Skp2 Inhibitor C1Inhibits Skp2-mediated p27 degradation; induces cell cycle arrest CAS# 432001-69-9 |
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| Cas No. | 432001-69-9 | SDF | Download SDF |
| PubChem ID | 5733396 | Appearance | Powder |
| Formula | C18H13BrN2O4S2 | M.Wt | 465.34 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | SKPin C1 | ||
| Solubility | DMSO : 6.4 mg/mL (13.75 mM; Need ultrasonic) | ||
| Chemical Name | 2-[4-bromo-2-[(Z)-[4-oxo-3-(pyridin-3-ylmethyl)-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl]phenoxy]acetic acid | ||
| SMILES | C1=CC(=CN=C1)CN2C(=O)C(=CC3=C(C=CC(=C3)Br)OCC(=O)O)SC2=S | ||
| Standard InChIKey | IYCJJVVXEHZJHE-CHHVJCJISA-N | ||
| Standard InChI | InChI=1S/C18H13BrN2O4S2/c19-13-3-4-14(25-10-16(22)23)12(6-13)7-15-17(24)21(18(26)27-15)9-11-2-1-5-20-8-11/h1-8H,9-10H2,(H,22,23)/b15-7- | ||
| 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 | Inhibitor of Skp2-mediated p27 degradation. Induces p27 accumulation in metastatic melanoma cell lines. Promotes G1/S cell cycle arrest in T47D cells and LNCaP cells; induces G2/M cell cycle arrest in MCF-7 cells. |
Skp2 Inhibitor C1 Dilution Calculator
Skp2 Inhibitor C1 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.149 mL | 10.7448 mL | 21.4897 mL | 42.9793 mL | 53.7242 mL |
| 5 mM | 0.4298 mL | 2.149 mL | 4.2979 mL | 8.5959 mL | 10.7448 mL |
| 10 mM | 0.2149 mL | 1.0745 mL | 2.149 mL | 4.2979 mL | 5.3724 mL |
| 50 mM | 0.043 mL | 0.2149 mL | 0.4298 mL | 0.8596 mL | 1.0745 mL |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2149 mL | 0.4298 mL | 0.5372 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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Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts. IC50 value: Target: Skp2 inhibitor; p27 regulator in vitro: T47D cells treated with C1 (5 μM for 16 hours) displayed an increase in G1 phase (p < 0.0001) and a decrease in S phase (p < 0.0001), correlating with p27 protein induction. In contrast, MCF-7 cells responded to C1 with a significant reduction in G1 phase (35%, p < 0.0001) and an increase in G2-M phase (43%, p < 0.0001). This G1 reduction and G2/M arrest is dose dependent on C1 (Figure 5C right; p < 0.001 and p < 0.01, respectively) and correlates with increased p27 protein levels (Figure 5E left, S4A top right) [1].
References:
[1]. Wu L, et al. Specific small molecule inhibitors of Skp2-mediated p27 degradation. Chem Biol. 2012 Dec 21;19(12):1515-24.
[2]. Pavlides SC, et al. Inhibitors of SCF-Skp2/Cks1 E3 ligase block estrogen-induced growth stimulation and degradation of nuclear p27kip1: therapeutic potential for endometrial cancer. Endocrinology. 2013 Nov;154(11):4030-45.
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Skipping cancer: small molecule inhibitors of SKP2-mediated p27 degradation.[Pubmed:23261592]
Chem Biol. 2012 Dec 21;19(12):1497-8.
The cullin-RING ubiquitin ligase, CRL1(SKP2), directing the degradation of the tumor suppressor p27, is a well validated drug target in a wide variety of human cancers. In this issue of Chemistry & Biology, Wu and colleagues describe first-in-class small molecule inhibitors of CRL1(SKP2)-mediated degradation of p27.
Specific small molecule inhibitors of Skp2-mediated p27 degradation.[Pubmed:23261596]
Chem Biol. 2012 Dec 21;19(12):1515-24.
In the ubiquitin proteasome system, the E3 ligase SCF-Skp2 and its accessory protein, Cks1, promote proliferation largely by inducing the degradation of the CDK inhibitor p27. Overexpression of Skp2 in human cancers correlates with poor prognosis, and deregulation of SCF-Skp2-Cks1 promotes tumorigenesis in animal models. We identified small molecule inhibitors specific to SCF-Skp2 activity using in silico screens targeted to the binding interface for p27. These compounds selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts. In cancer cells, the compounds induced p27 accumulation in a Skp2-dependent manner and promoted cell-type-specific blocks in the G1 or G2/M phases. Designing SCF-Skp2-specific inhibitors may be a novel strategy to treat cancers dependent on the Skp2-p27 axis.
