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  4. 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.

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CDK9/10/GSK3β-IN-1 Chemical Structure

CDK9/10/GSK3β-IN-1 Chemical Structure

CAS No. : 2423045-06-9

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CDK9/10/GSK3β-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 59 nM (HsGSK3β), 64 nM (HsCDK9/CyclinT), 1.093 µM (HsCDK5/p25), 1.725 µM (HsCDK2/CyclinA)[1].
Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
181 nM
Compound: 13c
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
[PMID: 32402934]
K562 IC50
50.8 nM
Compound: 13c
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
[PMID: 32402934]
MIA PaCa-2 IC50
52.9 nM
Compound: 13c
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
[PMID: 32402934]
NCI-N87 IC50
49 nM
Compound: 13c
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
[PMID: 32402934]
PC-3 IC50
85 nM
Compound: 13c
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
[PMID: 32402934]
SK-BR-3 IC50
53.7 nM
Compound: 13c
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
[PMID: 32402934]
SK-OV-3 IC50
0.094 μM
Compound: 13c
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
[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.

CDK9/10/GSK3β-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: SKOV3, NCIeN87, SKBR3, PC3, MiaPaCa-2, HCT116, K562 cells
Concentration: Series concentration
Incubation Time: 72 h
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.
Molecular Weight

546.04

Formula

C29H24ClN3O4S
CAS No.
SMILES

ClC1=CC(SC2=NC3=CC=CC=C3N2C)=CC=C1C(OC4=C5C(O)=CC(O)=C4C(CC6)=CCN6C)=CC5=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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CDK9/10/GSK3β-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.

Keywords:

CDK9/10/GSK3β-IN-12423045-06-9OthersflavopiridolcancerSKOV3NCIeN87SKBR3PC3MiaPaCa-2HCT116K562Inhibitorinhibitorinhibit

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