A dual inhibitor of FTase and GGTase I (IC50s = 2 and 98 nM

L-778,123 – 25 mg

Brand:
Cayman
CAS:
183499-57-2
Storage:
-20
UN-No:
Non-Hazardous - /

L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50 = 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50 = 98 nM).{41263} It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner. Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and Rap1a prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on Ki-Ras prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL2 cells (IC50 = 0.81 μM).{41264}  

 

Available on backorder

Add to quotes
SKU: 32504 - 25 mg Category:

Description

A dual inhibitor of FTase and GGTase I (IC50s = 2 and 98 nM, respectively); inhibits prenylation of FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively); inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner; reduces HDJ2 and Rap1a prenylation ex vivo in dog PBMCs when administered at a dose of 35-50 mg/kg per day; has no effect on Ki-Ras prenylation in patient-derived PBMCs; inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively); inhibits IL-2-induced proliferation of CTLL2 cells (IC50 = 0.81 μM)

Formal name: 4-[[5-[[4-(3-chlorophenyl)-3-oxo-1-piperazinyl]methyl]-1H-imidazol-1-yl]methyl]-benzonitrile

Synonyms: 

Molecular weight: 405.9

CAS: 183499-57-2

Purity: ≥95%

Formulation: A crystalline solid

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 250 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 1 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 10 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 100 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page