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| 1mg |
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| 5mg |
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| Targets |
SJ572403 targets p27Kip1, a cyclin-dependent kinase inhibitor. p27Kip1 is an intrinsically disordered protein that plays a critical role in regulating cell cycle progression by binding to and inhibiting CDK complexes. The compound specifically binds to the D2 subdomain of the p27-KID (kinase inhibitory domain). By binding to p27Kip1, the compound modulates its function, which can affect CDK activity and cell proliferation. It is a tool for studying intrinsically disordered proteins and their role in cell cycle control.
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| ln Vitro |
SJ572403 (SJ403) (3 mM) exhibits a Kd value of 2.2 mM[1], indicating a specific interaction with a particular region within the D2 subdomain of p27-KID. The Cdk regulation of p27 is modulated by SJ572403 (0-3 mM) [1]. SJ572403 (10 μM-3 mM) partially recovers Cdk2 kinase activity by substituting p27-D2 in Cdk2/cyclin A [1].
In vitro, SJ572403 binds to p27Kip1 with a Kd of 2.2 mM. It is specific for the D2 subdomain. In biochemical assays, SJ572403 (10 µM–3 mM) displaces p27-D2 from the Cdk2/cyclin A complex and partially restores Cdk2 kinase activity. This enables precise interrogation of p27-dependent cell-cycle control. The compound's binding can be studied using techniques such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Its effect on p27Kip1 function can be assessed by measuring its impact on CDK activity. |
| ln Vivo |
In vivo, SJ572403 can be used in studies about diseases with intrinsically disordered proteins. By modulating p27Kip1 function, it can affect cell cycle regulation and tumor suppression. Its potential applications are in cancer research and in studying diseases where protein disorder plays a role. Further studies are needed to evaluate its in vivo efficacy and safety.
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| Enzyme Assay |
The in vitro binding assay for SJ572403 involves measuring its affinity for the D2 subdomain of p27-KID. Recombinant p27-KID or the D2 subdomain is immobilized on a sensor chip or labeled with a fluorescent probe. Varying concentrations of SJ572403 (0.1 mM-10 mM) are added, and binding affinity (Kd) is measured using surface plasmon resonance (SPR) or fluorescence polarization. The compound's effect on Cdk2/cyclin A complex formation can be assessed by immunoprecipitation or pull-down assays. Cdk2 kinase activity is measured using a kinase assay with a suitable substrate.
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| Cell Assay |
In vitro cellular assays for SJ572403 use cell lines where p27Kip1 plays a regulatory role. Cells are cultured in appropriate media and treated with the compound at concentrations of 0.1-10 mM for 24-72 hours. Cell cycle analysis is performed by flow cytometry. CDK activity is measured by immunoprecipitating CDK complexes and assaying kinase activity. Cell viability is assessed using MTT or CCK-8 assays. The compound's effect on cell proliferation is evaluated. These assays help characterize the compound's mechanism as a p27Kip1 modulator.
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| Animal Protocol |
In vivo animal studies for SJ572403 would typically involve mouse models of cancer or other diseases where p27Kip1 is dysregulated. Mice are treated with the compound via oral gavage or intraperitoneal injection at doses of 1-50 mg/kg. Tumor growth is monitored. p27Kip1 levels and CDK activity in tumor tissues are measured. The compound's effect on cell cycle progression and tumor growth is assessed. Further studies are needed to establish its in vivo efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SJ572403 are not extensively reported. The compound has a molecular weight of 275.31 and a molecular formula of C13H17N5O2. It has a purity of ≥95%. It is soluble in DMSO. The compound should be stored at -20°C for long-term preservation. Based on its physicochemical properties, the compound is expected to have reasonable membrane permeability. Further studies on oral bioavailability, plasma half-life, and tissue distribution are needed.
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| References | |
| Additional Infomation |
SJ572403 is a p27Kip1 inhibitor with the CAS number 19970-45-7. Its molecular formula is C13H17N5O2 and molecular weight is 275.31. It binds to the D2 subdomain of p27-KID with a Kd of 2.2 mM. The compound is a research tool for studying intrinsically disordered proteins. It is not for human therapeutic use.
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| Molecular Formula |
C13H17N5O2
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|---|---|
| Molecular Weight |
275.3064
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| Exact Mass |
275.138
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| CAS # |
19970-45-7
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| PubChem CID |
3162678
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| Appearance |
White to off-white solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
456
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C2=C(N(C([H])([H])[H])C(N1C([H])([H])[H])=O)N=C1N(C([H])([H])C([H])([H])[H])C(C([H])([H])[H])=C(C([H])([H])[H])N12
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| InChi Key |
JKJLETUKWLALKV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H17N5O2/c1-6-17-7(2)8(3)18-9-10(14-12(17)18)15(4)13(20)16(5)11(9)19/h6H2,1-5H3
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| Chemical Name |
6-ethyl-2,4,7,8-tetramethylpurino[7,8-a]imidazole-1,3-dione
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| Synonyms |
SJ 403; SJ-403; SJ403
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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 : ~13.89 mg/mL (~50.45 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.39 mg/mL (5.05 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 13.9 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: ≥ 1.39 mg/mL (5.05 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 13.9 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: ≥ 1.39 mg/mL (5.05 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 | 3.6323 mL | 18.1613 mL | 36.3227 mL | |
| 5 mM | 0.7265 mL | 3.6323 mL | 7.2645 mL | |
| 10 mM | 0.3632 mL | 1.8161 mL | 3.6323 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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