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Cat. No.: HY-151375

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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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

CDK9/10/GSK3β-IN-1 Chemical Structure

CAS No.: 2423045-06-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 59 nM (HsGSK3β), 64 nM (HsCDK9/CyclinT), 1.093 µM (HsCDK5/p25), 1.725 µM (HsCDK2/CyclinA)^[1].

All CDK Isoforms :

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.

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.

Chemical Information

CAS No. 2423045-06-9
Molecular Weight 546.04
Formula C₂₉H₂₄ClN₃O₄S
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ibrahim N, et al. Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency. Eur J Med Chem. 2020 Aug 1;199:112355. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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CDK9/10/GSK3β-IN-1

All CDK Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

CDK9/10/GSK3β-IN-1 Related Classifications

HY-151375 Related Classifications