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GS-444217

CAS No. : 1262041-49-5

MCE 站：GS-444217

产品活性：GS-444217 是一种有效的，可口服的，选择性 ATP 竞争性凋亡信号调节激酶 1 (ASK1) 抑制剂，IC₅₀ 为 2.87 nM。

研究领域：MAPK/ERK Pathway  |  Apoptosis

作用靶点：MAP3K  |  Apoptosis

In Vitro: Treatment with GS-444217 reduces ASK1 phosphorylation and prevents the phosphorylation of MKK3/6, MKK4, p38, and JNK at concentrations of 0.3 μM and above with full suppression of ASK1 activity at 1 μM. GS-444217 (1 μM) reduces ASK1 activity within 5 minutes of addition to the cultures, reaching a maximum level of inhibition by 30 minutes. Removal of GS-444217 from the cultures results in reactivation of ASK1 autophosphorylation within 10 minutes and near-complete recovery 2 hours after drug washout.

In Vivo: GS-444217 reduces oxidative stress (OS)-induced ASK1 signaling in kidney and inhibits acute renal tubular injury in rats. GS-444217 (30 mg/kg) inhibits activation of ASK1, p38, and JNK in rat kidney. GS-444217 has an in vivo EC₅₀ of approximately 1.6 μM for inhibiting the ASK1 pathway in rodent kidney.

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