CDK16/CycY-IN-1
CDK16/CycY-IN-1 is a CDK16/CycY inhibitor (IC50 = 125.2 nM) and also inhibits CDK6/CycD1, CDK9/CycT1, and CDK4/CycD3. CDK16/CycY-IN-1 exhibits anti-tumor cell proliferation activity, inhibits colony formation, migration, and p53 Ser315 phosphorylation, and induces S-phase cell cycle accumulation and apoptosis. CDK16/CycY-IN-1 shows anti-tumor activity in the H460 xenograft tumor model. CDK16/CycY-IN-1 can be used for research on non-small cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- Formula: C25H27N3O4
- Molecular Weight:433.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Biological Activity
Description
CDK16/CycY-IN-1 is a CDK16/CycY inhibitor (IC50 = 125.2 nM) and also inhibits CDK6/CycD1, CDK9/CycT1, and CDK4/CycD3. CDK16/CycY-IN-1 exhibits anti-tumor cell proliferation activity, inhibits colony formation, migration, and p53 Ser315 phosphorylation, and induces S-phase cell cycle accumulation and apoptosis. CDK16/CycY-IN-1 shows anti-tumor activity in the H460 xenograft tumor model. CDK16/CycY-IN-1 can be used for research on non-small cell lung cancer (NSCLC)[1].
IC50 & Target
[1]|
CDK16/Cyclin Y 125.2 nM (IC50) |
CDK6/cycD1 |
CDK9/CycT1 |
CDK4/CycD3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H460 | GI50 |
1.82 μM
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Antiproliferative activity against human H460 cells assessed as GI50 by CCK-8 assay after 72 hrs incubation.
Antiproliferative activity against human H460 cells assessed as GI50 by CCK-8 assay after 72 hrs incubation.
|
j.bioorg.2026.110559 |
| A549 | GI50 |
1.97 μM
|
Antiproliferative activity against human A549 cells assessed as GI50 by CCK-8 assay after 72 hrs incubation.
Antiproliferative activity against human A549 cells assessed as GI50 by CCK-8 assay after 72 hrs incubation.
|
j.bioorg.2026.110559 |
| MV4-11 | GI50 |
2.30 μM
|
Antiproliferative activity against human MV-4-11 cells assessed as GI50 by CCK-8 assay after 72 hrs incubation.
Antiproliferative activity against human MV-4-11 cells assessed as GI50 by CCK-8 assay after 72 hrs incubation.
|
j.bioorg.2026.110559 |
| HCT-116 | GI50 |
9.56 μM
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Antiproliferative activity against human HCT116 cells assessed as GI50 by CCK-8 assay after 72 hrs incubation.
Antiproliferative activity against human HCT116 cells assessed as GI50 by CCK-8 assay after 72 hrs incubation.
|
j.bioorg.2026.110559 |
| HepG2 | GI50 |
10 μM
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Antiproliferative activity against human HepG2 cells assessed as GI50 greater than 10 μM by CCK-8 assay after 72 hrs incubation.
Antiproliferative activity against human HepG2 cells assessed as GI50 greater than 10 μM by CCK-8 assay after 72 hrs incubation.
|
j.bioorg.2026.110559 |
| MCF7 | GI50 |
10 μM
|
Antiproliferative activity against human MCF-7 cells assessed as GI50 greater than 10 μM by CCK-8 assay after 72 hrs incubation.
Antiproliferative activity against human MCF-7 cells assessed as GI50 greater than 10 μM by CCK-8 assay after 72 hrs incubation.
|
j.bioorg.2026.110559 |
| THLE-2 | GI50 |
10 μM
|
Antiproliferative activity against human THLE-2 cells assessed as GI50 greater than 10 μM by CCK-8 assay after 72 hrs incubation.
Antiproliferative activity against human THLE-2 cells assessed as GI50 greater than 10 μM by CCK-8 assay after 72 hrs incubation.
|
j.bioorg.2026.110559 |
| H9c2 | GI50 |
10 μM
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Antiproliferative activity against rat H9c2 cells assessed as GI50 greater than 10 μM by CCK-8 assay after 72 hrs incubation.
Antiproliferative activity against rat H9c2 cells assessed as GI50 greater than 10 μM by CCK-8 assay after 72 hrs incubation.
|
j.bioorg.2026.110559 |
In Vitro
Anti-cancerApoptosisCell Cycle RegulationOthers
Anti-cancer
CDK16/CycY-IN-1 shows low micromolar antiproliferative activity in H460 (GI50 1.82 μM), A549 (GI50 1.97 μM), and MV-4-11 (GI50 2.30 μM) cells, with weaker activity in HCT116 and other tested cell lines[1].
CDK16/CycY-IN-1 (1-4 μM; 24 h) reduces H460 colony formation in a concentration-dependent manner[1].
CDK16/CycY-IN-1 (1-4 μM; 24 h) reduces wound closure of H460 in wound healing assays; reduces H460 cell migration in Transwell assays; decreases the relative phosphorylation level of p53 Ser315 and increases total p53 protein in H460 cells[1].
CDK16/CycY-IN-1 (1-4 μM; 24 h) reduces H460 colony formation in a concentration-dependent manner[1].
CDK16/CycY-IN-1 (1-4 μM; 24 h) reduces wound closure of H460 in wound healing assays; reduces H460 cell migration in Transwell assays; decreases the relative phosphorylation level of p53 Ser315 and increases total p53 protein in H460 cells[1].
Anti-cancer
Cell Cycle Regulation
CDK16/CycY-IN-1 (1-4 μM; 12 h) is associated with S-phase accumulation in H460 cells[1].
Others
CDK16/CycY-IN-1 (AT-11) inhibits recombinant human CDK16/CycY with an IC50 of 125.2 nM[1].
CDK16/CycY-IN-1 (1 μM) shows the strongest inhibitory effect on CDK16/CycY (90.3%), followed by CDK6/CycD1 (76.4%), CDK9/CycT1 (58.7%), and CDK4/CycD3 (52.1%)[1].
CDK16/CycY-IN-1 (1 μM) shows the strongest inhibitory effect on CDK16/CycY (90.3%), followed by CDK6/CycD1 (76.4%), CDK9/CycT1 (58.7%), and CDK4/CycD3 (52.1%)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
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Cell Line:H460 cells
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Concentration:1, 2, 4 μM
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Incubation Time:24 h exposure; 10-14 days fresh medium culture
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Result:Reduced H460 colony formation in a concentration-dependent manner.
Cell Cycle Analysis[1]
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Cell Line:H460 cells
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Concentration:1, 2, 4 μM
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Incubation Time:12 h
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Result:Reached S‑phase populations of 22.22%, 36.37%, and 42.82% at 1, 2, and 4 μM, respectively; attained G0/G1 populations of 57.36%, 45.86%, and 47.85%; and obtained G2/M populations of 20.42%, 17.77%, and 9.33%.
Apoptosis Analysis[1]
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Cell Line:H460 cells
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Combined early- and late-apoptotic fractions were 40.89%, 60.87%, and 79.68% at 1, 2, and 4 μM, respectively.
Cell Migration Assay [1]
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Cell Line:H460 cells
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Reduced H460 cell migration in the Transwell assay.
Reduced H460 wound closure in the wound healing assay.
Western Blot Analysis[1]
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Cell Line:H460 cells
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Reduced relative p53 Ser315 phosphorylation and increases total p53 protein in H460 cells.
In Vivo
Anti-cancer
CDK16/CycY-IN-1 (AT-11) (20 mg/kg; i.v.; once every other day; 15 days) produces a 48.2% tumor growth inhibition rate in the BALB/c nude mouse H460 xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Related Protocols :
- Cell migration
- Somatic Cell Culture
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Apoptosis Solutions
- Soft Agar Colony Formation Assay
- MTT Cell Proliferation Assay
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Molecular Weight 433.50
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Formula C25H27N3O4
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SMILES
O=C(N(C(C)C)C1=C2OC(C3=CC=C(CN4CCC(N)CC4)C=C3)=C5)OC1=CC=C2C5=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
References
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CDK16/CycY-IN-1 Related Classifications
HY-190643 Related Classifications
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