SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
IC50&Target
DNMT3B
7.5 μM (IC50)
DNMT3A
8 μM (IC50)
DNMT1
12.5 μM (IC50)
体外研究
SGI-1027 is a DNMT inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate. SGI-1027 shows an IC50 of 6 μM for DNMT1 (hemimethylated DNA). SGI-1027 (1, 2.5, or 5 µM) causes selective degradation of DNMT1 in several human cancer cell lines, but shows little or no cytotoxic effect on rat hepatoma cells, and does not induce apoptosis in rat hepatoma cells. SGI-1027 shows an EC50 of 0.9 μM for hDNMT3A, and causes cytotoxicity on KG-1 cells, with an EC50 of 4.4 μM.
分子式
C27H23N7O
分子量
461.52
CAS号
1020149-73-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 27 mg/mL (58.50 mM; Need ultrasonic and warming)