HDAC6/8/BRPF1-IN-1

Names

[ CAS No. ]:
2484255-65-2

[ Name ]:
HDAC6/8/BRPF1-IN-1

Biological Activity

[Description]:

HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer[1].

[Related Catalog]:

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

[Target]

HDAC1:797 nM (IC50)

HDAC6:344 nM (IC50)

HDAC8:908 nM (IC50)


[In Vitro]

HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively[1]. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM[1].

[References]

[1]. Ehab Ghazy, 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 ]:
C18H17N3O5S

[ Molecular Weight ]:
387.41

Related Compounds