SZL P1-41Selective Skp2 inhibitor; suppresses E3 ligase activity CAS# 222716-34-9 |
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| Cas No. | 222716-34-9 | SDF | Download SDF |
| PubChem ID | 1286902 | Appearance | Powder |
| Formula | C24H24N2O3S | M.Wt | 420.52 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 4.3 mg/mL (10.23 mM; Need ultrasonic and warming) | ||
| Chemical Name | 3-(1,3-benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)chromen-4-one | ||
| SMILES | CCC1=C(C(=C2C(=C1)C(=O)C(=CO2)C3=NC4=CC=CC=C4S3)CN5CCCCC5)O | ||
| Standard InChIKey | JKIXLEKBXHMXTN-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H24N2O3S/c1-2-15-12-16-22(28)18(24-25-19-8-4-5-9-20(19)30-24)14-29-23(16)17(21(15)27)13-26-10-6-3-7-11-26/h4-5,8-9,12,14,27H,2-3,6-7,10-11,13H2,1H3 | ||
| 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 | Skp2 inhibitor; thought to prevent assembly of Skp2-Skp1 complexes. Selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the activity of other SCF complexes. Also inhibits Skp2-mediated p27 and Akt ubiquitination in vivo and in vitro. Suppresses the survival of cancer cells and cancer stem cells by triggering cell senescence and inhibiting glycolysis. Exhibits antitumor effects in multiple animal models and cancer cell lines. |
SZL P1-41 Dilution Calculator
SZL P1-41 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.378 mL | 11.89 mL | 23.7801 mL | 47.5602 mL | 59.4502 mL |
| 5 mM | 0.4756 mL | 2.378 mL | 4.756 mL | 9.512 mL | 11.89 mL |
| 10 mM | 0.2378 mL | 1.189 mL | 2.378 mL | 4.756 mL | 5.945 mL |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 0.9512 mL | 1.189 mL |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.4756 mL | 0.5945 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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SZL P1-41 is Skp2 inhibitor, selectively suppresses Skp2 E3 ligase activity, but not activity of other SCF complexes. target: Skp2 In vitro: SZL P1-41 also phenocopies the effects observed upon genetic Skp2 deficiency, such as suppressing survival, Akt-mediated glycolysis as well as triggering p53-independent cellular senescence. SZL P1-41 prevent Skp2-Skp1 interactions and Skp2 SCF E3 ligase activity. The reference concentration is 5 uM. SZL P1-41 restricts cancer cell survival through triggering p53-independent cellular senescence and inhibiting aerobic glycolysis. In vivo: SZL P1-41 exhibits potent anti-tumor activities in multiple animal models and cooperates with chemotherapeutic agents to reduce cancer cell survival.
References:
[1]. Chan CH et al. Pharmacological inactivation of Skp2 SCF ubiquitin ligase restricts cancer stem cell traits and cancer progression. Cell. 2013 Aug 1;154(3):556-68.
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Pharmacological inactivation of Skp2 SCF ubiquitin ligase restricts cancer stem cell traits and cancer progression.[Pubmed:23911321]
Cell. 2013 Aug 1;154(3):556-68.
Skp2 E3 ligase is overexpressed in numerous human cancers and plays a critical role in cell-cycle progression, senescence, metabolism, cancer progression, and metastasis. In the present study, we identified a specific Skp2 inhibitor using high-throughput in silico screening of large and diverse chemical libraries. This Skp2 inhibitor selectively suppresses Skp2 E3 ligase activity, but not activity of other SCF complexes. It also phenocopies the effects observed upon genetic Skp2 deficiency, such as suppressing survival and Akt-mediated glycolysis and triggering p53-independent cellular senescence. Strikingly, we discovered a critical function of Skp2 in positively regulating cancer stem cell populations and self-renewal ability through genetic and pharmacological approaches. Notably, Skp2 inhibitor exhibits potent antitumor activities in multiple animal models and cooperates with chemotherapeutic agents to reduce cancer cell survival. Our study thus provides pharmacological evidence that Skp2 is a promising target for restricting cancer stem cell and cancer progression.
