A myeloperoxidase inhibitor (Ki = 346.74 nM in a cell-free assay); selective for MPO over TPO and a panel of more than 50 enzymes

PF-1355 – 1 mg

Brand:
Cayman
CAS:
1435467-38-1
Storage:
-20
UN-No:
Non-Hazardous - /

PF-1355 is an irreversible myeloperoxidase (MPO) inhibitor (Ki = 346.74 nM in a cell-free assay).{51086} It is selective for MPO over thyroid peroxidase (TPO) and over a panel of more than 50 enzymes, receptors, transporters, and ion channels. It inhibits MPO activity in isolated human whole blood with an IC50 value of 1.5 µM. PF-1355 reduces MPO activity in plasma and peritoneal lavage fluid in a mouse model of peritonitis.{51087} It also reduces lung edema, decreases plasma levels of TNF-α, MCP-1/CCL2, MIP-2/CXCL2, and KC/CXCL1 and transiently increases and then reduces neutrophil levels in bronchoalveolar lavage fluid (BALF) in a mouse model of pulmonary immune complex vasculitis when administered at doses of 20 and 100 mg/kg.  

 

Out of stock

Add to quotes
SKU: 22222 - Category:

Description

A myeloperoxidase inhibitor (Ki = 346.74 nM in a cell-free assay); selective for MPO over TPO and a panel of more than 50 enzymes, receptors, transporters, and ion channels; inhibits MPO activity in isolated human whole blood (IC50 = 1.5 µM); reduces lung edema, decreases plasma levels of TNF-α, MCP-1/CCL2, MIP-2/CXCL2, and KC/CXCL1 and transiently increases and then reduces neutrophil levels in BALF in a mouse model of pulmonary immune complex vasculitis at 20 and 100 mg/kg

Formal name: 6-(2,5-dimethoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-1(2H)-pyrimidineacetamide

Synonyms:  PF-06281355

Molecular weight: 321.4

CAS: 1435467-38-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ox Stress Reagents|Antioxidants||Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cardiovascular System|Cardiovascular Diseases||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Immunology & Inflammation|Innate Immunity

Related products

  • 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 – 1 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 - 1 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
  • 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 – 500 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 - 500 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 – 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