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.
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- Formule: C50H60ClN9O5
- Masse moléculaire:902.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
CDK9 8.9 nM (IC50) |
EZH2 |
Caspase-3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| U2932 | IC50 |
19.3 nM
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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.
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42542216 |
| KARPAS-422 | IC50 |
9.1 nM
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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.
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42542216 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-2932 and KARPAS-422 cells
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Concentration:100 nM
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Incubation Time:48 h
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Result:Significantly downregulated the protein expression levels of p-Pol II Ser2, c-Myc, and Mcl-1.
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Cell Line:KARPAS-422 cells
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Concentration:15 nM, 30 nM, 60 nM
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Incubation Time:48 h
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Result:Significantly increased the apoptosis rate of cells in a concentration-dependent manner.
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Cell Line:U-2932 cells
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Concentration:15 nM, 30 nM
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Incubation Time:48 h
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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.
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Cell Line:KARPAS-422 cells
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Concentration:15 nM, 30 nM, 60 nM
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Incubation Time:48 h
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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.
Chemical Information
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Masse moléculaire 902.52
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Formule C50H60ClN9O5
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK9/EZH2-IN-2 Related Classifications
HY-189422 Related Classifications
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