R 59-022 (hydrochloride)

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].

Product Specifications

CAS Number

[93076-98-3]

Product Name Alternative

DKGI-I (hydrochloride) ; Diacylglycerol kinase inhibitor I (hydrochloride)

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-immunoregulation

Field of Research

Cancer; Infection; Inflammation/Immunology

Assay Protocol

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

Purity

98.88

Solubility

DMSO : 25 mg/mL (ultrasonic)

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

Molecular Formula

C27H27ClFN3OS

Molecular Weight

496.04

Precautions

P264-P270-P280-P302+P352-P305+P351+P338-P330-P362+P364-P501

References & Citations

[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.