An inhibitor of CRT (IC50 = 40.3 nM); inhibits β-catenin/Tcf4 binding (Kis = 53.51 μM); inhibits Notch

iCRT14 – 25 mg

Brand:
Cayman
CAS:
677331-12-3
Storage:
-20
UN-No:
Non-Hazardous - /

iCRT14 is a potent inhibitor of β-catenin-responsive transcription (CRT) that inhibits Wnt signaling in a reporter assay in vitro (IC50 = 40.3 nM).{39368} It inhibits the interaction between β-catenin and T cell factor 4 (Tcf4) in quantitative reporter assays of β-catenin/Tcf4 binding (Ki = 53.51 μM).{39369} It inhibits Notch, hedgehog (Hh), and JAK/STAT signaling in reporter assays with IC50 values of 69.2, 194, and 70 nM, respectively. iCRT14 (50 mg/kg, i.p.) reduces the number of proliferating cells and leads to a decrease of approximately 50% in the initial tumor growth rate in mouse xenograft models of colon carcinoma. iCRT14 also inhibits proliferation of leukemia cell lines and suppresses ATP-driven migration of the MCF-7 and MDA-MB-231 breast cancer cell lines.{39370,39371}  

 

Out of stock

Add to quotes
SKU: 22132 - Category:

Description

An inhibitor of CRT (IC50 = 40.3 nM); inhibits β-catenin/Tcf4 binding (Kis = 53.51 μM); inhibits Notch, Hh, and JAK/STAT signaling (IC50s = 69.2, 194, and 70 nM, respectively); reduces proliferation and initial tumor growth rate in mouse xenografts of colon carcinoma (50 mg/kg i.p.); inhibits proliferation of leukemia cell lines; suppresses ATP-driven migration of the MCF-7 and MDA-MB-231 breast cancer cell lines

Formal name: 5-[[2,5-dimethyl-1-(3-pyridinyl)-1H-pyrrol-3-yl]methylene]-3-phenyl-2,4-thiazolidinedione

Synonyms: 

Molecular weight: 375.4

CAS: 677331-12-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Hedgehog Signaling||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Cell Signaling|Notch Signaling||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cancer|Transcription Factors|STATs||Research Area|Cell Biology|Cell Signaling|Hedgehog Signaling||Research Area|Cell Biology|Cell Signaling|Notch Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

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
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 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 - 25 mg

    Available on backorder

    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
    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
    View product page