PKC-theta inhibitor 1

PKC-theta inhibitor 1 is an orally active and selective ATP-competitive inhibitor of Protein Kinase Cθ (PKCθ), with a Ki value of 6 nM. PKC-theta inhibitor 1 inhibits T-cell-mediated inflammatory responses by suppressing the release of proinflammatory cytokines (IL-2 IC50 = 0.21 μM in anti-CD3/CD28-stimulated PBMCs; IL-17 IC50 = 1 μM in CD3/CD28-stimulated Th17 cells) PKC-theta inhibitor 1 significantly reduces symptoms in mice with ongoing experimental autoimmune encephalomyelitis (EAE) . PKC-theta inhibitor 1 can be used for the study of T-cell-mediated inflammatory diseases such as multiple sclerosis[1].

Product Specifications

CAS Number

[1160501-81-4]

UNSPSC

12352005

Target

Interleukin Related; PKC

Type

Reference compound

Related Pathways

Epigenetics; Immunology/Inflammation; TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/pkc-theta-inhibitor-1.html

Purity

99.73

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

NCC1(C2=CC=CC(C3=C4C(NN=C4C(F)(F)F)=NC=C3)=C2)COC1

Molecular Formula

C17H15F3N4O

Molecular Weight

348.32

References & Citations

[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.