1801787-56-3

1801787-56-3 structure

Name: OICR 9429
Chemical Name: oicr-9429
CAS Number: 1801787-56-3
Molecular Formula: C₂₉H₃₂F₃N₅O₃
Molecular Weight: 555.591
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2018-06-21 04:00:35
Modify Date: 2025-08-20 15:44:46
OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation .target: Wdr5IC 50: 5 uMIn vitro: OICR-9429 inhibit proliferation and induce differentiation in p30-expressing human AML cells. OICR-9429 cause a significant decrease in viability in the majority of patient cells with mutations in the N-terminal part of the CEBPA gene. OICR-9429 displays exquisite cellular selectivity and specificity in disrupting critical protein-protein interactions between WDR5. [1] reduce the viability of primary human AML cells with N-terminal C/EBPα mutations by about 50% (mean value, n = 8) at 5 μM[2]In vivo:The reference for OICR-9429 to mice (female NOD-SCID) is 3 mg/kg.

Name	oicr-9429
Synonyms	OICR-9429 N-[4-(4-Methyl-1-piperazinyl)-3'-(4-morpholinylmethyl)-3-biphenylyl]-6-oxo-4-(trifluormethyl)-1,6-dihydro-3-pyridincarboxamid N-[4-(4-Methyl-1-piperazinyl)-3'-(4-morpholinylmethyl)-3-biphenylyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydro-3-pyridinecarboxamide N-[4-(4-Méthyl-1-pipérazinyl)-3'-(4-morpholinylméthyl)-3-biphénylyl]-6-oxo-4-(trifluorométhyl)-1,6-dihydro-3-pyridinecarboxamide 3-Pyridinecarboxamide, 1,6-dihydro-N-[4-(4-methyl-1-piperazinyl)-3'-(4-morpholinylmethyl)[1,1'-biphenyl]-3-yl]-6-oxo-4-(trifluoromethyl)- OICR9429

Description	OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation .target: Wdr5IC 50: 5 uMIn vitro: OICR-9429 inhibit proliferation and induce differentiation in p30-expressing human AML cells. OICR-9429 cause a significant decrease in viability in the majority of patient cells with mutations in the N-terminal part of the CEBPA gene. OICR-9429 displays exquisite cellular selectivity and specificity in disrupting critical protein-protein interactions between WDR5. [1] reduce the viability of primary human AML cells with N-terminal C/EBPα mutations by about 50% (mean value, n = 8) at 5 μM[2]In vivo:The reference for OICR-9429 to mice (female NOD-SCID) is 3 mg/kg.
Related Catalog	Signaling Pathways >> Epigenetics >> Histone Methyltransferase Research Areas >> Cancer
References	[1]. Grebien F et al. Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat Chem Biol. 2015 Aug;11(8):571-8. [2]. Getlik M et al. Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J Med Chem. 2016 Mar 24;59(6):2478-96.