ICRT-14

iCRT-14 is a potent inhibitor of β-catenin-responsive transcription (CRT) that inhibits Wnt signaling in a reporter assay in vitro (IC50 = 40.3 nM). 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).

Product information

CAS Number: 677331-12-3

Molecular Weight: 375.44

Formula: C21H17N3O2S

Synonym:

iCRT14

iCRT-14

iCRT 14

Wnt inhibitor

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

Smiles: CC1=C(C=C2SC(=O)N(C3C=CC=CC=3)C2=O)C=C(C)N1C1=CN=CC=C1

InChiKey: NCSHZXNGQYSKLR-UNOMPAQXSA-N

InChi: 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-

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

iCRT14 can interfere with TCF binding to DNA in addition to its ability to influence TCF-β-cat interaction. iCRT14 (10, 25, 50 μM) effectively inhibits cell proliferation in BT-549 cells in a dose- and time-dependent manner, but still less potent than iCRT3.

In Vivo:

iCRT14 (50 mg/kg, i.p.) markedly decreases CycD1, proliferation of the tumors in HCT116 xenografts.

References:

1. More S, Yang X, Zhu Z, Bamunuarachchi G, Guo Y, Huang C, Bailey K, Metcalf JP, Liu L. Regulation of influenza virus replication by Wnt/β-catenin signaling. PLoS One. 2018 Jan 11;13(1):e0191010. doi: 10.1371/journal.pone.0191010. eCollection 2018. PubMed PMID: 29324866; PubMed Central PMCID: PMC5764324.
2. Gufler S, Artes B, Bielen H, Krainer I, Eder MK, Falschlunger J, Bollmann A, Ostermann T, Valovka T, Hartl M, Bister K, Technau U, Hobmayer B. β-Catenin acts in a position-independent regeneration response in the simple eumetazoan Hydra. Dev Biol. 2018 Jan 15;433(2):310-323. doi: 10.1016/j.ydbio.2017.09.005. Epub 2017 Nov 3. PubMed PMID: 29108673.
3. Zhang JL, Liu Y, Yang H, Zhang HQ, Tian XX, Fang WG. ATP-P2Y2-β-catenin axis promotes cell invasion in breast cancer cells. Cancer Sci. 2017 Jul;108(7):1318-1327. doi: 10.1111/cas.13273. Epub 2017 Jun 6. PubMed PMID: 28474758; PubMed Central PMCID: PMC5497932.
4. Zhu L, Thunuguntla P, Liu Y, Hancock M, Jones C. The β-catenin signaling pathway stimulates bovine herpesvirus 1 productive infection. Virology. 2017 Jan;500:91-95. doi: 10.1016/j.virol.2016.10.014. Epub 2016 Oct 24. PubMed PMID: 27788397.
5. Mathur R, Sehgal L, Braun FK, Berkova Z, Romaguerra J, Wang M, Rodriguez MA, Fayad L, Neelapu SS, Samaniego F. Targeting Wnt pathway in mantle cell lymphoma-initiating cells. J Hematol Oncol. 2015 Jun 6;8:63. doi: 10.1186/s13045-015-0161-1. PubMed PMID: 26048374; PubMed Central PMCID: PMC4460883.

Products are for research use only. Not for human use.