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R 59-022

CAT: 0804-HY-107613-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-107613-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
MUC4; PKC

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Alternative Products

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B2975-5R-59-022
E7773-1mgR 59-022
T72322-01R 59-022 hydrochloride
256394-01R 59-022 discontinued. See 463438
463438-01R-59-022 (Diacylglycerol Kinase Inhibitor I)
463439R-59-022-d5 (Mono-defluoro Ritanserin-d5)
B6725-10YM 022
532982YM-022

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