2. Epigenetics
  3. Epigenetic Reader Domain
  4. GSK040

GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases.

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

GSK040 Chemical Structure

GSK040 Chemical Structure

CAS No. : 2752331-09-0

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GSK040 Related Antibodies

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Description

GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases[1].

IC50 & Target[1]

BD2

8.3 (pIC50)

In Vivo

GSK040 (1 mg/kg; i.v.) exhibits t1/2 (0.19 h), CLb (50 mL/min/kg) and Vss (0.6 L/kg) in rats[1].
GSK040 (3 mg/kg; p.o.) exhibits oral bioavailability (16%), tmax (0.25 h), Cmax (398 nM) in rats[1].

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

502.60

Formula

C29H34N4O4
CAS No.
SMILES

O=C(C(C=C1C)=CN(C)C1=O)N([C@H](C2CCOCC2)C(NC)=O)C[C@H](C3=CC=CC=C3)C4=NC=CC=C4
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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GSK040 Related Classifications

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

GSK0402752331-09-0GSK 040GSK-040Epigenetic Reader DomainBETBD2oncologyimmunologyInhibitorinhibitorinhibit

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