A cardiotonic steroid with diverse biological activities; inhibits human kidney Na+/K+-ATPase (IC50 = 44.2 nM); increases contraction force in isolated frog ventricle strips by 30.2% at 9.9 μg/ml; cytotoxic to HL-60

Telocinobufagin – 10 mg

Brand:
Cayman
CAS:
472-26-4
Storage:
-20
UN-No:
Non-Hazardous - /

Telocinobufagin is a cardiotonic steroid that has been found in skin secretions of the toad B. rubescens and has diverse biological activities.{29914,46344,46345,46346} It inhibits human kidney Na+/K+-ATPase with an IC50 value of 44.2 nM.{46345} Telocinobufagin (9.9 μg/ml) increases contraction force in isolated frog ventricle strips by 30.2%.{46344} It is cytotoxic to HL-60, HCT8, SF295, MDA-MB-435 cancer cells and human peripheral blood lymphocytes (IC50s = 0.06, 0.06, 0.03, 0.11, and 0.05 μM, respectively).{46346} Telocinobufagin is also active against E. coli and S. aureus (MICs = 64 and 128 μg/ml, respectively).{46344}  

 

Available on backorder

Add to quotes
SKU: 27981 - 10 mg Category:

Description

A cardiotonic steroid with diverse biological activities; inhibits human kidney Na+/K+-ATPase (IC50 = 44.2 nM); increases contraction force in isolated frog ventricle strips by 30.2% at 9.9 μg/ml; cytotoxic to HL-60, HCT8, SF295, MDA-MB-435 cancer cells, and human peripheral blood lymphocytes (IC50s = 0.06, 0.06, 0.03, 0.11, and 0.05 μM, respectively); active against E. coli and S. aureus (MICs = 64 and 128 μg/ml, respectively)

Formal name: 3β,5β,14-trihydroxy-bufa-20,22-dienolide

Synonyms:  NSC 119989|NSC 90782|Telobufotoxin|Telocinobufogenin

Molecular weight: 402.5

CAS: 472-26-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antibiotics||Product Type|Biochemicals|Lipids|Sterol Lipids||Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Small Molecule Inhibitors|ATPases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Cell Death||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Bacterial Diseases

Related products

  • 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 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
  • 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
  • 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