A selective inhibitor of 12-LO (IC50 = 0.34 µM) with greatly reduced potency for 15-LO-1

ML355 – 10 mg

Brand:
Cayman
CAS:
1532593-30-8
Storage:
-20
UN-No:
Non-Hazardous - /

Platelet-type 12-lipoxygenase (12-LO; Item No. 10341) catalyzes the formation of 12-HpETE (Item No. 44570) from arachidonic acid (Item No. 90010).{3606} It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines.{25127} It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function.{25127} ML355 is a selective inhibitor of 12-LO with an IC50 value of 0.34 µM.{25127} It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX-1 and -2.{25127} In cell-based assays, ML355 has been shown to decrease calcium mobilization and thrombin receptor PAR4-induced platelet aggregation in patient-derived human platelets and to significantly inhibit arachidonic acid and calcium- ionophore-induced 12-HpETE synthesis in mouse BTC3 cells and human islets.{25127}  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A selective inhibitor of 12-LO (IC50 = 0.34 µM) with greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX1/2; decreases platelet aggregation in patient-derived human platelets and inhibits arachidonic acid and calcium ionophore-induced 12-HpETE in mouse BTC3 cells and human islets

Formal name: N-2-benzothiazolyl-4-[[(2-hydroxy-3-methoxyphenyl)methyl]amino]-benzenesulfonamide

Synonyms: 

Molecular weight: 441.5

CAS: 1532593-30-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Lipoxygenases||Research Area|Immunology & Inflammation||Research Area|Lipid Biochemistry|Lipoxygenase Pathways

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 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 - 5 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
  • 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 – 10 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 - 10 mg

    Available on backorder

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

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 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 - 50 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page