CHDI 00390576

Modify Date: 2024-01-14 13:57:27

CHDI 00390576 Structure
CHDI 00390576 structure
Common Name CHDI 00390576
CAS Number 1629729-98-1 Molecular Weight 391.32
Density N/A Boiling Point N/A
Molecular Formula C19H13F4N3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CHDI 00390576


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].

 Names

Name CHDI-390576

 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
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
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