R 59-022

R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM) . R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC) . R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4].

Product Specifications

CAS Number

[93076-89-2]

Product Name Alternative

DKGI-I; Diacylglycerol kinase inhibitor I

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

5-HT Receptor; PKC

Type

Reference compound

Related Pathways

Epigenetics; GPCR/G Protein; Neuronal Signaling; TGF-beta/Smad

Applications

COVID-19-anti-virus

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/r-59-022.html

Purity

99.82

Solubility

DMSO : 125 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1C(CCN(CC/2)CCC2=C(C3=CC=CC=C3)/C4=CC=C(F)C=C4)=C(C)N=C5N1C=CS5

Molecular Formula

C27H26FN3OS

Molecular Weight

459.58

Precautions

H302, H315, H319

References & Citations

[1]de Chaffoy de Courcelles DC, 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. 1985 Dec 15;260 (29) :15762-70.|[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.