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

iCRT14 – 5 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}  

 

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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

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