A potent and selective inhibitor of PI3Kδ (Ki = 79 pM); has >1

GSK2292767 – 1 mg

Brand:
Cayman
CAS:
1254036-66-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM).{32991} It has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ with Ki values of 501, 630, and 501 nM, respectively. GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. It inhibits IFN-γ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay. GSK2292767 also protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation.  

 

Out of stock

Add to quotes
SKU: 21757 - Category:

Description

A potent and selective inhibitor of PI3Kδ (Ki = 79 pM); has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ (Kis = 501, 630, and 501 nM, respectively); >100-fold selective for PI3Kδ over a panel of 250 kinases; inhibits IFNγ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay; protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation,

Formal name: rel-N-[5-[4-[5-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]-methanesulfonamide

Synonyms: 

Molecular weight: 512.6

CAS: 1254036-66-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity

Related products

  • 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
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 10 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 10 mg

    Available on backorder

    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 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 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • 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