300817-68-9

Name	BH3I-1
Synonyms	BHI1 BH3I1 BH3I-1 BH 3I1 BH3I 1 5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid 5-(p-Bromobenzylidene)-a-isopropyl-4-oxo-2-thioxo-3-thiazolidine acetic acid 3-Thiazolidineacetic acid, 5-[(4-bromophenyl)methylene]-α-(1-methylethyl)-4-oxo-2-thioxo-
CAS	300817-68-9

Molecular Formula	C15H14BrNO3S2
Molar Mass	400.31
Density	1?+-.0.1 g/cm3(Predicted)
Boling Point	535.2±60.0 °C(Predicted)
Solubility	DMSO: >10mg/mL, soluble
Appearance	powder, yellow
pKa	3.39±0.10(Predicted)
Storage Condition	Sealed in dry,2-8°C
In vitro study	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 K d =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 K i of 7.8±0.9 μM.

Hazard Symbols	Xn - Harmful
Risk Codes	20/21/22 - Harmful by inhalation, in contact with skin and if swallowed.
Safety Description	36 - Wear suitable protective clothing.
WGK Germany	3

Last Update：2024-01-02 23:10:35

biological activity	BH3I-1 is a Bcl-2 family antagonist that inhibits the binding of Bak BH3 peptide to Bcl-xL, ki was 2.4±0.2 μm. On BH3I-1, the Kd of p53/mDM2 was 5.3 μm.
Target	Bcl-2 Bcl-xL Bim Bak p53/mDM2 5.3 μm (Kd)
in vitro study	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 scanning assurance, plays by a well studied assay with purified protein. The results from the FP assay validates the split-luciferase screen and demonstrates that BH3I-1 has a K d =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 K I of 7.8±0.9 μM.

Last Update：2024-04-10 22:29:15

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300817-68-9

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