GNF362

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

GNF362 是肌醇三磷酸3'激酶 B (Itpkb) 的选择性，有效且可口服生物利用的抑制剂，IC50为 9 nM。 GNF362 还抑制 Itpka 和 Itpkc，IC50 值分别为 20 nM 和 19 nM。 肌醇三磷酸3'激酶 B (Itpkb) 是一种 Ca2+ 依赖性激酶，其磷酸化 Ins (1,4,5) P3 的 3' 位置，生成肌醇 1,3,4,5-四磷酸 [Ins (1,3,4,5) P4]。

GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].

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.GNF362 augments SOC responses following antigen receptor cross-linking, with an EC50 of 12 nM in primary B or T lymphocytes.

GNF362 (orally administration; 6 or 20 mg/kg; twice daily; 21 days) shows minimal block in antibody production but shows significant inhibition of joint swelling at 6 mg/kg, reduces inflammatory cell infiltrate, joint damage, and proteoglycan loss at 20 mg/kg.Animal Model:A Lewis rat antigen-induced arthritis (rAIA) model Dosage:6 or 20 mg/kg Administration:Orally administration; 6 or 20 mg/kg; twice daily; 21 days Result:Reduced knee swelling in both the 20mg/kg and 6mg/kg treatment groups of GNF362 by 47% and 34%, respectively.

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Metabolic Enzyme/Protease

Phosphatase

Phosphatase

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1003019-41-7

426.44

C22H21F3N6

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (234.50 mM; 超声助溶 ) Ethanol 中的溶解度 : ≥ 50 mg/mL (117.25 mM)

C[C@@H]1CN(Cc2cn[nH]c2-c2ccc(cc2)C#N)CCN1c1ccc(cn1)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years