R 59022

CAS No. 93076-89-2

R 59022( R 59-022 | R59022 )

Catalog No. M16660 CAS No. 93076-89-2

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    R 59022
  • Note
    Research use only, not for human use.
  • Brief Description
    A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM.
  • Description
    A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets; concomitantly stimulates PKC activity, selectively suppresses U46619-induced enhancement of mouse portal vein contraction under high glucose conditions; also induces caspase-mediated apoptosis in glioblastoma cells and in other cancers, but lacks toxicity in noncancerous cells.
  • In Vitro
    Western Blot Analysis Cell Line:HeLa cells Concentration:40 uM Incubation Time:30 min Result:Increased the phosphorylation of PKC downstream targets by about 2.5-fold.
  • In Vivo
    Animal Model:SCID mice implanted with U87 GBM cells Dosage:10 mg/kg Administration:Intraperitoneal injection (i.p.) Result:Increased median survival and decreased tumor volume.
  • Synonyms
    R 59-022 | R59022
  • Pathway
    Others
  • Target
    DGK
  • Recptor
    DGK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    93076-89-2
  • Formula Weight
    459.58
  • Molecular Formula
    C27H26FN3OS
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 62.5 mg/mL (135.99 mM)
  • SMILES
    O=C1C(CCN2CC/C(CC2)=C(C3=CC=C(F)C=C3)\C4=CC=CC=C4)=C(C)N=C5N1C=CS5
  • Chemical Name
    6-[2-[4-[(4-Fluorophenyl)phenylmethylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Dominguez CL, et al. Cancer Discov. 2013 Jul;3(7):782-97. 2. de Chaffoy de Courcelles DC, et al. J Biol Chem. 1985 Dec 15;260(29):15762-70. 3. Nunn DL, et al. Biochem J. 1987 May 1;243(3):809-13. 4. Nobe K, et al. Br J Pharmacol. 2004 Sep;143(1):166-78.
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  • R 59022

    A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM.