OICR-9429 ( OICR9429;OICR 9429 )

Catalog No. M12746 CAS No. 1801787-56-3

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

OICR-9429
Note

Research use only, not for human use.
Brief Description

A potent, selective, small-molecule antagonist of WDR5-MLL interaction that binds to WDR5 with Kd of 93±28 nM.
Description

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

OICR9429;OICR 9429
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

WDR5
Research Area

Cancer
Indication

——

CAS Number

1801787-56-3
Formula Weight

555.59
Molecular Formula

C29H32F3N5O3
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 32 mg/mL
SMILES

O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=CC(C3=CC=CC(CN4CCOCC4)=C3)=CC=C2N5CCN(C)CC5
Chemical Name

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

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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