An ANO1 channel activator; increases chloride currents in FRT cells expressing human ANO1 (EC50 = 3 µM); selective for ANO1 over CFTR and ENaCs in FRT cells at 10 µM; increases the rate of submucosal gland fluid secretion in human bronchi isolated from patients with cystic fibrosis and healthy individuals at 20 µM; increases production of mitochondrial ROS

Eact – 25 mg

Brand:
Cayman
CAS:
461000-66-8
Storage:
-20
UN-No:
Non-Hazardous - /

Eact is an activator of the calcium-activated chloride channel anoctamin 1 (ANO1).{48862} It increases chloride currents in FRT cells expressing human ANO1 (EC50 = 3 µM). It is selective for ANO1 over cystic fibrosis transmembrane conductance regulator (CFTR) chloride channels and epithelial sodium channels (ENaCs) in FRT cells at 10 µM. Eact (20 µM) increases the rate of submucosal gland fluid secretion in human bronchi isolated from patients with cystic fibrosis and healthy individuals. It increases production of mitochondrial reactive oxygen species (ROS), reduces the mitochondrial membrane potential, and induces apoptosis in rat lung microvascular endothelial cells (RLMVECs), as well as reduces total cell counts in pulmonary artery endothelial cell populations isolated from patients with idiopathic pulmonary arterial hypertension (IPAH).{48863} Eact also activates transient receptor potential vanilloid 1 (TRPV1) in HEK293T cells expressing the mouse receptor (EC50 = 11.6 µM) and induces scratching and licking behaviors in wild-type, but not Trpv1-/-, mice.{48864}  

 

Available on backorder

Add to quotes
SKU: 29791 - 25 mg Category:

Description

An ANO1 channel activator; increases chloride currents in FRT cells expressing human ANO1 (EC50 = 3 µM); selective for ANO1 over CFTR and ENaCs in FRT cells at 10 µM; increases the rate of submucosal gland fluid secretion in human bronchi isolated from patients with cystic fibrosis and healthy individuals at 20 µM; increases production of mitochondrial ROS, reduces the mitochondrial membrane potential, and induces apoptosis in RLMVECs; reduces total cell counts in pulmonary artery endothelial cell populations isolated from patients with IPAH; activates TRPV1 in HEK293T cells expressing the mouse receptor (EC50 = 11.6 µM); induces scratching and licking behaviors in wild-type, but not Trpv1-/-, mice

Formal name: 3,4,5-trimethoxy-N-(2-methoxyethyl)-N-(4-phenyl-2-thiazolyl)-benzamide

Synonyms: 

Molecular weight: 428.5

CAS: 461000-66-8

Purity: ≥98%

Formulation: A crystalline solid

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 – 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) – 25 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 - 25 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • 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 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
    Add to quotes
    View product page