产品描述
GNF362 is a selective and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb; IC50: 9 nM). GNF362 also inhibits Itpka and Itpkc (IC50s: 20 nM and 19 nM).
体外活性
GNF362 augments SOC responses following antigen receptor cross-linking, with an EC50 of 12 nM in primary B or T lymphocytes.GNF362 (0-10 mM) blocks Ins (1,3,4,5) P4 production, enhances antigen receptor-driven Ca2+ responses and lead to apoptosis of activated T cells in an Itpkb-dependent manner in lymphocytes.
体内活性
GNF362 ?shows minimal block in antibody production but shows significant inhibition of joint swelling at 6 mg/kg, reduces inflammatory cell infiltrate, proteoglycan los, and sjoint damage?at 20 mg/kg.
Cas No.
1003019-41-7
分子式
C22H21F3N6
分子量
426.44
别名
GNF362
储存和溶解度
DMSO:125 mg/mL (293.12 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years