High affinity and selective activator of Bax (Ki = 43.3nM). Binds to the S184 binding pocket to block Bax phosphorylation. Does not bind to other Bcl-2 family members, including Bcl-2, Bak and Bid. Facilitates Bax insertion into the mitochondrial membrane and promotes Bax-dependent cytochrome c release. Induces apoptosis in lung cancer cell lines expressing high levels of Bax selectively over normal cells expressing low levels of Bax. Represses tumor growth of A549 lung cancer xenografts in mice.
Chemical Name: 2-[(2-Nitro-9H-fluorene-9-ylidene)methyl]phenol
CAS Number: 906440-37-7
Solubility: Soluble to 100mM in DMSO and to 10mM in ethanol with gentle warming
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