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R 59-022 hydrochloride

Catalog No. T72322 CAS 93076-98-3

Synonyms: DKGI-I hydrochloride, Diacylglycerol kinase inhibitor I hydrochloride, DKGI-I hydrochloride ; Diacylglycerol kinase inhibitor I hydrochloride

R 59-022 hydrochloride (DKGI-I hydrochloride) is a 5-HT Receptor antagonist that activates protein kinase C (PKC).R 59-022 hydrochloride is a DGK inhibitor (IC50:2.8 µM) that inhibits the phosphorylation of OAG to OAPA.R 59-022 enhances thrombin-induced triglyceride production in platelets and inhibits the production of phosphatidic acid in neutrophils. R 59-022 enhances thrombin-induced diglyceride production in platelets and inhibits phosphatidic acid production in neutrophils.

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R 59-022 hydrochloride Chemical Structure

R 59-022 hydrochloride, CAS 93076-98-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 478.00
100 mg	In stock	$ 688.00
500 mg	In stock	$ 1,420.00

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Purity: 97.7%

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Description	R 59-022 hydrochloride (DKGI-I hydrochloride) is a 5-HT Receptor antagonist that activates protein kinase C (PKC).R 59-022 hydrochloride is a DGK inhibitor (IC50:2.8 µM) that inhibits the phosphorylation of OAG to OAPA.R 59-022 enhances thrombin-induced triglyceride production in platelets and inhibits the production of phosphatidic acid in neutrophils. R 59-022 enhances thrombin-induced diglyceride production in platelets and inhibits phosphatidic acid production in neutrophils.
Targets&IC50	DGK:2.8 µM
In vitro	R 59-022 (10 μM; 1 min) Hydrochloride enhances platelet aggregation.[1] R 59-022 (30 μM; 0-60 min) Hydrochloride increases the release of norepinephrine in chromaffin cells.[2] R 59-022 (40 μM; 30 min) Hydrochloride activates PKC in HeLa and U87 cells.[3] R 59-022 (0-10 μM; 4 h) Hydrochloride blocks the entry of EBOV GP into Vero cells.[4]
In vivo	R 59-022 (2 mg/kg; i.p.; 12 days) significantly increased the median survival of SCID mice implanted with U87 GBM cells.[6]

Synonyms	DKGI-I hydrochloride, Diacylglycerol kinase inhibitor I hydrochloride, DKGI-I hydrochloride ; Diacylglycerol kinase inhibitor I hydrochloride
Molecular Weight	496.04
Formula	C27H27ClFN3OS
CAS No.	93076-98-3

Storage

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

References and Literature

1. Nunn DL, et al. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochem J. 1987;243(3):809-813. 2. Jones JA, et al. Influence of phorbol esters, and diacylglycerol kinase and lipase inhibitors on noradrenaline release and phosphoinositide hydrolysis in chromaffin cells. Br J Pharmacol. 1990;101(3):521-526. 3. Boroda S, et al. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017;123:29-39. 4. Stewart CM, et al. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells. Viruses. 2019;11(3):206. 5. 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;260(29):15762-15770. 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;3(7):782-797.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Membrane Protein-targeted Compound Library Inhibitor Library TGF-beta/Smad Compound Library GPCR Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Bioactive Compound Library Neurotransmitter Receptor Compound Library

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Keywords

R 59-022 hydrochloride 93076-98-3 Chromatin/Epigenetic Cytoskeletal Signaling GPCR/G Protein Neuroscience PKC 5-HT Receptor R 59-022 Hydrochloride Diacylglycerol kinase inhibitor I Hydrochloride DKGI-I Hydrochloride DKGI-I hydrochloride Diacylglycerol kinase inhibitor I hydrochloride DKGI-I hydrochloride ; Diacylglycerol kinase inhibitor I hydrochloride inhibitor inhibit

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