2. Cell Cycle/DNA Damage
  3. CDK
  4. 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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CDK2-IN-28 Chemical Structure

CDK2-IN-28 Chemical Structure

CAS No. : 3025006-64-5

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CDK2-IN-28 Related Antibodies

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  • Biological Activity

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Description

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)[1].

IC50 & Target

CDK7

54.7 nM (Ki, [1])

CDK2

1 nM (Ki, [1])

CDK5

15.8 nM (Ki, [1])

CDK9

12.8 nM (Ki, [1])

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.

CDK2-IN-28 Related Antibodies

Western Blot Analysis[1]

Cell Line: MKN1 cells
Concentration: 37 nM, 111.1 nM, 333.3 nM, 1000 nM, 3000 nM
Incubation Time: 24 h
Result: Significantly downregulated Rb phosphorylation at Ser807/811 and Ser780 in dose dependent way.

Cell Cycle Analysis[1]

Cell Line: MKN1 cells
Concentration: 111.1 nM and 333.3 nM
Incubation Time: 24 h
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

CDK2-IN-28 (10 mg/kg; po; single dose) provides poor plasma exposure in mouse, and CDK2-IN-28 (1 mg/kg; iv; single dose) also shows high plasma clearance (159-236 mL/min/kg) in mouse PK assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

513.66

Formula

C25H35N7O3S
CAS No.
SMILES

CS(C1=CC=C(CN2)C(OCCCCCN(CC3CNC3)C4=NC5=C(C(C)C)C=NN5C2=N4)=C1)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CDK2-IN-28 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK2-IN-283025006-64-5CDKCyclin dependent kinaseCCNE1 amplificationCyclin-dependent kinase 2MacrocycleMolecular dynamic simulationsSmall molecule inhibitorInhibitorinhibitorinhibit

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