An inhibitor of RalA and RalB; binds to RalB when it is bound to GDP (Kd = 7.7 µM); decreases RalA and RalB activity in H2122 and H358 cells at 10 µM; inhibits colony formation of Ral-dependent H2122 and H358 cells (IC50s = 2 and 1.3 µM

BQU57 – 25 mg

Brand:
Cayman
CAS:
1637739-82-2
Storage:
-20
UN-No:
Non-Hazardous - /

BQU57 is an inhibitor of the Ras-like GTPases RalA and RalB.{27339} It binds to RalB when RalB is bound to GDP with a Kd value of 7.7 µM, as determined by isothermal titration calorimetry (ITC). BQU57 (10 µM) decreases RalA and RalB activity in H2122 and H358 cells. It also inhibits colony formation of Ral-dependent H2122 and H358 cells (IC50s = 2 and 1.3 µM, respectively) but not Ral-independent H460 and Calu-6 cells. BQU57 (10, 20, and 50 mg/kg per day) decreases RalA and RalB, but not Ras or RhoA, activity and reduces tumor growth in a dose-dependent manner in an H2122 mouse xenograft model.  

 

Out of stock

Add to quotes
SKU: - Category:

Description

An inhibitor of RalA and RalB; binds to RalB when it is bound to GDP (Kd = 7.7 µM); decreases RalA and RalB activity in H2122 and H358 cells at 10 µM; inhibits colony formation of Ral-dependent H2122 and H358 cells (IC50s = 2 and 1.3 µM, respectively); decreases RalA and RalB activity and reduces tumor growth in an H2122 mouse xenograft model at 10, 20, and 50 mg/kg

Formal name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile

Synonyms: 

Molecular weight: 334.3

CAS: 1637739-82-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|GTPases

Related products

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

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 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 - 25 mg

    Available on backorder

    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 – 50 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 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 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 - 100 µg

    Available on backorder

    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
    View product page