Bcl-2
Bcl-2 (B-cell lymphoma 2), encoded in humans by the BCL2 gene, is the founding member of the Bcl-2 family of regulator proteins that regulate cell death (apoptosis), by either inducing (pro-apoptotic) or inhibiting (anti-apoptotic) apoptosis. Bcl-2 is specifically considered an important anti-apoptotic protein but it is NOT considered a proto-oncogene because it is not a growth signal transducer.BCL-2 is localized to the outer membrane of mitochondria, where it plays an important role in promoting cellular survival and inhibiting the actions of pro-apoptotic proteins.
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AT 101是Downregulates Bcl-2,Mcl-1, pro-apoptotic。
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ABT-199 (GDC-0199)是一种Bcl-2选择性抑制剂,Ki为<0.01 nM,比作用于Bcl-xL和Bcl-w选择性高4800倍以上,对Mcl-1没有抑制活性。
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UMI-77是一种新型Mcl-1 SMI选择性抑制剂, 结合至Mcl-1BH3结构沟, Ki值为490 nM, 对抗凋亡的Bcl-2家族其他成员具有选择性。
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Gambogic Acid可激活caspases,EC50为0.78-1.64 μM,同时能竞争性抑制Bcl-XL,Bcl-2,Bcl-W,Bcl-B,Bfl-1和Mcl-1,IC50分别为1.47,1.21,2.02。
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AT101乙酸盐对Bcl-2, Bcl-xL和Mcl-1的结合Ki值分别为0.32,0.48和0.18uM。
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