Chk2억제제

Chk2억제제 화학적 특성, 용도, 생산

• 용도

  Chk2 Inhibitor is a checkpoint kinase inhibitor that mediates apoptosis and cell cycle arrest.

• 일반 설명

  A cell-permeable, ATP competitive, and reversible indoloazepine compound that displays anti-proliferative and anti-inflammatory properties. Acts as a potent inhibitor of Chk2 (IC₅₀ = 8 nM) that targets the ATP binding pocket. Exhibits selectivity for Chk2 over MEK1, Chk1, CK1δ, PKCα, PKCβII and CK2 (IC₅₀ = 89 nM, 237 nM, 1.352 μM, 2.539 μM, 3.381 μM, and >10.0 μM, respectively). Blocks the production of IL-2 and TNF-α by preventing the transcriptional activation of NF-κB (IC₅₀ = 3.55 μM for IL-2 production in PMA-stimulated Jurkat T cells; 8.16 μM for TNF-α production in LPS-stimulated THP-1 cells). Also reported to suppress the growth of leukemic T cells (GI₅₀ = 1.73 μM).

• Biochem/physiol Actions

  Primary TargetChk2

Chk2억제제 공급 업체

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