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Cat. No.: HY-189422

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CDK9/EZH2-IN-2

CDK9/EZH2-IN-2 is a potent dual CDK9 and EZH2 inhibitor with an IC₅₀ of 8.9 nM against EZH2. CDK9/EZH2-IN-2 inhibits anti-apoptotic proteins and induces DNA damage by blocking the activity of CDK9 and EZH2, ultimately leading to tumor cell apoptosis. CDK9/EZH2-IN-2 can be used for research on diffuse large B-cell lymphoma.

For research use only. We do not sell to patients.

Formula: C₅₀H₆₀ClN₉O₅
Molecular Weight:902.52

Storage:

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

CDK9/EZH2-IN-2 Chemical Structure

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Amount: USD 0.00

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Use of MCE Products

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

^[1]

CDK9

8.9 nM (IC₅₀)

EZH2

Caspase-3

All CDK Isoforms :

All Histone Methyltransferase Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
U2932	IC₅₀	19.3 nM	Antiproliferative activity against human U-2932 cells assessed as reduction in cell viability incubated for 7 days. Antiproliferative activity against human U-2932 cells assessed as reduction in cell viability incubated for 7 days.	42542216
KARPAS-422	IC₅₀	9.1 nM	Antiproliferative activity against human KARPAS-422 cells assessed as reduction in cell viability incubated for 7 days. Antiproliferative activity against human KARPAS-422 cells assessed as reduction in cell viability incubated for 7 days.	42542216

In Vitro

Anti-cancerApoptosisOthers

Anti-cancer

CDK9/EZH2-IN-2 (Compound A9) (7 days) exhibits potent antiproliferative activity against U-2932 (IC₅₀ = 19.3 nM) and KARPAS-422 (IC₅₀ = 9.1 nM) DLBCL cell lines^[1].
CDK9/EZH2-IN-2 (0.1 μM; 24 h) downregulates p-Pol II Ser2, c-Myc, and Mcl-1 protein expression in U-2932 and KARPAS-422 cells^[1].

Apoptosis

Anti-cancer

CDK9/EZH2-IN-2 (15-60 nM; 48 h) dose-dependently induces apoptosis and triggers DNA damage in KARPAS-422 and U-2932 cells^[1].

Others

CDK9/EZH2-IN-2 exhibits dual inhibitory activity against EZH2 (IC₅₀ = 8.9 nM) and CDK9 (55.4% inhibition at 100 nM)^[1].

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

Western Blot Analysis^[1]

Cell Line:

U-2932 and KARPAS-422 cells
Concentration:

100 nM
Incubation Time:

48 h
Result:

Significantly downregulated the protein expression levels of p-Pol II Ser2, c-Myc, and Mcl-1.

Apoptosis Analysis^[1]

Cell Line:

KARPAS-422 cells
Concentration:

15 nM, 30 nM, 60 nM
Incubation Time:

48 h
Result:

Significantly increased the apoptosis rate of cells in a concentration-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

U-2932 cells
Concentration:

15 nM, 30 nM
Incubation Time:

48 h
Result:

Significantly increased the apoptosis rate of cells in a concentration-dependent manner, and its pro-apoptotic effect was stronger than the combined treatment of two single-target inhibitors.

Western Blot Analysis^[1]

Cell Line:

KARPAS-422 cells
Concentration:

15 nM, 30 nM, 60 nM
Incubation Time:

48 h
Result:

Promoted the cleavage of PARP and Caspase-3 (increased Cleaved-PARP and Cleaved-Caspase3 levels) in a concentration-dependent manner, while downregulating Rad51 expression and upregulating γ-H2AX levels, triggering a strong DNA damage response.

Related Protocols :

Chemical Information

Molecular Weight 902.52
Formula C₅₀H₆₀ClN₉O₅
SMILES

CC1=C(C(NCC2=C(C)C=C(C)NC2=O)=O)C=C(C3=CC=C(C(N[C@H]4CC[C@H](NC(NC5=CC(C6=C(CC(C)(C)C7)N7N=C6)=C(Cl)C=N5)=O)CC4)=O)C=C3)C=C1N(C8CCOCC8)CC
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

Handling Instructions (2659 KB)

References

[1]. Han Y, et al. Design and synthesis of dual-target CDK9-EZH2 inhibitors using a pharmacophore fusion strategy. Bioorganic & medicinal chemistry letters. 2026 Dec;141:130747.

Calculators

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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

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CDK9/EZH2-IN-2

All CDK Isoforms

All Histone Methyltransferase Isoforms

All Caspase Isoforms