A p53 reactivator; selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM

NSC 319726 – 5 mg

Brand:
Cayman
CAS:
71555-25-4
Storage:
-20
UN-No:
Non-Hazardous - /

NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}  

 

Available on backorder

Add to quotes
SKU: 23701 - 5 mg Category:

Description

A p53 reactivator; selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively); induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM; restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells; inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model when administered at a dose of 1 mg/kg; has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells

Formal name: 2-[1-(2-pyridinyl)ethylidene]hydrazide, 1-azetidinecarbothioic acid

Synonyms: 

Molecular weight: 234.3

CAS: 71555-25-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antifungals||Product Type|Biochemicals|Small Molecule Activators||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53||Research Area|Immunology & Inflammation

Related products

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

    (R)-Roscovitine – 10 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 - 10 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) – 100 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 - 100 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 – 500 µg

    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 - 500 µg

    Available on backorder

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

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 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 - 10 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page