BH3I-1
CAS No. : 300817-68-9
(Synonyms: BHI1)
| Size | Price | Stock |
|---|---|---|
| 5mg | $65 | In-stock |
| 10mg | $105 | In-stock |
| 25mg | $195 | In-stock |
| 50mg | $320 | In-stock |
| 100mg | $520 | In-stock |
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| Cat. No. : | HY-100383 |
| M.Wt: | 400.31 |
| Formula: | C15H14BrNO3S2 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
IC50 & Target:Bcl-2[1]
Kd: 5.3 μM (p53/mDM2)[2]
In Vitro: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[2].
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[3].
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