ICRT-14

Cas：677331-12-3

Product Information：

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).

Chemical Formula: C21H17N3O2S

Exact Mass: 375.1041

Molecular Weight: 375.446

Elemental Analysis: C, 67.18; H, 4.56; N, 11.19; O, 8.52; S, 8.54

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

InChi Key: 

NCSHZXNGQYSKLR-XDHOZWIPSA-N

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+

Smiles Code:

O=C(N(C1=CC=CC=C1)C/2=O)SC2=C\C3=C(C)N(C4=CC=CN=C4)C(C)=C3

Technical Data：

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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.