HDAC8/BRPF1-IN-1

Names

[ CAS No. ]:
2484255-85-6

[ Name ]:
HDAC8/BRPF1-IN-1

Biological Activity

[Description]:

HDAC8/BRPF1-IN-1 (Compound 23a) is a dual inhibitor of HDAC8 and BRPF1 with an IC50 of 443 nM against human HDAC8 and a Kd of 67 nM against human BRPF1. HDAC8/BRPF1-IN-1 shows low in vitro activity against HDAC1 and 6[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Signaling Pathways >> Epigenetics >> HDAC
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

hHDAC8:443 nM (IC50)

hBRPF1:67 nM (Ki)


[In Vitro]

HDAC8/BRPF1-IN-1 (Compound 23a) (4-100 μM; 24 h) shows antiproliferative activity against acute myeloid leukemia cells[1]. Cell Proliferation Assay[1] Cell Line: Acute myeloid leukemia cells THP-1 and HL60 Concentration: 4, 20 and 100 μM Incubation Time: 24 h Result: Inhibited THP-1 and HL60 cells growth.

[References]

[1]. Ghazy E, et al. Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. Eur J Med Chem. 2020 Aug 15;200:112338.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H19N3O6S

[ Molecular Weight ]:
417.44

Related Compounds