An inhibitor of β-catenin-responsive transcription
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iCRT14

Item No. 22132

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[2,5-dimethyl-1-(3-pyridinyl)-1H-pyrrol-3-yl]methylene]-3-phenyl-2,4-thiazolidinedione
CAS Number
677331-12-3
Molecular Formula
C21H17N3O2S
Formula Weight
375.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
371 nm
SMILES
O=C(S/C1=C\C2=C(C)N(C3=CN=CC=C3)C(C)=C2)N(C4=CC=CC=C4)C1=O
InChi Code
InChI=1S/C21H17N3O2S/c1-14-11-16(15(2)23(14)18-9-6-10-22-13-18)12-19-20(25)24(21(26)27-19)17-7-4-3-5-8-17/h3-13H,1-2H3/b19-12-
InChi Key
NCSHZXNGQYSKLR-UNOMPAQXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $107

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    10 mg

    $203

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    25 mg

    $477

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    50 mg

    $794

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    Cayman Chemical
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    Product Description

    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).1 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).2 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.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gonsalves, F.C., Klein, K.O., Carson, B.B., et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proc. Natl. Acad. Sci. USA 108(15), 5954-5963 (2011).

    2. Huang, Z., Zhang, M., Burton, S.D., et al. Targeting the Tcf4 G13ANDE17 binding site to selectively disrupt β-catenin/T-cell factor protein-protein interactions. ACS Chem Biol. 9(1), 193-201 (2014).

    3. Dandekar, S., Romanos-Sirakis, E., Pais, F., et al. Wnt inhibition leads to improved chemosensitivity in paediatric acute lymphoblastic leukemia. Br. J. Haematol. 167(1), 87-99 (2014).

    4. Zhang, J.L., Liu, Y., Yang, H., et al. ATP-P2Y2-β-catenin axis promotes cell invasion in breast cancer cells. Cancer Sci. 108(7), 1318-1327 (2017).