1. Epigenetics
    TGF-beta/Smad
    GPCR/G Protein
    Neuronal Signaling
  2. PKC
    5-HT Receptor
  3. R 59-022

R 59-022 (Synonyms: DKGI-I; Diacylglycerol kinase inhibitor I)

Cat. No.: HY-107613 Purity: >99.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

R 59-022 Chemical Structure

R 59-022 Chemical Structure

CAS No. : 93076-89-2

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10 mM * 1 mL in DMSO USD 354 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target[1][2][3]

PKC

 

serotonin

 

diacylglycerol kinase

2.8 μM (IC50)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

459.58

Formula

C₂₇H₂₆FN₃OS

CAS No.

93076-89-2

SMILES

O=C1C(CCN(CC/2)CCC2=C(C3=CC=CC=C3)/C4=CC=C(F)C=C4)=C(C)N=C5N1C=CS5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: >99.0%

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Keywords:

R 59-022DKGI-I Diacylglycerol kinase inhibitor IPKC5-HT ReceptorProtein kinase CSerotonin Receptor5-hydroxytryptamine ReceptorthrombinplateletsphosphatidicacidneutrophilsfilovirusviralEBOVInhibitorinhibitorinhibit

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R 59-022
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