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GSK2982772

CAS No. : 1622848-92-3

MCE 站：GSK2982772

产品活性：GSK2982772 是可口服的、有效的 ATP 竞争型的 RIP1 酶抑制剂，对人和猴子 RIP1 的 IC₅₀ 值分别为 16 nM 和 20 nM。

研究领域：Apoptosis

作用靶点：RIP kinase

In Vitro: GSK2982772 shows more than 1,000-fold selectivity for ERK5 over a panel of over 339 kinases at 10 μM. In stimulated cellular systems,GSK2982772 is also able to reduce spontaneous production of cytokines (IL-1β and IL-6) in a concentration-dependent fashion from ulcerative colitis explant tissue in overnight incubations. GSK2982772 produces a weak concentration dependent inhibition of hERG in human embryonic kidney (HEK-293) cells, with an estimated IC₅₀ of 195 μM, and also shows a weak activation of the human Pregnane X receptor (hPXR) with an EC₅₀ of 13 μM.

In Vivo: GSK2982772 is dosed orally 15 min prior to TNF and shows 68, 80, and 87% protection from temperature loss over 6 h, at doses of 3, 10, and 50 mg/kg, respectively. In the corresponding TNF/zVAD model, GSK2982772 shows 13, 63, and 93% protection from temperature loss over 3 h. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, GSK2982772 has low brain penetration in rat (4%) despite possessing good cell permeability (21×10^-6 cm/s).

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  NF-κB Signaling Compound Library  |  Clinical Compound Library  |  CNS-Penetrant Compound Library  |  Drug Repurposing Compound Library  |  Anti-COVID-19 Compound Library  |  Pyroptosis Compound Library  |  Orally Active Compound Library  |  Necrostatin-1  |  GSK-872  |  GSK583  |  GSK840  |  GSK-843  |  HS-1371  |  RIP2 kinase inhibitor 2  |  PROTAC RIPK degrader-2  |  RIPK-IN-4  |  RIPK1-IN-4  |  RIPK1-IN-7  |  PROTAC RIPK degrader-6  |  Kongensin A  |  GNE684  |  cRIPGBM

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