Bcl-2 Family
The Bcl-2 Family consists of apoptosis regulator Bcl-2 and its homologues. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, BAD, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). Bcl-x(L), Bcl-x(S) and Bcl-xβ are three isoforms derived by alternative RNA splicing.
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Masitinib, a novel phenylaminothiazole-type derivative, is an inhibitor of the class III receptor tyrosine kinase stem-cell growth factor receptor (c-Kit) with IC50 of 200 nM, platelet-derived growth factor receptor α and β and the non-receptor tyrosine kinase Lyn(PDGFRα/β with IC50 of 540 nM/800 nM).
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Muristerone A是Muristerone A has antiapoptotic activity and stimulates Bcl-XL mRNA transcription。
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ABT-263 (Navitoclax)是一种有效的Bcl-xL， Bcl-2和Bcl-w抑制剂，Ki分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。
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Obatoclax (GX15-070)是Bcl-2 homology domain-3 (BH3)的类似物，对各种抗凋亡的Bcl-2家族蛋白的IC50平均为3 uM，如对Mcl-1(IC50为2.9 uM)和Bfl-1(IC50为5 uM)。
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ABT-737是一种类BH3抑制剂，能同时抑制Bcl-xL， Bcl-2和Bcl-w ，EC50分别为78.7 nM，30.3 nM和197.8 nM；但对Mcl-1， Bcl-B及Bfl-1没有抑制作用。
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