iCRT 14CRT inhibitor CAS# 677331-12-3 |
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Quality Control & MSDS
3D structure
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| Cas No. | 677331-12-3 | SDF | Download SDF |
| PubChem ID | 5967294 | Appearance | Powder |
| Formula | C21H17N3O2S | M.Wt | 375.44 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 29 mg/mL (77.24 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (5Z)-5-[(2,5-dimethyl-1-pyridin-3-ylpyrrol-3-yl)methylidene]-3-phenyl-1,3-thiazolidine-2,4-dione | ||
| SMILES | CC1=CC(=C(N1C2=CN=CC=C2)C)C=C3C(=O)N(C(=O)S3)C4=CC=CC=C4 | ||
| Standard InChIKey | NCSHZXNGQYSKLR-UNOMPAQXSA-N | ||
| Standard 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- | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent inhibitor of β-catenin-responsive transcription (CRT) (IC50 = 40.3 nM in assays of Wnt pathway activity). Thought to directly influence the interaction between β-catenin and TCF4. Induces marked G0/G1 cell cycle arrest in HCT-116 and HT29 cell lines. |
iCRT 14 Dilution Calculator
iCRT 14 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6635 mL | 13.3177 mL | 26.6354 mL | 53.2708 mL | 66.5885 mL |
| 5 mM | 0.5327 mL | 2.6635 mL | 5.3271 mL | 10.6542 mL | 13.3177 mL |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6635 mL | 5.3271 mL | 6.6589 mL |
| 50 mM | 0.0533 mL | 0.2664 mL | 0.5327 mL | 1.0654 mL | 1.3318 mL |
| 100 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.5327 mL | 0.6659 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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iCRT 14 is a potent and specific inhibitor of β-catenin responsive transcription (CRT) with IC50 value of 40.3 nM [1].
iCRT 14 belongs to the thiazolidinedione class and is screened out by the dTF12-luciferase reporter assay. It inhibits the direct interaction between β-catenin and TCF4 and does not affect the interaction of β-catenin with other cognate protein partners. iCRT 14 also inhibits the mammalian Wnt responsive STF16 luciferase reporter in HEK293 cells with IC50 value of 40.3 nM. Besides that, iCRT 14 is specific against CRT over other conserved cell signaling pathways. It had no effect on the phosphorylation of Dvl induced by Wnt [1].
iCRT 14 can also interfere with TCF binding to DNA. Moreover, the inhibition of CRT resulted in the modulation of CRT-induced molecular and morphological changes including cell transformation phenotype and cell invasion. Furthermore, the treatment of HCT116 and HT29 cells with iCRT 14 exhibited cell cycle arrest in the G0/G1 phase. In the xenograft models of HCT116 and HT29, administration of iCRT 14 at dose of 50 mg/kg caused significant decrease in CycD1 and the subsequent suppression of tumor growth [1].
References:
[1] Gonsalves F C, Klein K, Carson B B, et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proceedings of the National Academy of Sciences, 2011, 108(15): 5954-5963.
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