GSK046

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK046 是一种有效、选择性和口服活性的 BET 蛋白 BD2 bromodomain 抑制剂（IC50 分别为 264 nM (BRD2 BD2)、98 nM (BRD3 BD2)、49 nM (BRD4 BD2) 和 214 nM (BRDT BD2)。

GSK046 is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins(IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively). It has immunomodulatory activity.

Cell Proliferation Assay Cell Line:Human primary CD4+ T cell Concentration:0.001, 0.01, 0.1, 1, 10 μM Incubation Time:72 hours Result:Did not affect the proliferative activity of the cells but still inhibited the production of effector cytokines.

Animal Model:Male C57BL/6 mice (8/10-weeks-old) are injected with keyhole limpet hemocyanin (KLH)Dosage:40?mg/kg/QD Administration:S.c. injections for 14 days Result:Reduced the production of anti-keyhole limpet hemocyanin (KLH) IgM and was well tolerated.Animal Model:Female C57BL/6 mice Dosage:10?mg/kg (Pharmacokinetic Analysis)Administration:Oral administration Result:Cmax (1859 ng/mL), T1/2 (1.8 h).Animal Model:Male C57BL/6 mice Dosage:40?mg/kg (Pharmacokinetic Analysis)Administration:Oral administration Result:Cmax (2993 ng/mL), T1/2 (1.9 h).Animal Model:Female Lewis rat Dosage:10?mg/kg (Pharmacokinetic Analysis) Administration:Oral administration Result:Cmax (202 ng/mL), T1/2 (1.4 h).

iBET-BD2

Chromatin/Epigenetic

Epigenetic Reader Domain

BRD2-BD2|BRD3-BD2|BRD4-BD2|BRDT-BD2

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2474876-09-8

414.48

C23H27FN2O4

>98% (HPLC)

DMSO:83.33 mg/mL?(201.05 mM;?Need ultrasonic)

O=C(N[C@@H]1CC[C@@H](O)CC1)C2=CC(O[C@H](C3=CC=CC=C3)C)=C(NC(C)=O)C(F)=C2

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(-20℃)

With Ice Pack

≥ 2 years