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Purity: ≥98%
Skp2 inhibitor C1 (also known as SKPin C1) is a specific and selective small-molecule inhibitor of Skp2-mediated p27 degradation, it selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts. Skp2 Inhibitor C1 induces cell cycle arrest. 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).
| ln Vitro |
Skp2 Inhibitor C1 (10–50 μM; 12 hours) reduces THP-1, U266, and RPMI 8226 cell viability.[1].
By blocking ubiquitination, Skp2 Inhibitor C1 (25 μM) raises the levels of p27 protein in U266 and RPMI 8226 cells[1].
Skp2 Inhibitor C1 (25 μM) inhibits U266 and RPMI 8226 cells' cell cycle.[1].
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| ln Vivo |
By using the tail suspension test (TST), forced swimming test (FST), and social interaction test (SIT), Skp2 Inhibitor C1 (5 mg/kg and 10 mg/kg; three times within 24 h: 24, 5, and 1 h before the test) shows the antidepressant-like effect in mouse models following chronic treatment.[2]
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| Cell Assay |
Cell Line:THP-1, U266, RPMI 8226, and B lymphocytes
Concentration: 0, 5, 10, 25, and 50 μM Incubation Time: 12 hr, 24 hr, 36 hr, and 48 hr Result: significantly reduced U266 and RPMI 8226 cell viability at 10 μM for a 12-hour period. had no discernible effect on the viability of B cells at 50 μM. THP-1 cell viability was reduced for 12 hours at 50 μM. |
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| References |
| Molecular Formula |
C18H13BRN2O4S2
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| Molecular Weight |
465.34
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| Exact Mass |
463.95
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| Elemental Analysis |
C, 46.46; H, 2.82; Br, 17.17; N, 6.02; O, 13.75; S, 13.78
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| CAS # |
432001-69-9
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
O=C(O)COC1=CC=C(Br)C=C1/C=C(SC(N2CC3=CC=CN=C3)=S)/C2=O
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| InChi Key |
O=C(O)COC1=CC=C(Br)C=C1/C=C(SC(N2CC3=CC=CN=C3)=S)/C2=O
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| InChi Code |
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-
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| Chemical Name |
2-[4-Bromo-2-[[4-oxo-3-(3-pyridinylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]phenoxy]acetic acid
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| Synonyms |
MDK-1699; MDK 1699; MDK1699; Skp2 inhibitor C1 and SKPin C1.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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 :20.83~ 93 mg/mL ( 44.76~199.85 mM )
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 5% DMSO + Corn oil: 1.2mg/ml (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1490 mL | 10.7448 mL | 21.4897 mL | |
| 5 mM | 0.4298 mL | 2.1490 mL | 4.2979 mL | |
| 10 mM | 0.2149 mL | 1.0745 mL | 2.1490 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.
 In silicoandin vitroscreens for Skp2 ligase inhibitors.Chem Biol. 2012 Dec 21; 19(12): 1515–1524. |
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 Structure-function approach to identify key contacts.Chem Biol. 2012 Dec 21; 19(12): 1515–1524. |
 Binding of inhibitors disrupts the Skp2-p27 interaction.Chem Biol. 2012 Dec 21; 19(12): 1515–1524. |
 Inhibitors induces p27 protein in melanoma cells.Chem Biol. 2012 Dec 21; 19(12): 1515–1524. |
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 Skp2 ligase inhibitors induce cell cycle changes.Chem Biol. 2012 Dec 21; 19(12): 1515–1524. |
 Skp2E3LIs increase nuclear p27 in the ECA cell line, ECC-1.Endocrinology.2013 Nov;154(11):4030-45. |
 Skp2E3LI, C2, increases nuclear p27 in ECC-1 cells determined by super resolution fluorescent microscopy and quantitation.Endocrinology.2013 Nov;154(11):4030-45. |
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 The Skp2E3LIs, C5, C2, and C20, inhibit cell proliferation, block cells in G1, are not cytotoxic, and do not induce apoptosis in ECC-1 cells.Endocrinology.2013 Nov;154(11):4030-45. |
 The Skp2E3LI, C2 increases nuclear p27 while decreasing p27 in the cytoplasm over time; C2 and C20 increase p27 half-life over controls in ECC-1 cells.Endocrinology.2013 Nov;154(11):4030-45. |
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