UNC3230

Phosphatidylinositol-4-phosphate 5-kinase type-1 gamma (PIP5K1C) is a lipid kinase that generates phosphatidylinositol-4,5-bisphosphate (PIP2) in nociceptive dorsal root ganglia (DRG). Pain sensitization is regulated by multiple signaling pathways that are initiated by phospholipase C-mediated hydrolysis of PIP2. UNC3230 is a small molecule inhibitor of PIP5K1C (IC50 = 41 nM, Kd = 51 nM). It does not inhibit any other lipid kinases that regulate phosphoinositide levels, including phosphatidylinositol 3-kinases. At 100 nM, UNC3230 decreases PIP2 membrane levels in cultured DRG neurons by 45% and significantly reduces calcium signaling. At 2 nM, it displays antinociceptive effects in mouse models of chronic pain when administered intrathecally or injected into inflamed hindpaw.Formal Name: 5-[(cyclohexylcarbonyl)amino]-2-(phenylamino)-4-thiazolecarboxamide. CAS Number: 1031602-63-7. Molecular Formula: C17H20N4O2S. Formula Weight: 344.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 0.2 mg/ml. lambdamax: 287, 336 nm. SMILES: O=C(C1CCCCC1)NC2=C(C(N)=O)N=C(S2)NC3=CC=CC=C3. InChi Code: InChI=1S/C17H20N4O2S/c18-14(22)13-16(21-15(23)11-7-3-1-4-8-11)24-17(20-13)19-12-9-5-2-6-10-12/h2,5-6,9-11H,1,3-4,7-8H2,(H2,18,22)(H,19,20)(H,21,23). InChi Key: RZCNASHHHSKTGP-UHFFFAOYSA-N.