2484255-85-6

2484255-85-6 structure

Name: HDAC8/BRPF1-IN-1
Chemical Name: HDAC8/BRPF1-IN-1
CAS Number: 2484255-85-6
Molecular Formula: C₁₉H₁₉N₃O₆S
Molecular Weight: 417.44
Catalog: Signaling Pathways Cell Cycle/DNA Damage HDAC
Create Date: 2022-11-21 15:10:47
Modify Date: 2024-01-30 19:14:14
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].

Name	HDAC8/BRPF1-IN-1

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.

Molecular Formula	C₁₉H₁₉N₃O₆S
Molecular Weight	417.44