OICR 9429

Names

[ Name ]:
OICR 9429

[Synonym ]:
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

Biological Activity

[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.

[Related Small Molecules]

GSK126 | Tazemetostat (EPZ-6438) | UNC 0642 | GSK343 | Pinometostat (EPZ5676) | 3-Deazaneplanocin A (hydrochloride) | Pemrametostat (GSK3326595) | UNC1999 | BIX-01294 | EPZ031686 | AZ505 (ditrifluoroacetate) | MS023 | EPZ 004777 | EPZ015666 | EPZ015866(GSK591)

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
693.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₉H₃₂F₃N₅O₃

[ Molecular Weight ]:
555.591

[ Flash Point ]:
372.9±31.5 °C

[ Exact Mass ]:
555.245728

[ LogP ]:
1.84

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.602

[ Storage condition ]:
-20℃

Related Compounds

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