PROTAC PIN1 degrader-2
PROTAC PIN1 degrader-2 is a PROTAC PIN1 degrader. PROTAC PIN1 degrader-2 reduces PIN1-mediated oncogene expression, upregulates PIN1-inhibited tumor suppressor genes, and exerts killing effects on cancer cells. PROTAC PIN1 degrader-2 inhibits tumor growth in breast cancer mouse xenograft models. PROTAC PIN1 degrader-2 can be used for the research of breast cancer.
(Pink: PIN1 ligand (HY-186219); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3083422-10-7
- Formula: C28H34ClN3O10S
- Molecular Weight:640.10
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
PROTAC PIN1 degrader-2 (compound A1) (2.2 μM-20 μM; 0-36 h) specifically degrades PIN1 protein in MCF-7 breast cancer cells with a DC50 of 269 nM, achieving 90% degradation at 2.2 μM and reaching maximum degradation at 12 hours post-treatment[1].
PROTAC PIN1 degrader-2 (2.2 μM-20 μM; 0-36 h) degrades PIN1 protein in PATU-8988t pancreatic cancer cells, with effective degradation at 2.2 μM and a Hook effect occurring at 20 μM[1].
PROTAC PIN1 degrader-2 (0.08 μM-20 μM; 72 h) inhibits the viability of MCF-7 breast cancer cells, and this inhibitory activity is enhanced in an additive manner when combined with RO3306[1].
PROTAC PIN1 degrader-2 (0.08 μM-20 μM; 72 h) inhibits the viability of PATU-8988t pancreatic cancer cells, and this inhibitory activity is enhanced in an additive manner when combined with RO3306[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 breast cancer cells
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Concentration:2.2; 6.7; 20 μM
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Incubation Time:0; 6; 12; 18; 24; 36 h
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Result:Significantly reduced PIN1 protein levels.
Achieved 90% degradation efficiency at 2.2 μM.
Exhibited a DC50 value of 269 nM for PIN1 degradation.
Reached peak PIN1 degradation at 12 hours, followed by protein recovery after 12 hours.
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Cell Line:MCF-7 breast cancer cells
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Concentration:0.08; 0.25; 0.74; 2.22; 6.66; 20 μM
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Incubation Time:72 h
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Result:Inhibited MCF-7 cell viability in a concentration-dependent manner when used alone.
Showed additive cell viability inhibition effect when combined with 1 μM or 5 μM RO3306, with significantly stronger inhibition than the degrader alone at equivalent concentrations.
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Cell Line:PATU-8988t pancreatic cancer cells
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Concentration:0.08; 0.25; 0.74; 2.22; 6.66; 20 μM
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Incubation Time:72 h
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Result:Inhibited PATU-8988t cell viability in a concentration-dependent manner when used alone.
Showed additive cell viability inhibition effect when combined with 1 μM or 5 μM RO3306, with significantly stronger inhibition than the degrader alone at equivalent concentrations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-Nude mice (female, 5 weeks old, MCF-7 cell xenograft model with estradiol pre-treatment)[1]
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Dosage:50 mg/kg
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Administration:i.p.; every other day; 20 days
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Result:Inhibited tumor growth significantly compared to vehicle control group after 20 days.
Maintained stable body weight and exhibited normal behavior with no observed toxicity.
Chemical Information
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CAS No. 3083422-10-7
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Molecular Weight 640.10
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Formula C28H34ClN3O10S
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SMILES
O=C(CCCOC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)OCC(C)(CN(C4CCS(=O)(C4)=O)C(CCl)=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)
PROTAC PIN1 degrader-2 Related Classifications
HY-186218 Related Classifications
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