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| Targets |
NSC-689857 targets the Skp2-Cks1 protein-protein interaction and p27Kip1 ubiquitination. Skp2 (S-phase kinase-associated protein 2) is a substrate recognition component of the SCF (Skp1-Cul1-F-box protein) ubiquitin ligase complex. Cks1 is an adaptor protein that facilitates the binding of Skp2 to p27Kip1, a cyclin-dependent kinase inhibitor. NSC-689857 inhibits the Skp2-Cks1 interaction (IC50 = 36 μM), preventing the ubiquitination and degradation of p27Kip1. It also inhibits p27 phosphorylation (IC50 = 30 μM).
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| ln Vitro |
NSC-689857 is an inhibitor of the Skp2-Cks1 protein-protein interaction and p27Kip1 ubiquitination. It has an IC50 of 36 μM for Skp2-Cks1 and inhibits p27 phosphorylation with an IC50 of 30 μM. NSC-689857 has varying activities in different cancer types, with higher activity against leukemia cell lines than other cancer/tumor cells. These in vitro studies confirm NSC-689857's activity as an inhibitor of the Skp2-Cks1 interaction.
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| ln Vivo |
In vivo activity data for NSC-689857 is limited, as the compound is primarily used as a research tool in in vitro studies. However, its mechanism of action—inhibiting Skp2-Cks1 interaction and preventing p27 degradation—suggests potential in vivo applications in cancer research. The compound could be used in animal models to study the effects of Skp2 inhibition on tumor growth. However, specific in vivo protocols and results are not detailed.
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| Enzyme Assay |
In vitro assays for NSC-689857 measure its inhibition of the Skp2-Cks1 protein-protein interaction. These assays typically use purified proteins or cell lysates and techniques such as fluorescence polarization, AlphaScreen, or co-immunoprecipitation. NSC-689857 is added at increasing concentrations, and the inhibition of the interaction is measured. The IC50 for Skp2-Cks1 is 36 μM. p27 ubiquitination assays can be performed using in vitro ubiquitination systems.
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| Cell Assay |
In vitro cell-based assays for NSC-689857 are used to study its effects on p27Kip1 levels and cell cycle regulation. Cancer cells are treated with NSC-689857, and the levels of p27Kip1 protein are measured by Western blotting. Cell cycle analysis is performed by flow cytometry. Cell proliferation is assessed using assays such as MTT or CellTiter-Glo. These assays confirm the compound's activity as an inhibitor of Skp2-mediated p27 degradation.
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| Animal Protocol |
In vivo animal experiments for NSC-689857 are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a Skp2 inhibitor would involve its administration to animal models of cancer. However, specific protocols for NSC-689857 are not detailed.
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| ADME/Pharmacokinetics |
NSC-689857 has a molecular weight not specified in standard product descriptions. It is a solid compound. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for NSC-689857 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. NSC-689857 is an inhibitor of Skp2-Cks1 and EGFR, and its toxicity would be related to its effects on these targets in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
NSC-689857 is a research compound and is not approved for any clinical or therapeutic use. It is a potent inhibitor of the Skp2-Cks1 protein-protein interaction and p27Kip1 ubiquitination in vitro. NSC-689857 inhibits the Skp2-Cks1 interaction with an IC50 of 36 μM and inhibits p27 phosphorylation with an IC50 of 30 μM. It has higher activity against leukemia cell lines. NSC-689857 is a research tool for studying the ubiquitin-proteasome pathway and cell cycle regulation.
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| Molecular Formula |
C25H29NO4
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| Molecular Weight |
407.502067327499
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| Exact Mass |
407.209
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| CAS # |
241127-79-7
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| PubChem CID |
391131
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| Appearance |
White to off-white solid powder
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| LogP |
5.4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
573
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C(C1C=CC(=CC=1)NCC1C=C(C=CC=1O)O)=O)CC12CC3CC(CC(C3)C1)C2
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| InChi Key |
MXKHJVTZHIIIMQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H29NO4/c27-22-5-6-23(28)20(10-22)14-26-21-3-1-19(2-4-21)24(29)30-15-25-11-16-7-17(12-25)9-18(8-16)13-25/h1-6,10,16-18,26-28H,7-9,11-15H2
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| Chemical Name |
1-adamantylmethyl 4-[(2,5-dihydroxyphenyl)methylamino]benzoate
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| Synonyms |
NSC-689857 NSC689857 NSC 689857
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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 |
| 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 : ~100 mg/mL (~245.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.13 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4540 mL | 12.2699 mL | 24.5399 mL | |
| 5 mM | 0.4908 mL | 2.4540 mL | 4.9080 mL | |
| 10 mM | 0.2454 mL | 1.2270 mL | 2.4540 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.
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