Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 94.00 | |
5 mg | In stock | $ 198.00 | |
10 mg | In stock | $ 318.00 | |
25 mg | In stock | $ 597.00 | |
50 mg | In stock | $ 852.00 | |
100 mg | In stock | $ 1,170.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 211.00 |
Description | GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth. |
Targets&IC50 | DNMT1:36 nM |
In vitro | In MV4-11 cells, GSK3685032 (0.1-1000 nM, 1-6 days) exhibited growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course. GSK3685032 (10-10000 nM, day 4) increased the immune-related gene transcription in a dose dependent manner[1]. GSK3685032 (3.2-10,000 nM, 2 days) inhibited DNMT1 protein expression. In 15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells, GSK3685032 (6 days) showed cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM. GSK3685032 induced DNA hypomethylation and gene activation[1]. |
In vivo | In MV4-11 xenograft models or SKM-1 xenograft models, GSK-3685032 (1-45 mg/kg; s.c.) inhibited dose-dependent tumor growth with clear regression at ≥30 mg/kg[1]. |
Molecular Weight | 420.53 |
Formula | C22H24N6OS |
CAS No. | 2170137-61-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (23.78 mM), Sonification is recommended
You can also refer to dose conversion for different animals. More
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GSK3685032 2170137-61-6 Chromatin/Epigenetic DNA Methyltransferase Inhibitor lymphoma DNMTs cancer DNA MTases inhibit GSK-3685032 GSK 3685032 MV4–11 leukemia GDM-1 multiple myeloma inhibitor