CHDI 00390576

Names

[ Name ]:
CHDI 00390576

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₃F₄N₃O₂

[ Molecular Weight ]:
391.32

Related Compounds

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