BH3I-1 是一种 Bcl-2家族 拮抗剂，抑制 Bak BH3 肽与 Bcl-xL 结合，K_i 为 2.4±0.2 μM。BH3I-1 作用于 p53/mDM2，K_d 为 5.3 μM。

BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a K i of 2.4±0.2 μM in FP assay. BH3I-1 has a K d of 5.3 μM against the p53/MDM2 pair.

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Bcl-2 Bcl-xL

BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1α interactions. This surprising promiscuity, displays by a well studied compound leads to further interrogate the p53/hDM2 interaction utilizing a standard fluorescence polarization (FP) assay with purified protein. The results from the FP assay validates the split-luciferase screen and demonstrates that BH3I-1 has a Kd=5.3 μM against the p53/mDM2 pair, which is comparable to its low micromolar potency reported for the BH3 family of receptors. BH3I-1 inhibits interaction between the BH3 domain and Bcl-xL. NMR analyses reveal that BH3I-1 targets the BH3-binding pocket of Bcl-xL with a Ki of 7.8±0.9 μM. has not independently confirmed the accuracy of these methods. Th

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[1]. Wang L, et al. Development of dimeric modulators for anti-apoptotic Bcl-2 proteins. Bioorg Med Chem Lett. 2008 Jan 1;18(1):236-40.
[2]. Degterev A, et al. Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL. Nat Cell Biol. 2001 Feb;3(2):173-82.
[3]. Porter JR, et al. Pro

In Vitro: DMSO : 100 mg/mL (249.81 mM; Need ultrasonic)配制储备液