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Purity: ≥98%
iCRT 14 is a novel and potent inhibitor of β-catenin-responsive transcription (CRT) with IC50 of 40.3 nM against Wnt responsive STF16 luciferase in a homogeneous fluorescence polarization (FP) assay. Immunofluorescence staining of β-catenin in TNBC cell lines showed both nuclear and cytoplasmic localization, indicating activation of Wnt pathway in TNBC cells. iCRT-14 was an effective compound for inhibiting proliferation and antagonizing Wnt signaling in TNBC cells. In addition, treatment with iCRT-14 resulted in increased apoptosis in vitro. Knockdown of the Wnt pathway transcription factor, SOX4 in triple negative BT-549 cells resulted in decreased cell proliferation and migration, and combination treatment of iCRT-3 with SOX4 knockdown had a synergistic effect on inhibition of cell proliferation and induction of apoptosis.
| ln Vitro |
Apart from its impact on the TCF-β-cat response, iCRT 14 has the ability to obstruct TCF's DNA binding [1]. Although it was still less than iCRT 3, iCRT 14 (10, 25, 50 μM) efficiently and time- and dose-dependently reduced the growth of BT-549 cells [2].
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| ln Vivo |
In HCT116 xenografts, iCRT 14 (50 mg/kg, i.p.) dramatically decreases CycD1, tumor swelling [1].
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| References |
[1]. Gonsalves FC, et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proc Natl Acad Sci USA. 2011 Apr 12;108(15):5954-63.
[2]. Bilir B, et al. Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells. J Transl Med. 2013 Nov 4;11:280 |
| Molecular Formula |
C21H17N3O2S
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|---|---|
| Molecular Weight |
375.44358
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| CAS # |
677331-12-3
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| Related CAS # |
901751-47-1(iCRT3); 18623-44-4 (iCRT5)
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| SMILES |
O=C(N(C1=CC=CC=C1)C/2=O)SC2=C\C3=C(C)N(C4=CC=CN=C4)C(C)=C3
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| InChi Key |
NCSHZXNGQYSKLR-XDHOZWIPSA-N
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| 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+
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| Chemical Name |
5-[[2,5-dimethyl-1-(3-pyridinyl)-1H-pyrrol-3-yl]methylene]-3-phenyl-2,4-thiazolidinedione
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| Synonyms |
iCRT14; iCRT-14; iCRT 14
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 29 mg/mL (~77.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6635 mL | 13.3177 mL | 26.6354 mL | |
| 5 mM | 0.5327 mL | 2.6635 mL | 5.3271 mL | |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6635 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 iCRT-14 effectively inhibits cell proliferation in BT-549 cells in a dose- and time-dependent manner.J Transl Med.2013 Nov 4;11:280. |
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 (A) Primary screen. dsRNA-mediated knockdown of Axin results in cytoplasmic stabilization of β-cat, which, on translocation to the nucleus, results in activation of the β-cat responsive dTF12 reporter.Proc Natl Acad Sci U S A.2011 Apr 12;108(15):5954-63. |
 (A) Effect of candidate compounds on the interaction of purified β-cat-His and GST-TCF4. iCRT3, -5, and -14 show a significant inhibitory effect on these interactions compared with nontreated (NT) and DMSO-treated binding reactions.Bottomshows comparable amounts of GST-TCF4 being pulled down.Proc Natl Acad Sci U S A.2011 Apr 12;108(15):5954-63 |
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