DIACYLGLYCEROL KINASE INHIBITOR I

Product Name: DIACYLGLYCEROL KINASE INHIBITOR I
CAS No.: 93076-89-2
Chemical Name: DIACYLGLYCEROL KINASE INHIBITOR I
Synonyms: DKI;DAGK;DGKE;DGKI;DAGK4;DAGK7;DGK-θ;DAGK2;R59022;DKGI-I
CBNumber: CB3335279
Molecular Formula: C27H26FN3OS
Formula Weight: 459.58
MOL File: 93076-89-2.mol

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DIACYLGLYCEROL KINASE INHIBITOR I Property

Boiling point:: 619.8±65.0 °C(Predicted)
Density: 1.26±0.1 g/cm3(Predicted)
storage temp.: -20°C
solubility: 0.1 M HCl: slightly soluble
form: solid
pka: 7.76±0.20(Predicted)
color: pale yellow
biological source: synthetic (organic)
Stability:: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

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Safety

Safety Statements: 23-24/25
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: D5919
Product name: Diacylglycerol Kinase Inhibitor I
Purity: solid
Packaging: 1mg
Price: $131
Updated: 2025/07/31

Sigma-Aldrich

Product number: 266785
Product name: Diacylglycerol Kinase Inhibitor I
Packaging: 5mg
Price: $177
Updated: 2025/07/31

Cayman Chemical

Product number: 16772
Product name: R-59-022
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 16772
Product name: R-59-022
Purity: ≥98%
Packaging: 5mg
Price: $90
Updated: 2024/03/01

Sigma-Aldrich

Product number: D5919
Product name: Diacylglycerol Kinase Inhibitor I
Purity: solid
Packaging: 5mg
Price: $452
Updated: 2025/07/31

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DIACYLGLYCEROL KINASE INHIBITOR I Chemical Properties,Usage,Production

Description

R-59022 (93076-89-2) is a diacylglycerol kinase (DAGK) inhibitor, nonselective for DAGK isotypes (IC50=2.8 μM in intact platelets).1 Induces autophagy and apoptosis in NG108-15 neuronal cells via an mTOR-independent mechanism.2 Prevents conjugated linoleic acid-mediated inflammatory signaling and insulin resistance in human adipocytes.3 Blocks filovirus internalization in host cells.4

Uses

R-59-022 acts as an inducer of apoptosis in glioblastoma cells and avoids apoptosis in non-cancerous cells. This selectivity makes this drug a highly effective anti-cancer agent. Diacylglycerol Kinase inhibitor.

Definition

ChEBI: 6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]-1-piperidinyl]ethyl]-7-methyl-5-thiazolo[3,2-a]pyrimidinone is a diarylmethane.

Biological Activity

Diacylglycerol (DAG) kinase inhibitor (IC 50 = 2.8 μ M); increases protein kinase C activity. Potentiates thrombin-induced platelet aggregation and induces neutrophil chemotaxis. Inhibits U46619-induced contractions in mouse aorta and porcine coronary artery.

in vivo

R 59-022 (2 mg/kg, i.p., 12 days) significantly increases median survival in SCID mice implanted with U87 GBM cells^[6].

Animal Model:	SCID mice implanted with U87 GBM cells^[6]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection (i.p.)
Result:	Increased median survival and decreased tumor volume.

IC 50

PKC; serotonin; diacylglycerol kinase: 2.8 μM (IC₅₀)

References

[1] D C DE CHAFFOY DE COURCELLES H V B P Roevens. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet.[J]. The Journal of Biological Chemistry, 1985, 260 29: 15762-15770.
[2] TSUYOSHI TAKITA. Diacylglycerol kinase inhibitor R59022-induced autophagy and apoptosis in the neuronal cell line NG108-15[J]. Archives of biochemistry and biophysics, 2011, 509 2: Pages 197-201. DOI:10.1016/j.abb.2011.02.007
[3] KRISTINA MARTINEZ. Diacylglycerol kinase inhibitor R59022 attenuates conjugated linoleic acid-mediated inflammation in human adipocytes.[J]. Journal of Lipid Research, 2013, 54 3: 662-670. DOI:10.1194/jlr.m031211
[4] CORINA M STEWART. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells.[J]. Viruses-Basel, 2019, 11 3. DOI:10.3390/v11030206

DIACYLGLYCEROL KINASE INHIBITOR I Preparation Products And Raw materials

Raw materials

Preparation Products

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DIACYLGLYCEROL KINASE INHIBITOR I Suppliers

China 70 Germany 2 Japan 2 Switzerland 2 United Kingdom 2 United States 13 Global 91

3B Pharmachem (Wuhan) International Co.,Ltd.

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93076-89-2, DIACYLGLYCEROL KINASE INHIBITOR IRelated Search:

TRIS(2,2,6,6-TETRAMETHYL-3,5-HEPTANEDIONATO)DYSPROSIUM(III) SALCOMINE COBALT(II) ACETYLACETONATE DICHLORO(ETHYLENEDIAMINE)PLATINUM(II) Ritanserin TERT-BUTYL ISOCYANIDE Cupric acetylacetonate METHYL ISOCYANOACETATE TRIS(2,2,6,6-TETRAMETHYL-3,5-HEPTANEDIONATO)EUROPIUM(III) Aluminum acetylacetonate Tris(2,4-pentanedionato)chroMiuM(III) Benzyl isocyanide Ethyl isocyanoacetate PHENYLSELENOL 1,1,3,3-TETRAMETHYLBUTYL ISOCYANIDE Tosylmethyl isocyanide 2,4-PENTANEDIONE, SILVER DERIVATIVE N-BUTYLISOCYANIDE

6-[2-[4-[(P-FLUOROPHENYL)PHENYLMETHYLENE]-1-PIPERIDINYL]ETHYL]-7-METHYL-5H-THIAZOLO(3,2-A)PYRIMIDINE-5-ONE

6-[2-[(4-FLUOROPHENYL)PHENYLMETHYLENE]-1-PIPERIDINYL)ETHYL]-7-METHYL-5H-THIAZOLO-[3,2-A]-PYRIMIDIN-5-ONE

6-[2-[4-[(4-FLUOROPHENYL)PHENYLMETHYLENE]-1-PIPERIDINYL]ETHYL]-7-METHYL-5H-THIAZOLO[3,2-A]PYRIMIDIN-5-ONE

DIACYLGLYCEROL KINASE

DIACYLGLYCEROL KINASE INHIBITOR I

DIACYLGLYCEROL KINASE INHIBITOR I (R59 022)

DAGK

DAG KINASE

EC 2.7.1.107

EC: 2.7.1.107

DKI

SN-1,2-DIACYLGLYCEROL KINASE

SN-1,2-DIACYLGLYCEROL KINASE, RECOMBINANT, E COLI

R59022

DIACYLGLYCEROL KINASE FROM E. COLI

6-[2-[4-[(4-fluorophenyl)phenylmethylene]-1-piperidin-yl]ethyl]-7-methyl-5h-thiazolo-[3,2-a]-pyrimidin-5-one

DIACYLGLYCEROL KINASE SOLUTION

R59022, 6-[2-[4-[(4-Fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo-[3,2-a]-pyrimidin-5-one

Diacylglycerol Kinase from Escherichia coli

sn-1,2-Diacylglycerol kinase, DAGK

5H-Thiazolo(3,2-A)pyrimidin-5-one, 6-(2-(4-((4-fluorophenyl)phenylmethylene)-1-piperidinyl)ethyl)-7-methyl-

6-(2-(4-((4-Fluorophenyl)phenylmethylene)-1-piperidinyl)ethyl)-7-methyl-5H-thiazolo(3,2-A)pyrimidine-5-one

6-[2-[4-[(4-Fluorophenyl)phenylMethylene]-1-piperidin-yl]ethyl]-7-Methyl-5H-thiazolo-[3,2-a]-pyriMidin-5-one, R59022

DGKE

Anti-DGKQ, C-Terminal antibody produced in rabbit

DAGK4

DAGK7

DGK-θ

Anti-DGKI, C-Terminal antibody produced in rabbit

DGKI

Diglyceride kinase κ

Anti-DGKD, N-Terminal antibody produced in rabbit

6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one

Diacylglycerol Kinase Inhibitor I - CAS 93076-89-2 - Calbiochem

DKGI-I

R 59022,R 59 022

6-(2-(4-((4-Fluorophenyl)(phenyl)methylene)piperidin-1-yl)ethyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one

DAGK2

KIAA0718

93076-89-2

Diacylglycerol kinase (DAGK)

Enzymes, Inhibitors, and Substrates

Signal Transduction

Serine/Threonine Kinase Inhibitors

Kinase/Phosphatase Biology

Cell Biology

Cell Signaling and Neuroscience

Cell Signaling Enzymes

Application Index

Biochemicals and Reagents

BioChemical

Lipid signaling