CDK9/10/GSK3β-IN-1
CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 μM) and HsCDK2/CyclinA (IC50=1.725 μM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines.
For research use only. We do not sell to patients.
- CAS No.: 2423045-06-9
- Formula: C29H24ClN3O4S
- Molecular Weight:546.04
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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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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
IC50: 59 nM (HsGSK3β), 64 nM (HsCDK9/CyclinT), 1.093 µM (HsCDK5/p25), 1.725 µM (HsCDK2/CyclinA)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
181 nM
Compound: 13c
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
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[PMID: 32402934] |
| K562 | IC50 |
50.8 nM
Compound: 13c
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Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
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[PMID: 32402934] |
| MIA PaCa-2 | IC50 |
52.9 nM
Compound: 13c
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Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
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[PMID: 32402934] |
| NCI-N87 | IC50 |
49 nM
Compound: 13c
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Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
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[PMID: 32402934] |
| PC-3 | IC50 |
85 nM
Compound: 13c
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Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
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[PMID: 32402934] |
| SK-BR-3 | IC50 |
53.7 nM
Compound: 13c
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Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
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[PMID: 32402934] |
| SK-OV-3 | IC50 |
0.094 μM
Compound: 13c
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Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
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[PMID: 32402934] |
In Vitro
CDK9/10/GSK3β-IN-1 (series concentration,72 h) exhibits high antiproliferative activity to SKOV3, NCIeN87, SKBR3, PC3, MiaPaCa-2, HCT116, K562 cells[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:SKOV3, NCIeN87, SKBR3, PC3, MiaPaCa-2, HCT116, K562 cells
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Concentration:Series concentration
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Incubation Time:72 h
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Result:Showed high antiproliferative activity, with an IC50 < 100 nM on 6 cancer cell lines, and up to six times more potent on the pancreatic cancer cells (MiaPaCa-2) than the reference compound, flavopiridol.
Chemical Information
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CAS No. 2423045-06-9
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Molecular Weight 546.04
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Formula C29H24ClN3O4S
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SMILES
ClC1=CC(SC2=NC3=CC=CC=C3N2C)=CC=C1C(OC4=C5C(O)=CC(O)=C4C(CC6)=CCN6C)=CC5=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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK9/10/GSK3β-IN-1 Related Classifications
HY-151375 Related Classifications
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