CDK9-IN-42
CDK9-IN-42 is a potent and selective CDK9 inhibitor with an IC50of 3.8 nM. CDK9-IN-42 can inhibit the growth of cancer cells and induce apoptosis by downregulating Myc-1 and c-Myc. CDK9-IN-42 can be used for the research of cancer, such as breast and lungcancer.
For research use only. We do not sell to patients.
- Formula: C22H19FN6O3S2
- Molecular Weight:498.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
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CDK9 3.8 nM (IC50) |
Caspase 3 |
CDK9-IN-42 (Compound L18) (72 h) inhibits proliferation of various hematological tumor cells, with IC50 values of 0.049 μM, 0.071 μM, 0.062 μM, 0.093 μM and 0.175 μM against MV4-11, MOLM-13, THP-1, KG-1, and HL-60 cells, respectively[1].
CDK9-IN-42 (72 h) inhibits proliferation of various solid tumor cells, with IC50 values of 0.045 μM, 0.166 μM, 0.247 μM and 0.225 μM against HepG2, MCF-7, 22RV1 and A549 cells, respectively[1].
CDK9-IN-42 (0.1-1 μM, 72 h) exhibits low cytotoxicity against normal human bronchial epithelial cells, with an IC50 of 0.402 μM against BEAS-2B cells[1].
CDK9-IN-42 shows excellent selectivity for CDK9 over other CDK family members, with IC50 >1 μM for CDK1, CDK4, CDK6, and CDK7[1].
CDK9-IN-42 (0.1-0.5 μM, 12 h) downregulates protein levels of p-RNAPII-ser2, Mcl-1, c-Myc, CDK9 and Cyclin T1 protein in MV4-11 cells[1].
CDK9-IN-42 (0.5-1 μM, 12 h) induces apoptosis in MV4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:0.1, 0.25, 0.5, 1 and 2 μM
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Incubation Time:2, 4, 8, 12 and 24 h
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Result:Decreased levels of p-RNAPII-ser2, Mcl-1, c-Myc, CDK9 and Cyclin T1 protein.
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Cell Line:MV4-11 cells
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Concentration:0.5 and 1 μM
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Incubation Time:12 h
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Result:Increased apoptosis rates.
Downregulated PARP and Caspase-3 proteins.
Upregulated Cleaved-PARP and Cleaved-Caspase-3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice[1]
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Dosage:15, 30 and 50 mg/kg
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Administration:Intravenously, Subcutaneous
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Result:Showed no death or significant weight loss.
Chemical Information
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Molecular Weight 498.55
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Formula C22H19FN6O3S2
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SMILES
FC1=CC(OC)=C(C2=NC=NC(NC3=CC(CS(C)(=NC(C4=CN=CS4)=O)=O)=CC=C3)=N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)