CST651
CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin-dependent kinase CDK4/6 PROTAC degrader with DC50 values of 20 nM and 5.1 nM, respectively. CST651 recruits the VHL E3 ubiquitin ligase to mediate the ubiquitination and proteasomal degradation of CDK4/6. CST651 inhibits cancer cell proliferation and migration. CST651 can be used in research related to breast cancer, multiple myeloma, acute myeloid leukemia, and acute lymphoblastic leukemia.
(Pink: CDK4 and CDK6 ligand (HY-50767); Blue: VHL ligand (HY-125905); Black: linker (HY-W017440)).
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- No. CAS: 2489241-16-7
- Fòrmula: C56H72FN11O9S
- Peso molecular:1094.30
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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CDK6 5.1 nM (DC50, In MM.1S cells) |
CDK4 20 nM (DC50, In MM.1S cells) |
VHL |
CST651 (0.0001-1 μM; 3-96 h) potently and selectively degrades CDK6 but not CDK4 in MM.1S cells via the CRL2VHL- and proteasome-dependent pathway, with a CDK6 DC50 of 5.1 nM, and exerts a durable degradation effect after washout[2].
CST651 (0.1 nM-0.1 mM; 96 h) inhibits the viability of HEL acute myeloid leukemia cells with an IC50 of 0.45 μM, exhibiting stronger potency than Palbociclib (HY-50767)[2].
CST651 (0.1 μM; 24 h) reduces the migratory capacity of MDA-MB-231 breast cancer cells by 29% at a concentration of 0.1 μM, and its efficacy is superior to that of Palbociclib[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human multiple myeloma MM.1S cells
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Concentration:0.0001-1 μM (16 h); 0.1 μM (co-treated with 10 μM VH298, MG132, or MLN4924, 16 h); 0.1 μM (washout followed by 3-96 h incubation); 0.1 μM (96 h)
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Incubation Time:16 h (single treatment, co-treatment); 3-96 h (postwashout incubation); 96 h
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Result:Induced concentration-dependent degradation of CDK6 and CDK4, with a DC50 of 5.1 nM for CDK6 and >95% maximum CDK6 degradation at 100 nM after 16 h.
Reduced CDK6 levels to 1.4% and CDK4 levels to 44% at 0.1 μM after 16 h.
Abrogated CDK4/6 degradation when co-treated with 100-fold excess VH298.
Prevented proteasomal degradation of CDK6 when co-treated with MG132 or MLN4924.
Maintained CDK6 degradation for up to 72 h post-washout, with CDK6 levels remaining below 50% of baseline.
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Cell Line:human acute myeloid leukemia HEL cells
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Concentration:10-10-10-4 M
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Incubation Time:96 h
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Result:Inhibited HEL cell viability with an IC50 of 0.45 μM.
Exhibited greater potency than palbociclib (IC50 = 4.16 μM) and VHL-based PROTAC 27 (IC50 = 1.54 μM).
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Cell Line:human breast cancer MDA-MB-231 cells
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Concentration:0.1 μM
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Incubation Time:24 h
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Result:Reduced MDA-MB-231 cell migration by 29%.
Exhibited a greater effect than palbociclib (17% reduction).
Chemical Information
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No. CAS 2489241-16-7
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Peso molecular 1094.30
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Fòrmula C56H72FN11O9S
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SMILES
O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCN(CCOCCOCCOC6=CC(C7=C(C)N=CS7)=CC=C6CNC([C@H]8N(C([C@H](C(C)(C)C)NC(C9(CC9)F)=O)=O)C[C@H](O)C8)=O)CC5)C=N4)C
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Synonyms
PROTAC CDK4/6 degrader 34
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Kossakowski K, et al. FDA-approved kinase inhibitors in PROTAC design, development and synthesis. Journal of enzyme inhibition and medicinal chemistry. 2025 Dec;40(1):2542357. [Content Brief]
[2]. Steinebach C, et al. Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders. Chemical science. 2020 Apr 07;11(13):3474-3486. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CST651 Related Classifications
HY-134303 Related Classifications
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