WEHI-9625 |
Catalog No.GC62641 |
WEHI-9625는 삼환식 설폰으로 EC50이 69nM인 동급 최초의 세포자멸사 억제제입니다. WEHI-9625는 VDAC2에 결합하고 마우스 BAK에 의해 구동되는 세포자멸사를 억제하는 능력을 촉진합니다. WEHI-9625는 인간 BAK와 밀접하게 관련된 세포자멸사 효과기 BAX에 대해 완전히 비활성입니다.
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Cas No.: 2595314-46-6
Sample solution is provided at 25 µL, 10mM.
WEHI-9625 is a tricyclic sulfone, first-in-class inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX[1].
WEHI-9625 (0-10 µM; Mcl1-/-Bax-/- MEFs cells) treatment could prevent cell death mediated by BAK and potently inhibits BIM BH3-induced loss of mitochondrial membrane potential in Bax-/-, but not Bak-/-, cells[1].
WEHI-9625 demonstrates that blocking apoptosis at an early stage was both advantageous and pharmacologically tractable[1].
[1]. van Delft MF, et al. A small molecule interacts with VDAC2 to block mouse BAK-driven apoptosis. Nat Chem Biol. 2019 Oct 7.
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