Cyclin K degrader 2
Cyclin K degrader 2 is a molecular glue degrader of Cyclin K. By bridging CDK12 and DDB1, the receptor of the CRL4 E3 ligase, Cyclin K degrader 2 specifically induces the targeted degradation of Cyclin K within the CDK12-Cyclin K complex. Cyclin K degrader 2 can be used in studies related to acute myeloid leukemia.
For research use only. We do not sell to patients.
- Formula: C19H20N4OS2
- Molecular Weight:384.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
CDK1 |
CDK9 |
In Vitro
Cyclin K degrader 2 (compound S656) (0.5-10 µM; 5-14 days) exhibits significant growth inhibitory effects and antiproliferative activity in 56 primary AML samples; it displays a bimodal distribution of growth inhibition and cytotoxicity across 157 primary AML samples, and induces CRL4 complex-dependent cytotoxicity in OCI-AML1 (EKO) cells[1].
Cyclin K degrader 2 (5-8 µM; 5 h) significantly degrades the Cyclin K protein in OCI-AML5 cells and 3 primary AML samples[1].
Cyclin K degrader 2 (10 µM; 3 h) exhibits the ability to reduce fluorescence intensity and induce Cyclin K degradation in OCI-AML5 (G7 clone) cells expressing the cyclin K-eGFP reporter gene[1].
Cyclin K degrader 2 (1-10 µM; 4-6 h) dose-dependently degrades Cyclin K and CDK12 proteins in OCI-AML5 cells, and significantly downregulates the mRNA expression of DNA damage response (DDR) genes[1].
Cyclin K degrader 2 (1-5 µM; 4-24 h) induces G1-phase cell cycle arrest, dose-dependently triggers apoptosis, and depletes the anti-apoptotic protein Mcl-1 and the oncoprotein c-MYC in OCI-AML5 cells; it also induces γH2AX focus formation in U2OS cells[1].
Cyclin K degrader 2 (0.625 nM-10 µM; 1 h) induces the protein-protein interaction between CDK12 and DDB1 in a dose-dependent manner in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OCI-AML5 cells
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Concentration:1 µM, 3 µM, 10 µM
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Incubation Time:6 h
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Result:Induced the degradation of Cyclin K and CDK12 in a concentration-dependent manner.
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Cell Line:OCI-AML5 cells
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Concentration:5 µM
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Incubation Time:4 h
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Result:Significantly decreased the mRNA levels of DDR genes such as BRCA1, BRCA2, ATR, BLM, ERCC4, BARD1, and RAD51.
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Cell Line:OCI-AML5 cells
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Concentration:1 µM, 3 µM, 5 µM
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Incubation Time:24 h
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Result:Induced early and late apoptosis in a dose-dependent manner.
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Cell Line:OCI-AML5 cells
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Concentration:1µM, 3 µM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at the G1 phase.
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Cell Line:U2OS cells
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Concentration:2 µM
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Incubation Time:24 h
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Result:Increased the number of gH2AX foci in the nucleus, demonstrating the induction of DNA damage.
Chemical Information
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Molecular Weight 384.52
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Formula C19H20N4OS2
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SMILES
CN(C1=CC=C(C=C1)CC(NC2=NC=C(S2)SCC3=CC=CN=C3)=O)C
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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)