A potent PDE4 inhibitor (IC50s = 4.9

GSK256066 – 1 mg

Brand:
Cayman
CAS:
801312-28-7
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).{47799} It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-fold selective over PDE7. GSK256066 inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM). Intratracheal administration of GSK256066 inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg). It inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg).{47800}  

 

Available on backorder

Add to quotes
SKU: 28012 - 1 mg Category:

Description

A potent PDE4 inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively); >380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and >2,500-fold selective over PDE7; inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM); intratracheal adminstration inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg); inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg)

Formal name: 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide

Synonyms: 

Molecular weight: 518.6

CAS: 801312-28-7

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases

Related products

  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 500 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 500 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • 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 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 – 25 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 - 25 mg

    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 – 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
    Add to quotes
    View product page