INCB054329 ( INCB 054329 )

Catalog No. M12432 CAS No. 1628607-64-6

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Datasheet

HNMR

HPLC

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Product Name

INCB054329
Note

Research use only, not for human use.
Brief Description

INCB054329 is a novel potent, orally bioactive BET inhibitor that inhibits binding of BRD2, BRD3 and BRD4 to an acetylated histone H4 peptide with low nanomolar potency.
Description

INCB054329 is a novel potent, orally bioactive BET inhibitor that inhibits binding of BRD2, BRD3 and BRD4 to an acetylated histone H4 peptide with low nanomolar potency; inhibits expression of c-MYC and induced HEXIM1 in myeloma cell lines; inhibits growth of the majority of myeloma, AML, and lymphoma cell lines with IC50<100 nM; induces G1 arrest and cell apoptosis consistent with increased expression of pro-apoptotic regulators; inhibits tumor growth in vivo.
Synonyms

INCB 054329
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

1628607-64-6
Formula Weight

348.36
Molecular Formula

C19H16N4O3
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 100 mg/mL 287.06 mM
SMILES

O=C1N2[C@H](COC3=C2C(N1)=CC=C3C4=C(ON=C4C)C)C5=CC=CC=N5
Chemical Name

(S)-6-(3,5-dimethylisoxazol-4-yl)-3-(pyridin-2-yl)-3,4-dihydro-5-oxa-1,2a-diazaacenaphthylen-2(1H)-one

1. Phillip CC Liu, et al. DOI: 10.1158/1538-7445.AM2015-3523 Published August 2015
2. Pérez-Salvia M, et al. Epigenetics. 2017 May 4;12(5):323-339.

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