Cyclin K degrader 3
Cyclin K degrader 3 is a potent and selective cyclin K molecular glue degrader with a DC50 of 24 nM. Cyclin K degrader 3 is a CDK inhibitor with IC50 values of 86, 44, and 172 nM against CDK2/9/12, respectively.Cyclin K degrader 3 binds to the CDK12-cyclin K complex and recruits the DDB1-CUL4-RBX1 E3 ubiquitin ligase, thereby triggering ubiquitination and degradation of cyclin K. Cyclin K degrader 3 can be used for research on triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 294647-05-5
- Formula: C25H30N6O
- Molecular Weight:430.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CDK12/Cyclin K 24 nM (DC50) |
CDK2 86 nM (IC50) |
CDK9 44 nM (IC50) |
CDK12 172 nM (IC50) |
In Vitro
Cyclin K degrader 3 (1 μM; 6 h) induces a specific transcriptional signature (significantly alters the gene expression profile) in MDA-MB-231 cells, and this transcriptional signature is distinct from that of CDK inhibitors alone[1].
Cyclin K degrader 3 inhibits CDK2, CDK9, and CDK12 with IC50 values of 86, 44, and 172 nM, respectively[1].
CDK12 degrader-1 (5 h) degrades cyclin K in HEK293T cells expressing a cyclin K-eGFP reporter, with a DC50 of 24 nM[1].
Cyclin K degrader 3 (72 h) reduces cell viability in HEK293T-Cas9 cells with EC50 = 159 nM, and this effect is partially reversed by the Neddylation inhibitor MLN4924 (HY-70062), with EC50 = 703 nM after addition of MLN4924[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 294647-05-5
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Molecular Weight 430.55
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Formula C25H30N6O
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SMILES
CC[C@@H](NC1=NC(NCC2=CC=C(C3=CC=CC=C3)C=C2)=C4C(N(C(C)C)C=N4)=N1)CO
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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)
Cyclin K degrader 3 Related Classifications
HY-190210 Related Classifications
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