化学性质:
规格 | 10mg 50mg |
CAS | 331244-89-4 |
别名 | BAM 7;BAM-7 |
化学名 | (4E)-4-[(2-ethoxyphenyl)hydrazinylidene]-5-methyl-2-(4-phenyl-1,3-thiazol-2-yl)pyrazol-3-one |
分子式 | C21H19N5O2S |
分子量 | 405.47 |
溶解度 | DMF: 5 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.33 mg/ml,DMSO: 2 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
In the competitive fluorescence polarization assay (FPA), BAM7 competes with FITC–BIM SAHB for BAX binding site(BH3) in a dose dependent manner. BAM7 shows no antiapoptotic or BAKΔC competitive binding interactions even at 50 μM dosing, revealing a remarkable selectivity of BAM7 for BAX. The interaction between BAM7 and BAX at the very surface induces the characteristic structural changes that yield functional BAX oligomerization. In the in vitro assay, BAM7 induces BAX-dependent cell death but not the cells with BAK. BAM7 could be developed to a new generation of apoptotic modulators that directly activate BCL-2 family executioner proteins in cancer
and other diseases driven by pathologic apoptotic blockades [1].
References:
[1] Evripidis Gavathiotis, Denis E Reyna, Joseph A Bellairs, Elizaveta S Leshchiner, and Loren D Walensky. Direct and selective small-molecule activation of proapoptotic BAX. Nat Chem Biol. 2012 July ; 8(7): 639–645.
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标签:BAM7
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