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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 21,500 | |||
5 mg | 在庫あり | ¥ 45,500 | |||
10 mg | 在庫あり | ¥ 73,000 | |||
25 mg | 在庫あり | ¥ 137,000 | |||
50 mg | 在庫あり | ¥ 195,500 | |||
100 mg | 在庫あり | ¥ 268,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 48,500 |
説明 | 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. |
ターゲット&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]. |
分子量 | 420.53 |
分子式 | 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), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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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