INCB057643

Catalog No.S8714

INCB057643 Chemical Structure

Molecular Weight(MW): 415.46

INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones.

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Biological Activity

Description INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones.
Targets
BET [2]
()
In vitro

INCB057643 inhibits binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range, and is selective against other bromodomain containing proteins. In vitro analyses show that INCB057643 inhibits proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicate that G1 arrest and a concentration-dependent increase in apoptosis are seen within 48 hours of treatment with INCB057643. Production of several cytokines, including IL-6, IL-10 and MIP-1α, was repressed by INCB057643 in human and mouse whole blood stimulated ex vivo with LPS[1]. INCB057643 inhibits proliferation of prostate cancer cell lines. In short-term cell proliferation assays, INCB057643 appears more effective against androgen-dependent (VCaP and LNCaP) than androgen-independent (DU145 and PC3) cells[2].

In vivo

Oral administration of INCB057643 resulted in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL[1]. Treatment of mice bearing 22Rv1 tumor xenografts with INCB057643 (3 mg/kg) led to significant inhibition of tumor growth (T/C%:45%) and consistent reduction of tumor weight relative to vehicle-treated mice[2].

Protocol

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.77 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 415.46
Formula

C20H21N3O5S

CAS No. 1820889-23-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID