PIN1 degrader-3
PIN1 degrader-3 is a Pin1 (peptidyl-prolyl isomerase protein) (IC50 = 4.65 nM) degrader. PIN1 degrader-3 bound covalently to Pin1. PIN1 degrader-3-induced Pin1 degradation reduced cell viability, with EC50 values after 72 h of 8.4 μM in MIA PaCa-2 cells and 5.3 μM in KPC cell lines.PIN1 degrader-3 can destabilize Pin1 in vitro, causing its degradation in cells. PIN1 degrader-3 can be used for the study of pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 3101950-55-1
- Formula: C31H34Cl2N6O4
- Molecular Weight:625.55
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Pin1 4.65 nM (IC50) |
PIN1 degrader-3 (Compound 164B8; Compound H-3-V) (250 μM, 3 h) binds to Pin1, causing a conformational change that affects the loop FG and helix D regions[1].
PIN1 degrader-3 (0-15 μM, 24 h) effectively induces dose-dependent degradation of MIA PaCa-2 and Pin1 in human pancreatic cancer cell line BxPC3 and mouse pancreatic cancer cell line KPC[1].
PIN1 degrader-3 (5 μM, 24 h)-induced Pin1 degradation in BxPC3 and KPC cell lines is reversible[1].
PIN1 degrader-3 (0.5-10 μM, 24 h) induces dose-dependent degradation of Pin1 in all CAFs (Cancer-Associated Fibroblasts) (CAF-BTG for cholangiocarcinoma, CAF-APP for appendiceal cancer, and CAF-COL for colorectal cancer)[1].
PIN1 degrader-3 (72 h)-induced Pin1 degradation reduced cell viability, with EC50 values of 8.4 μM in MIA PaCa-2 cells and 5.3 μM in KPC cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC3 cells, MIA PaCa-2 cells, KPC cells
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Concentration:0 μM, 0.5 μM, 1 μM, 3 μM, 5 μM, 10 μM, 15 μM
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Incubation Time:24 h
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Result:Pin1 protein levels decreased in a dose-dependent manner in all three cell lines.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NSG mice were used to establish a peritoneal metastasis model by intraperitoneal injection of KPC pancreatic cancer cells expressing GFP and luciferase[1].
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Dosage:30 mg/kg, 60 mg/kg
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Administration:I.p., once a day, 5 days a week, for 2 weeks
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Result:Tumor burden decreased significantly in a dose-dependent manner.
Mild anemia and moderate thrombocytopenia occurred in the 60 mg/kg group.
Chemical Information
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CAS No. 3101950-55-1
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Molecular Weight 625.55
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Formula C31H34Cl2N6O4
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SMILES
O=C(NC)[C@@H](NC([C@@H]1CCCCN1C([C@@H](NC(CCl)=O)CC2=CNC3=C2C=CC(Cl)=C3)=O)=O)CC4=CNC5=C4C=CC=C5
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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)
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