R 59022

diacylglycerol kinase inhibitor; structure given in first source; platelet activator factor antagonist
Also Known As:
6-(2-(4-((4-fluorophenyl)phenylmethylene)-1-piperidinyl)ethyl)-7-methyl-5H-thiazolo(3,2-a)pyrimidine-5-one; R 59-022; R-59 022; R59022
Networked: 7 relevant articles (0 outcomes, 0 trials/studies)

Bio-Agent Context: Research Results


1. Xin, Wenjun: 1 article (07/2013)
2. Floyd, Desiree H: 1 article (07/2013)
3. Abounader, Roger: 1 article (07/2013)
4. Purow, Benjamin W: 1 article (07/2013)
5. Harris, Thurl E: 1 article (07/2013)
6. Kefas, Benjamin A: 1 article (07/2013)
7. Mullins, Garrett R: 1 article (07/2013)
8. Yacur, Melissa N: 1 article (07/2013)
9. Xiao, Aizhen: 1 article (07/2013)
10. Dominguez, Charli L: 1 article (07/2013)

Related Diseases

1. Neoplasms (Cancer)
03/01/1993 - "The present results show that the DAG kinase inhibitor, R 59022, suppressed tumor cell polarity and strongly inhibited cell locomotion at a concentration of 10(-4), thus supporting the earlier finding that an increased availability of DAGs can suppress the locomotor activity of Walker carcinosarcoma cells. "
11/13/1987 - "Neutrophils treated with formyl-peptide fMet-Leu-Phe did not display tumoricidal response, but the addition of diacylglycerol kinase inhibitor R59022 together with formyl-peptide induced the cytotoxic capacity against tumor target cells. "
07/01/2013 - "The attenuation of DGKα activity via DGKα-targeting siRNA and small-molecule inhibitors R59022 and R59949 induced caspase-mediated apoptosis in glioblastoma cells and in other cancers, but lacked toxicity in noncancerous cells. "
05/01/1990 - "Our conclusion that PKC is an essential component in the regulation of myoblast fusion is based in part on the following evidence: (1) an activator of PKC, the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA), at low concentration and for a brief exposure period, induces precocious fusion and stimulates Ca2+ influx; (2) 4 alpha-phorbol-12,13-didecanoate, an inactive analog of TPA, has no discernible effect on fusion or Ca2+ influx; (3) 1-oleoyl-2-acetyl glycerol, an analog of endogenous diacylglycerol (DAG) which activates PKC, promotes precocious fusion, as does the DAG kinase inhibitor R59022 (6-[2-[4-[(4-fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7- methyl-5H-thiazole-[3,2 alpha]-pyrimidin-5-one) which raises the level of endogenous DAG by inhibiting its catabolism; (4) 1-(5-isoquinolinesulfonyl)-2-methylpiperazine (H-7), a highly potent PKC inhibitor, reversibly blocks myogenesis at a point between alignment and fusion; and (5) H-7 also blocks the normal increase in Ca2+ influx preceding fusion."
2. Neuroblastoma
3. Insulin Resistance
4. Inflammation
5. Glioma (Gliomas)

Related Drugs and Biologics

1. Diacylglycerol Kinase
2. Protein Kinase Inhibitors
3. Small Interfering RNA (siRNA)
4. alpha-Tocopherol
5. Linoleic Acid (Linoleate)
6. 1- (5- Isoquinolinesulfonyl)- 2- Methylpiperazine (H 7)
7. Guanosine 5'-O-(3-Thiotriphosphate)
8. Tamoxifen
9. Polymyxin B (Aerosporin)
10. Inositol Phosphates