A structural analog of NAADP that blocks NAADP-dependent calcium release (IC50 = 6 nM) as well as NAADP binding to sea urchin egg homogenate (IC50 = 0.4 nM); does not affect either IP3-mediated calcium release or cyclic ADP-ribose-mediated calcium release

trans-Ned-19 – 5 mg

Brand:
Cayman
CAS:
1354235-96-3
Storage:
-20
UN-No:
Non-Hazardous - /

Nicotinic acid adenine dinucleotide phosphate (NAADP) is a dinucleotide second messenger that triggers the release of calcium from lysosomes and related cellular compartments.{28523} trans-Ned-19 is a structural analog of NAADP that blocks NAADP-dependent calcium release (IC50 = 6 nM) as well as NAADP binding to sea urchin egg homogenate (IC50 = 0.4 nM).{28527} The trans form of Ned-19 is significantly more potent than the cis isomer in both assays.{28527} Ned-19 does not affect either IP3-mediated calcium release or cyclic ADP-ribose-mediated calcium release.{28527} It directly binds NAADP receptors on lysosomes in mouse pancreatic beta cells and competitively antagonizes activation by NAADP.{28527,28526} It inhibits glucose-induced calcium oscillations in pancreatic islets and insulin-induced calcium increases in 3T3-L1 adipocytes.{28527,28525} Ned-19 also blocks calcium signaling induced by endothelin-1 or norepinephrine in renal afferent arterioles.{28424} Ned-19 dose-dependently reduces infection of host cells by Ebola virus.{28524}  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A structural analog of NAADP that blocks NAADP-dependent calcium release (IC50 = 6 nM) as well as NAADP binding to sea urchin egg homogenate (IC50 = 0.4 nM); does not affect either IP3-mediated calcium release or cyclic ADP-ribose-mediated calcium release

Formal name: (1R,3S)-1-[3-[[4-(2-fluorophenyl)-1-piperazinyl]methyl]-4-methoxyphenyl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic acid

Synonyms: 

Molecular weight: 514.6

CAS: 1354235-96-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cell Biology|Cell Signaling|Calcium Mobilization||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Viral Diseases|Ebola

Related products

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

    Anhydrotetracycline (hydrochloride) – 250 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 - 250 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page