CHDI-390576 |
| رقم الكتالوجGC64942 |
CHDI-390576 ، مثبط قوي ، منفذ للخلية ، ومانع اختراق من الفئة IIa هيستون ديستيلاز (HDAC) مع IC50s من 54 نانومتر ، 60 نانومتر ، 31 نانومتر ، 50 نانومتر للفئة IIa HDAC4 ، HDAC5 ، HDAC7 ، HDAC9 ، على التوالي ، يظهر> 500 - انتقائية مضاعفة على الفئة الأولى HDACs (1 ، 2 ، 3) والانتقائية 150 ضعفًا على HDAC8 والفئة IIb HDAC6 الشكل الإسوي.
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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