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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C50H60ClN9O5
- 分子量:902.52
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保管条件:
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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 |
体外実験
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].
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].
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.
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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.
化学情報
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分子量 902.52
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CDK9/EZH2-IN-2 関連分類
HY-189422 関連分類
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