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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-OICR-9429
OICR-9429

Chemical Structure : OICR-9429

CAS No.: 1801787-56-3

OICR-9429 (OICR9429;OICR 9429)

货号: PC-45120Not For Human Use, Lab Use Only.

OICR-9429 is a potent, selective, small-molecule antagonist of WDR5-MLL interaction that binds to WDR5 with Kd of 93±28 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

OICR-9429 is a potent, selective, small-molecule antagonist of WDR5-MLL interaction that binds to WDR5 with Kd of 93±28 nM.
OICR-9429 competitively disrupts the interaction with a high-affinity Wdr5-INteracting (WIN) peptide of MLL (Kdisp=64 nM).
OICR-9429 shows no significant binding or inhibition for 22 human methyltransferases, 9 different WD40- and histone reader domains.
OICR-9429 selectively inhibits proliferation and induces differentiation in p30-expressing human AML cells.

物理化学性质&存储条件

分子量 555.5913
分子式 C29H32F3N5O3
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

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

3-Pyridinecarboxamide, 1,6-dihydro-N-[4-(4-methyl-1-piperazinyl)-3'-(4-morpholinylmethyl)[1,1'-biphenyl]-3-yl]-6-oxo-4-(trifluoromethyl)-

参考文献

1. Grebien F, et al. Nat Chem Biol. 2015 Aug;11(8):571-578.

2. Getlik M, et al. J Med Chem. 2016 Mar 24;59(6):2478-96.

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