CDK2-IN-28
CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM).
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- CAS No.: 3025006-64-5
- Formule: C25H35N7O3S
- Masse moléculaire:513.66
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
IC50 & Target
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CDK7 54.7 nM (Ki, [1]) |
CDK2 1 nM (Ki, [1]) |
CDK5 15.8 nM (Ki, [1]) |
CDK9 12.8 nM (Ki, [1]) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MKN-1 | EC50 |
0.31 μM
Compound: 22
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Antiproliferative activity against human MKN-1 cells incubated for 5 days by CCK-8 assay
Antiproliferative activity against human MKN-1 cells incubated for 5 days by CCK-8 assay
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[PMID: 38583237] |
In Vitro
CDK2-IN-28 (37 nM-3 μM; 24 h) significantly down-regulates the level of Rb phosphorylation at Ser807/811 and Ser780 in MKN1 cells[1].
CDK2-IN-28 (333.3 nM; 24 h) CDK2 inhibition in MKN1 cells causes cell cycle arrest in the G2/M phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MKN1 cells
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Concentration:37 nM, 111.1 nM, 333.3 nM, 1000 nM, 3000 nM
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Incubation Time:24 h
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Result:Significantly downregulated Rb phosphorylation at Ser807/811 and Ser780 in dose dependent way.
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Cell Line:MKN1 cells
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Concentration:111.1 nM and 333.3 nM
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Incubation Time:24 h
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Result:Caused by CDK2 inhibition is accumulation of G0/G1 cells as the CDK2/cyclin E-mediated phosphorylation of Rb relieves suppression of the E2Fs, thus allowing G1/S transition through the restriction point.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3025006-64-5
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Masse moléculaire 513.66
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Formule C25H35N7O3S
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SMILES
CS(C1=CC=C(CN2)C(OCCCCCN(CC3CNC3)C4=NC5=C(C(C)C)C=NN5C2=N4)=C1)(=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK2-IN-28 Related Classifications
HY-161463 Related Classifications
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