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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-INCB054329
INCB054329

Chemical Structure : INCB054329

CAS No.: 1628607-64-6

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INCB054329 (INCB 054329)

货号: PC-62281Not For Human Use, Lab Use Only.

INCB 054329 (INCB054329) is a potent, selective, pan-BET bromodomain inhibitor with biochemical IC50 of 1-119 nM against BRD2, BRD3, and BRD4 and BRDT.

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

INCB 054329 (INCB054329) is a potent, selective, pan-BET bromodomain inhibitor with biochemical IC50 of 1-119 nM against BRD2, BRD3, and BRD4 and BRDT.
INCB 054329 exhibits broad antiproliferative activity against hematologic cancer cell lines and antagonizes c-MYC expression in vitro (mean IC50=152 nM) and in vivo.
INCB054329 reduces BRD4 binding to the IgH enhancer and reduces expression of target genes.
INCB054329 potently inhibited the binding of tetra-acetylated histone H4 peptide to BRD2, BRD3, and BRD4, with modest selectivity for BRDT-BD1 and BRDT-BD2, showed no inhibition against 16 non-BET bromodomains at 3 uM.
INCB 054329 strongly affected c-MYC, and other putative oncogenes such as FGFR3 and pathways including JAK–STAT, also suppressed secretion of IL6 by immortalized, human stromal cell lines, sensitizes myeloma cells to clinical JAK inhibitor ruxolitinib or itacitinib.
INCB054329 showed synergistic effects on tumor growth when combined with JAK inhibitor in the subcutaneous INA-6 human myeloma xenograft model.

物理化学性质&存储条件

分子量 348.362
分子式 C19H16N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

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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