2. PI3K/Akt/mTOR
  3. PIN1
  4. 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.

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PIN1 degrader-3

PIN1 degrader-3 Chemical Structure

CAS No. : 3101950-55-1

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PIN1 degrader-3 Related Antibodies

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Description

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[1].

IC50 & Target

Pin1

4.65 nM (IC50)

In Vitro

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.

PIN1 degrader-3 Related Antibodies

Western Blot Analysis[1]

Cell Line: BxPC3 cells, MIA PaCa-2 cells, KPC cells
Concentration: 0 μM, 0.5 μM, 1 μM, 3 μM, 5 μM, 10 μM, 15 μM
Incubation Time: 24 h
Result: Pin1 protein levels decreased in a dose-dependent manner in all three cell lines.
In Vivo

PIN1 degrader-3 (Compound 164B8; Compound H-3-V) (30-60 mg/kg, i.p., once a day, 5 days a week, for 2 weeks) can effectively inhibit KPC cell allograft tumors, reduce tumor burden, and directly lead to the degradation of Pin1 in tumor tissue, but high doses may cause hematological toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 30 mg/kg, 60 mg/kg
Administration: I.p., once a day, 5 days a week, for 2 weeks
Result: Tumor burden decreased significantly in a dose-dependent manner.
Mild anemia and moderate thrombocytopenia occurred in the 60 mg/kg group.
Molecular Weight

625.55

Formula

C31H34Cl2N6O4
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PIN1 degrader-3 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PIN1 degrader-33101950-55-1PIN1peptidylprolyl cis/trans isomerase, NIMA-interacting 1Pin1Pancreatic cancerCancer-associated fibroblastsCAFsInhibitorinhibitorinhibit

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