WEHI-9625 是一种首创的，三环砜小分子凋亡抑制剂，EC50 值为 69 nM。WEHI-9625 与 VDAC2 结合可促进其抑制小鼠 BAK 诱导的细胞凋亡的能力，但对人 BAK 和与凋亡效应密切相关的 BAX 因子均完全无效。
货号:ajcx34126
CAS:2595314-46-6
分子式:C34H27NO5S2
分子量：593.71
溶解度:DMSO : 100 mg/mL (168.43 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.