1. Epigenetics
  2. Epigenetic Reader Domain
  3. I-BET432

I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases.

For research use only. We do not sell to patients.

I-BET432 Chemical Structure

I-BET432 Chemical Structure

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Description

I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases[1].

In Vitro

I-BET432 inhibits BRD4 BD1 and BD2 with pIC50 values of 7.5 and 7.2, respectively[1].
I-BET432 inhibits human whole blood MCP-1 with an pIC50 value of 7.4[1].
I-BET432 inhibits hERG with an pIC50 value <4.3[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

I-BET432 shows great oral bioavailability in rats and dogs[1].
1.19 Pharmacokinetic Properties of I-BET432 in Rats and Dogs[1].

Rats
PO/IV 3/1 mg/kg
Dogs
PO/IV 1.5/0.5 mg/kg
CLb (mL/min/kg) 26 28
CLb,u (mL/min/kg) 38 20
Vss (L/kg) 1.3 2.7
Vss,u (L/kg) 1.9 5.7
t1/2 (h) 0.74 1.4
Fpo (%) 67 79
fub 0.68 0.47

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

327.38

Formula

C18H21N3O3

SMILES

O=C1N(C)C=C(C2=CN(C)N=C2)C3=CC([C@@H](O)CO)=CC=C3[C@H]1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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I-BET432 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
I-BET432
Cat. No.:
HY-151894
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