2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK2-IN-51

CDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC50 of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal cancer.

For research use only. We do not sell to patients.

CDK2-IN-51

CDK2-IN-51 Chemical Structure

CAS No. : 1443-10-3

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CDK2-IN-51 Related Antibodies

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Description

CDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC50 of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

CDK2

23.47 nM (IC50)

CDK2

4.11 μM (Ki)

In Vitro

CDK2-IN-51 (compound 6) (10-50 μM; 24-72 h) demonstrates significant antiproliferative activity against HCT-116 and HT-29 cells with no cytotoxicity to NCM-460D cells[1].
CDK2-IN-51 (40-50 μM; 48 h) induces pre-G1 phase arrest in HCT-116 and HT-29 cells without S-phase arrest[1].
CDK2-IN-51 (40-50 μM; 48-72 h) downregulates CDK2 protein targets involved in DNA replication process; Polα, MCM7, ORC2, and ORC4 in HCT-116 and HT-29 cells, and does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression[1].

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

CDK2-IN-51 Related Antibodies

Cell Viability Assay[1]

Cell Line: HCT-116, HT-29, NCM-460D
Concentration: 10 μM, 20 μM, 40 μM, 50 μM
Incubation Time: 24 h, 48 h, 72 h
Result: At 72 h, exhibited significant antiproliferative effects on HCT-116 and HT-29 cells, with IC50 values of 46.41 μM and 61.47 μM, respectively, and showed no cytotoxicity on NCM-460D cells, with an IC50 value of >100 μM.

Cell Cycle Analysis[1]

Cell Line: HCT-116, HT-29
Concentration: 40 μM, 50 μM
Incubation Time: 48 h
Result: Caused a significant increase in the pre-G1 phase population in both HCT-116 and HT-29 cells, indicating cell death, and no S-phase arrest was observed, suggesting that the compound did not induce apoptosis.

Western Blot Analysis[1]

Cell Line: HCT-116, HT-29
Concentration: 40 μM, 50 μM
Incubation Time: 48 h, 72 h
Result: Reduced the expression of CDK2 targets, MCM7, ORC2, and ORC4 proteins.
Reduced Polα levels. 
Molecular Weight

288.35

Formula

C18H16N4
CAS No.
SMILES

CC1=NC2=NN3C(C)=CC(C)=NC3=C2C(C4=CC=CC=C4)=C1
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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-51 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-511443-10-3CDKCyclin dependent kinaseCDK2HT-29PyrazolopyridineHCT-116NCM-460DColorectal CancerPyrazoloStructure-activity relationship (SAR)Pyrazolo[3,4-b]pyridineInhibitorinhibitorinhibit

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