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PKC-theta inhibitor 1

Names

[ CAS No. ]:
1160501-81-4

[ Name ]:
PKC-theta inhibitor 1

Biological Activity

[Description]:

PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis[1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC
Research Areas >> Inflammation/Immunology
Signaling Pathways >> TGF-beta/Smad >> PKC

[Target]

PKCθ:6 nM (Ki)

PKCδ:392 μM (Ki)

PKCα:1020 μM (Ki)

IL-2 production:0.19 μM (IC50)


[References]

[1]. Collier PN, et al. Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis. ACS Med Chem Lett. 2019 Jun 27;10(8):1134-1139.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H15F3N4O

[ Molecular Weight ]:
348.32

Related Compounds