| Identification | Back Directory | [Name]
PKC-theta inhibitor 1 | [CAS]
1160501-81-4 | [Synonyms]
PKCθ inhibitor 22
PKC-theta inhibitor 1
PKCtheta inhibitor 1,PKC theta inhibitor 1
3-Oxetanemethanamine, 3-[3-[3-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-4-yl]phenyl]- | [Molecular Formula]
C17H15F3N4O | [MDL Number]
MFCD32201103 | [MOL File]
1160501-81-4.mol | [Molecular Weight]
348.32 |
| Chemical Properties | Back Directory | [Boiling point ]
444.7±55.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
9.65±0.29(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
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. DOI:10.1021/acsmedchemlett.9b00134 |
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