1. Apoptosis
  2. Bcl-2 Family
    MDM-2/p53

BH3I-1 (Synonyms: BHI1; BH 3I1)

Cat. No.: HY-100383 Purity: >98.0%
Handling Instructions

BH3I-1 is a Bcl-2 antagonist. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.

For research use only. We do not sell to patients.
BH3I-1 Chemical Structure

BH3I-1 Chemical Structure

CAS No. : 300817-68-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 88 In-stock
2 mg USD 60 In-stock
5 mg USD 100 In-stock
10 mg USD 150 In-stock
25 mg USD 300 In-stock
50 mg USD 500 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BH3I-1 is a Bcl-2 antagonist. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.

IC50 & Target[2]

Bcl-2

 

Bcl-xL

 

Bim

 

p53/mDM2

5.3 μM (Kd)

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.4981 mL 12.4903 mL 24.9806 mL
5 mM 0.4996 mL 2.4981 mL 4.9961 mL
10 mM 0.2498 mL 1.2490 mL 2.4981 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

400.31

Formula

C₁₅H₁₄BrNO₃S₂

CAS No.

300817-68-9

SMILES

O=C(O)C(C(C)C)N(C/1=O)C(SC1=C\C2=CC=C(Br)C=C2)=S

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 3.9 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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BH3I-1
Cat. No.:
HY-100383
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