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R 59-022 (hydrochloride)
$110 – $580
Products Details
Product Description
– R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4].
Web ID
– HY-107613A
Storage Temperature
– -20°C, 3 years (Powder)
Shipping
– Blue Ice
Applications
– COVID-19-immunoregulation
Molecular Formula
– C27H27ClFN3OS
References
– [1]de Chaffoy de Courcelles, D.C., et al. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet. J. Biol. Chem. 260(29), 15762-15770 (1985). |[2]Nunn DL, et al. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochem J. 1987 May 1;243(3):809-13. |[3]Jones JA, et al. Influence of phorbol esters, and diacylglycerol kinase and lipase inhibitors on noradrenalinerelease and phosphoinositide hydrolysis in chromaffin cells. Br J Pharmacol. 1990 Nov;101(3):521-6. |[4]Boroda S, et al. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017 Jan 1;123:29-39. |[5]Stewart CM, et al. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells. Viruses. 2019 Mar 1;11(3). pii: E206. |[6]Dominguez CL, et al. Diacylglycerol kinase α is a critical signaling node and novel therapeutic target in glioblastoma and other cancers. Cancer Discov. 2013 Jul;3(7):782-97.
CAS Number
– 93076-98-3
Molecular Weight
– 496.04
Compound Purity
– 98.88
SMILES
– O=C1C(CCN(CC/2)CCC2=C(C3=CC=CC=C3)/C4=CC=C(F)C=C4)=C(C)N=C5N1C=CS5.[H]Cl
Clinical Information
– No Development Reported
Research Area
– Cancer; Infection; Inflammation/Immunology
Solubility
– DMSO : 25 mg/mL (ultrasonic)
Target
– 5-HT Receptor;PKC
Isoform
– 5-HT Receptor;PKC
Pathway
– Epigenetics;GPCR/G Protein;Neuronal Signaling;TGF-beta/Smad
Product type
– Reference compound
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