1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK1-IN-1

CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent.

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CDK1-IN-1 Chemical Structure

CDK1-IN-1 Chemical Structure

CAS No. : 2761858-59-5

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Description

CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent[1].

IC50 & Target

CDK1/cycB

161.2 nM (IC50)

In Vitro

CDK1-IN-1 (compound 7a) (10 µM, 48 hours) has the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes[1].
CDK1-IN-1 (0.1-100 μM, 48 hours) has better selectivity for cancer cells over normal cell lines (IC50 of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8)[1].
CDK1-IN-1 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) has a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase[1].
CDK1-IN-1 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) can cause cell death mainly through apoptosis rather than necrosis and confirmed that its activity is more selective to cancerous cells than normal cells[1].
CDK1-IN-1 (6.28 μM; 48 hours) induce apoptosis in p53 dependent manner through the intrinsic apoptotic pathway in HCT-116 cells[1].

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

Cell Proliferation Assay

Cell Line: 60 human cancer cell lines (LOX IMVI, IGROV1, A498, COLO205 et al.)[1]
Concentration: 10 µM
Incubation Time: 48 hours
Result: Had the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes.

Cell Cytotoxicity Assay

Cell Line: HCT-116 and WI-38 cells[1]
Concentration: 0.1-100 μM
Incubation Time: 48 hours
Result: Had better selectivity for cancer cells over normal cell lines (IC50 of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8).

Cell Cycle Analysis

Cell Line: HCT-116 and WI-38 cells[1]
Concentration: 17.7 μM in WI-38 and 6.28 μM in HCT-116
Incubation Time: 48 hours
Result: Exerted a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase.
Molecular Weight

465.50

Formula

C27H23N5O3

CAS No.
SMILES

O=C(C1=C2N=C(C3=CC=CC=C3)C=C(C4=CC=CC=C4)N2N=C1NC5=CC=C(OC)C=C5OC)N

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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CDK1-IN-1 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.

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CDK1-IN-1
Cat. No.:
HY-115924
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