1629729-98-1

1629729-98-1 structure

Name: CHDI 00390576
Chemical Name: CHDI-390576
CAS Number: 1629729-98-1
Molecular Formula: C₁₉H₁₃F₄N₃O₂
Molecular Weight: 391.32
Catalog: Signaling Pathways Cell Cycle/DNA Damage HDAC
Create Date: 2019-06-04 17:48:02
Modify Date: 2024-01-14 13:57:27
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histonedeacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform[1].

Name	CHDI-390576

Description	CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histonedeacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC Signaling Pathways >> Epigenetics >> HDAC
Target	HDAC4:54 nM (IC50) HDAC5:60 nM (IC50) HDAC7:31 nM (IC50) hHDAC9:50 nM (IC50) HDAC1:39.7 μM (IC50) HDAC3:25.8 μM (IC50) HDAC8:9.1 μM (IC50) hHDAC6:6.2 μM (IC50)
In Vitro	The affinity (Kd) of CHDI-390576 to the catalytic domain of immobilized HDAC4 is 80 nM[1]. CHDI-390576 inhibits class I HDACs (1, 3, 8) and class IIb HDAC6 isoforms with IC50s of 39.7μM, 25.8 μM, 9.1 μM, 6.2 μM, respectively[1].
References	[1]. Luckhurst CA, et al. Development and characterization of a CNS-penetrant benzhydryl hydroxamic acid class IIa histone deacetylase inhibitor. Bioorg Med Chem Lett. 2019 Jan 1;29(1):83-88.

Molecular Formula	C₁₉H₁₃F₄N₃O₂
Molecular Weight	391.32