R 59-022
Modify Date: 2025-08-25 17:48:18
R 59-022 structure
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Common Name | R 59-022 | ||
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| CAS Number | 93076-89-2 | Molecular Weight | 459.57800 | |
| Density | 1.26g/cm3 | Boiling Point | 619.8ºC at 760mmHg | |
| Molecular Formula | C27H26FN3OS | Melting Point | N/A | |
| MSDS | USA | Flash Point | 328.6ºC | |
Use of R 59-022R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR 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]. |
| Name | 6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one |
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| Synonym | More Synonyms |
| Description | R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR 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]. |
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| Related Catalog | |
| In Vitro | In the intact platelet, R 59-022 is able to interrupts thrombin-induced inositol lipid cycling at the level of diacylglycerol and leads to an elevation of protein kinase C activity[1]. 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+[2]. 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 blocks entry of EBOV pseudotypes in a concentration-dependent manner (IC50: ~5 µM). R 59-022 dose-dependent decreases in entry by the VLPs harboring the EBOV GP (IC50: ~2 µM). 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[5]. |
| References |
| Density | 1.26g/cm3 |
|---|---|
| Boiling Point | 619.8ºC at 760mmHg |
| Molecular Formula | C27H26FN3OS |
| Molecular Weight | 459.57800 |
| Flash Point | 328.6ºC |
| Exact Mass | 459.17800 |
| PSA | 65.85000 |
| LogP | 5.28180 |
| Index of Refraction | 1.654 |
| InChIKey | MFVJXLPANKSLLD-UHFFFAOYSA-N |
| SMILES | Cc1nc2sccn2c(=O)c1CCN1CCC(=C(c2ccccc2)c2ccc(F)cc2)CC1 |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| Hazard Codes | Xi |
| Safety Phrases | S23-S24/25 |
| RIDADR | NONH for all modes of transport |
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Diacylglycerol kinase epsilon in bovine and rat photoreceptor cells. Light-dependent distribution in photoreceptor cells.
Exp. Eye Res. 112 , 139-50, (2013) The present study shows the selective light-dependent distribution of 1,2-diacylglycerol kinase epsilon (DAGKɛ) in photoreceptor cells from bovine and albino rat retina. Immunofluorescence microscopy ... |
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Insulin action on polyunsaturated phosphatidic acid formation in rat brain: an "in vitro" model with synaptic endings from cerebral cortex and hippocampus.
Neurochem. Res. 34(7) , 1236-48, (2009) The highly efficient formation of phosphatidic acid from exogenous 1-stearoyl-2-arachidonoyl-sn-glycerol (SAG) in rat brain synaptic nerve endings (synaptosomes) from cerebral cortex and hippocampus i... |
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The role of diacylglycerol as a modulator of oxytocin-stimulated phasic contractions in myometrium from pregnant and nonpregnant rats.
Am. J. Obstet. Gynecol. 182(4) , 943-9, (2000) The role of diacylglycerol in the phosphatidylinositol-signaling pathway is to activate protein kinase C. In the myometrium, protein kinase C activation leads to inhibition of phasic contractions. The... |
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Name: Primary cell-based high-throughput screening assay for identification of compounds th...
Source: Johns Hopkins Ion Channel Center
Target: regulator of G-protein signaling 4 isoform 2 [Homo sapiens]
External Id: JHICC_RGS_Act_HTS
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Name: Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro...
Source: NCGC
Target: N/A
External Id: SERCaMPGLuc-p1-antagonist
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Name: Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay
Source: ChEMBL
Target: N/A
External Id: CHEMBL1266185
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Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase
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Name: qHTS Validation Assay for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2...
Source: NCGC
Target: ubiquitin carboxyl-terminal hydrolase 2 isoform a [Homo sapiens]
External Id: UBCH001
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Name: uHTS identification of small molecule activators of the adaptive arm of the Unfolded ...
Source: Burnham Center for Chemical Genomics
Target: N/A
External Id: BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay
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Name: Rescue cell viability in cybrid cells with a genetic mutation in complex 1 of the mit...
Source: ICCB-Longwood/NSRB Screening Facility, Harvard Medical School
Target: N/A
External Id: HMS1315
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Name: High throughput fluorescence intensity-based biochemical assay to screen for small mo...
Source: University of Pittsburgh Molecular Library Screening Center
Target: furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens]
External Id: MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.
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Name: Tocris HTS for Inhibitors of Aerobactin Synthetase lucA
Source: 23265
External Id: IucA Pilot Assay Tocris Library
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Name: Confirmed allosteric antagonists of M1 Muscarinic receptor
Source: 1043
Target: Muscarinic acetylcholine receptor M1
External Id: SAID_435034
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| R 59022 |