CHDI-390576 |
| Catalog No.GC64942 |
클래스 IIa HDAC4, HDAC5, HDAC7, HDAC9에 대해 IC50이 각각 54nM, 60nM, 31nM, 50nM인 강력한 세포 투과성 및 CNS 침투성 클래스 IIa 히스톤 데아세틸라제(HDAC) 억제제인 CHDI-390576은 >500을 나타냅니다. - 클래스 I HDAC(1, 2, 3)에 대한 배 선택성 및 HDAC8 및 클래스 IIb HDAC6 동형에 대한 ~150배 선택성.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1629729-98-1
Sample solution is provided at 25 µL, 10mM.
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CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (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].
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].
[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.
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