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OICR-9429

Chemical Structure : OICR-9429

CAS No.: 1801787-56-3

OICR-9429 (OICR9429;OICR 9429)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 555.5913
Formula C29H32F3N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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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)-

References

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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