BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.
体外研究
BIO-acetoxime (BIA; Compound 13) is a potent and selective GSK-3α/β inhibitor, with IC50s of both 10 nM. BIO-acetoxime (BIA) shows weak effect on CDK5/p35 (IC50, 2.4 μM), CDK2/cyclin A (IC50, 4.3 μM), and CDK1/cyclin B (IC50, 63 μM). BIO-acetoxime (BIA) (5 μM and 10 μM) increases the viability of HSV-1-infected cells but shows little effect on morphology and viability of mockin-fected cells. Moreover, BIO-acetoxime (BIA) (0.625, 1.25, 2.5, 5, and 10 μM) significantly reduces the release of HSV-1 particles in OC3 cells, with an EC50 of 0.68 ± 0.28 μM. BIO-acetoxime (BIA) inhibits the expression of HSV-1 genes, and may not affect the nuclear targeting of HSV-1 capsids. In addition, delayed addition of BIO-acetoxime (BIA) also inhibits HSV-1 infection.
体内研究
BIO-acetoxime (BIA) shows anticonvulsant effects in the focal pilocarpine rat model at 0.5 mg/kg, and in 6-Hz fully kindled FVB/N mice at 0.5, 2.5, and 5 mg/kg via i.p. administration.
分子式
C18H12BrN3O3
分子量
398.21
CAS号
667463-85-6
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 : 20.83 mg/mL (52.31 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)