OICR 9429

Modify Date: 2024-01-30 09:54:33

OICR 9429 Structure
OICR 9429 structure
Common Name OICR 9429
CAS Number 1801787-56-3 Molecular Weight 555.591
Density 1.3±0.1 g/cm3 Boiling Point 693.0±55.0 °C at 760 mmHg
Molecular Formula C29H32F3N5O3 Melting Point N/A
MSDS N/A Flash Point 372.9±31.5 °C

 Use of OICR 9429


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.

 Names

Name oicr-9429
Synonym More Synonyms

 OICR 9429 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
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.

 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℃

 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
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