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JAK/HDAC-IN-1

Names

[ CAS No. ]:
2284621-75-4

[ Name ]:
JAK/HDAC-IN-1

Biological Activity

[Description]:

JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> JAK
Signaling Pathways >> Epigenetics >> JAK
Signaling Pathways >> Stem Cell/Wnt >> JAK
Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Signaling Pathways >> Epigenetics >> HDAC

[Target]

JAK2:4 nM (IC50)

JAK1:4.8 nM (IC50)

JAK3:7.4 nM (IC50)

Tyk2:49 nM (IC50)

HDAC:2 nM (IC50)

HDAC2:14 nM (IC50)

HDAC6:120 nM (IC50)

HDAC8:2470 nM (IC50)


[In Vitro]

JAK/HDAC-IN-1 (Compound 8m) exhibits IC50s of 4.8, 7.4 and 49 nM for JAK1, JAK3 and TYK2, and 14, 120, 2470 nM for HDAC2, HDAC6 and HDAC8, respectively[1].

[References]

[1]. Liang X, et al. Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies. J Med Chem. 2019 Apr 25;62(8):3898-3923.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H21Cl2N7O2

[ Molecular Weight ]:
450.32

Related Compounds