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R 59-022

Catalog No. T16709 CAS 93076-89-2

Synonyms: Diacylglycerol kinase inhibitor I, DKGI-I

R 59-022 is a 5-HTR antagonist and activates protein kinase C (PKC). R 59-022 is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.

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R 59-022, CAS 93076-89-2

Pack Size	Availability	Price/USD
1 mg	35 days	$ 93.00
5 mg	35 days	$ 225.00
10 mg	35 days	$ 393.00
50 mg	35 days	$ 1,670.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	R 59-022 is a 5-HTR antagonist and activates protein kinase C (PKC). R 59-022 is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
Targets&IC50	DGK:2.8 μM
In vitro	R 59-022 is able to interrupt thrombin-induced inositol lipid cycling at the level of diacylglycerol and leads to an elevation of protein kinase C activity, in the intact platelet. R 59-022 blocks entry of EBOV pseudotypes in a concentration-dependent manner (IC50: ~5 μM). R 59-022, an inhibitor of filovirus entry, prevents the macropinocytic uptake of filoviral particles, inhibits entry mediated by multiple filovirus GPs, and blocks replicative EBOV growth. R 59-022 dose-dependent decreases in entry by the VLPs harboring the EBOV GP (IC50: ~2 μM). R 59-022 (10 μM) potentiates aggregation, but not shape change induced by sub-maximal concentrations of thrombin. R59022 (10 μM) had no significant effect on the dose-response curve for the mobilization of intracellular Ca2+ by thrombin in either the presence or the absence of extracellular Ca2+. R 59-022 (2-12 μM; 1 hour) can inhibit EBOV GP-mediated entry in multiple cell types. R 59-022 (5 μM; 30 minutes) blocks macropinocytosis in vero cells[1][2][5].

Synonyms	Diacylglycerol kinase inhibitor I, DKGI-I
Molecular Weight	459.58
Formula	C27H26FN3OS
CAS No.	93076-89-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

R 59-022 93076-89-2 Others R 59022 Diacylglycerol kinase inhibitor I DKGI-I R 59 022 inhibitor inhibit

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