R-59-022

Diacylglycerol (DAG) kinases (DGKs) phosphorylate DAG to give phosphatidic acid (PA), reducing signaling through DAG and increasing signaling through PA. R-59-022 is an inhibitor of DGK (IC50 = 2.8 µM). This results in increased DAG-dependent PKC activity and potentiates aggregation of thrombin-stimulated platelets. R-59-022 also blocks vascular contraction induced by the thromboxane analog U-46619 (Cay-16450). At 10 µM, R-59-022 induces apoptosis in glioblastoma cells without being toxic to non-cancerous cells. It inhibits DGK-theta in vitro at concentrations below 1 µM and blocks DGK-theta activity in vivo. R-59-022 also inhibits A. thaliana DGK2 (IC50 = 50 µM) and suppresses root growth but does not affect DGK7 at 50 µM.Formal Name: 6-[2-[4-[(4-fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one. CAS Number: 93076-89-2. Synonyms: Diacylglycerol Kinase Inhibitor I. Molecular Formula: C27H26FN3OS. Formula Weight: 459.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS(pH7.2) (1:2): 0.25 mg/ml, DMSO: 5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 228, 324 nm. SMILES: FC1=CC=C(/C(C2=CC=CC=C2)=C3CCN(CCC4=C(C)N=C(SC=C5)N5C4=O)CC\3)C=C1. InChi Code: InChI=1S/C27H26FN3OS/c1-19-24(26(32)31-17-18-33-27(31)29-19)13-16-30-14-11-22(12-15-30)25(20-5-3-2-4-6-20)21-7-9-23(28)10-8-21/h2-10,17-18H,11-16H2,1H3. InChi Key: MFVJXLPANKSLLD-UHFFFAOYSA-N.