavage after 48 h | 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 | increases the expression of miRNA-124 at the concerntration of 5 μM | 25817229 | |
| A498 | 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 | |
| Ketr-3 | Function Assay | 10 µM | 72 h | induces the ADAMTS18 gene expression | 25569086 | |
| A253 | Function Assay | 10 µM | 0-4 d | increases the mRNA expression level of the M3R after 24 h | 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 | reduces the 5-methylcytosine content | 25485536 | |
| PC3 | Function Assay | 0.2 μM | 4 d | increases the gene expression of IGFBP7, SFRP1 and SLC6A15 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 | Growth Inhibition Assay | 0.2 μM | 4 d | decreases the cell growth to 20.3% combined with GSK126 | 25477340 | |
| MCF7 | Growth Inhibition Assay | 0.3 μM | 4 d | decreases the cell growth 24.8% combined with GSK126 | 25477340 | |
| BGC-823 | 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 | |
| SGC-7901 | Function Assay | 5 μM | 72 h | decreases the PRL-3 protein level signifcantly | 25475733 | |
| MKN45 | Function Assay | 5 μM | 72 h | decreases the PRL-3 protein level signifcantly | 25475733 | |
| BGC-823 | 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 | |
| SGC-7901 | Function Assay | 5 μM | 72 h | decreases the mRNA expression of PRL-3 significantly | 25475733 | |
| MKN45 | Function Assay | 5 μM | 72 h | decreases the mRNA expression of PRL-3 significantly | 25475733 | |
| HREC | Function Assay | 5/10 μM | 48 h | induces PEDF in a dose-dependent manner | 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 | 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 | down-regulates of VEGF, IL-1β, and MMP2 dose-dependently | 25352747 | |
| MSCs | Function Assay | 10 μM | 24 h | promotes the commitment of MSCs to myocardial differentiation | 25351395 | |
| HL-60 | Function Assay | 5 μM | 72 h | DMSO | significantly upregulates ZNF382 expression | 25319049 |
| MV4-11 | Function Assay | 5 μM | 72 h | DMSO | significantly upregulates ZNF382 expression | 25319049 |
| A2780 | Function Assay | 5 µM | 7 d | increases DNA methylation level | 25299694 | |
| CP70 | Function Assay | 5 µM | 7 d | increases DNA methylation level | 25299694 | |
| A2780 | Function Assay | 5 µM | 7 d | weakens the level of methylation | 25299694 | |
| CP70 | Function Assay | 5 µM | 7 d | weakens the level of methylation | 25299694 | |
| OCM3 | Growth Inhibition Assay | 0.5/1/2 μM | 7 d | DMSO | inhibits cell growth in a dose dependent manner | 25146981 |
| 92.1 | Growth Inhibition Assay | 0.5/1/2 μM | 7 d | DMSO | inhibits cell growth in a dose dependent manner | 25146981 |
| OCM1 | Growth Inhibition Assay | 0.5/1/2 μM | 7 d | DMSO | inhibits cell growth in a dose dependent manner | 25146981 |
| OMM1 | Growth Inhibition Assay | 0.5/1/2 μM | 7 d | DMSO | inhibits cell growth in a dose dependent manner | 25146981 |
| Mel 285 | Growth Inhibition Assay | 0.5/1/2 μM | 7 d | DMSO | inhibits cell growth in a dose dependent manner | 25146981 |
| Mel 290 | Growth Inhibition Assay | 0.5/1/2 μM | 7 d | DMSO | inhibits cell growth in a dose dependent manner | 25146981 |
| OCM3 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases clonogenicity dose-dependently | 25146981 |
| 92.1 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases clonogenicity dose-dependently | 25146981 |
| OCM1 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases clonogenicity dose-dependently | 25146981 |
| OMM1 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases clonogenicity dose-dependently | 25146981 |
| Mel 285 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases clonogenicity dose-dependently | 25146981 |
| Mel 290 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases clonogenicity dose-dependently | 25146981 |
| OCM3 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases invasion dose dependently | 25146981 |
| Mel 290 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases invasion dose dependently | 25146981 |
| OMM1 | Function Assay | 0.5/1 μM | 48 h | DMSO | decreases invasion dose dependently | 25146981 |
| OCM1 | Cell Viability Assay | 0.5/1 μM | 5 d | DMSO | decreases radiation-induced cell viability inhibition | 25146981 |
| 92.1 | Cell Viability Assay | 0.5/1 μM | 5 d | DMSO | decreases radiation-induced cell viability inhibition | 25146981 |
| OCM1 | Function Assay | 0.5/1 μM | 48 h | DMSO | causes global DNA hypomethylation at L-1 repeat loci | 25146981 |
| OCM3 | Function Assay | 0.5/1 μM | 48 h | DMSO | causes global DNA hypomethylation at L-1 repeat loci | 25146981 |
| 92.1 | Function Assay | 0.5/1 μM | 48 h | DMSO | causes global DNA hypomethylation at L-1 repeat loci | 25146981 |
| IMR32 | Function Assay | 3 μM | 72 h | DMSO | induces p19-INK4d expression significantly | 25104850 |
| IMR5-75 | Function Assay | 3 μM | 72 h | DMSO | induces p19-INK4d expression significantly | 25104850 |
| Be(2)-C | Function Assay | 3 μM | 72 h | DMSO | 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 | |
| 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 | ||
| 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 | |
| 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 | |||
| 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 | ||
| 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 | |
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 48 mg/mL
(196.56 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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| Molecular Weight | 244.2 | Formula | C8H12N4O5 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 320-67-2 | Download SDF | Storage of Stock Solutions |
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| Synonyms | 5-AzaC,Ladakamycin, AZA,5-Aza, CC-486,NSC 102816,5-Azacytidine | Smiles | C1=NC(=NC(=O)N1C2C(C(C(O2)CO)O)O)N | ||
| Targets/IC50/Ki |
DNA methyltransferase
(Cell-free assay) |
|---|---|
| In vitro |
Azacitidine (5-Azacytidine) is widely used to demonstrate the correlation between loss of methylation in specifc gene regions and activation of the associated genes. After incorporation into DNA, it inhibits DNA methyltransferase noncompetitively, causing a block in cytosine methylation in newly replicated DNA but not in resting, nondividing cells. This compound induces differentiation of Friend Erythroleukemia Cell C3H10T1/2 with myotube formation. It can be activated to the nucleoside triphosphate and incorporate into both DNA and RNA, leading to inhibition of DNA, RNA and protein synthesis in normal eukaryotic cells and in cancer cell lines, which could finally leads to cell death. Azacitidine also inhibits the incorporation of purine metabolites into macromolecules. It inhibits the L1210 cells growth with IC50 and of 0.019 μg/mL. |
| In vivo |
Azacitidine (5-Azacytidine) inhibits polynucleotide synthesis in leukemic BDF1 mice. At a dose of 3 mg/kg (i.p.), it increases the mean survival time in leukemic BDF1 mice inoculated with Ll210 ascites tumor cells. This compound markedly suppresses all enzyme activity in the polyamine-biosynthetic pathway, including ornithine decarboxylase activity, putrescine-dependent S-adenosyl-L-methionine decarboxylase activity, and spermidine-dependent S-adenosyl-L-methionine decarboxylase activity. It also inhibits the accumulations of polyamines in leukemic mice. |
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | DNMT1 |