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Cat. No.: HY-168037A

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PROTAC PIN1 degrader-1 TFA

PROTAC PIN1 degrader-1 TFA is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer.
(Pink: PIN1 ligand (HY-168038); Blue: Cereblon ligand (HY-14658); Black: linker).

For research use only. We do not sell to patients.

Formula: C₅₃H₅₃F₃N₁₀O₉
Molecular Weight:1031.04

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC PIN1 degrader-1 TFA Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC PIN1 degrader-1 TFA is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer^[1]. (Pink: PIN1 ligand (HY-168038); Blue: Cereblon ligand (HY-14658); Black: linker).

In Vitro

PROTAC PIN1 degrader-1 (compound D4) TFA (24 h) potently and selectively induces on-target degradation of PIN1 protein in MDA-MB-468 cells with a DC₅₀ of 18 nM and maximum degradation of 92.52%^[1].
PROTAC PIN1 degrader-1 (96 h) TFA does not exhibit significant antiproliferative activity in MDA-MB-468, PANC-1, or Huh-7 cancer cells, with a GI₅₀ greater than 30 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-468, PANC-1, and Huh-7 human cancer cells
Concentration:

serial concentrations
Incubation Time:

96 h
Result:

Exhibited no meaningful antiproliferative activity, with a GI₅₀ > 30 μM in all three tested cancer cell lines.

Chemical Information

Molecular Weight 1031.04
Formula C₅₃H₅₃F₃N₁₀O₉
SMILES

CC1=CC=CN=C1C2(CC2)C(NC(CC(N=N3)=CN3C(C=C4)=CC=C4C(C=C5)=CC=C5C#N)C(NC(CC6)CCN6CCCCCOC7=CC=CC(C8=O)=C7C(N8C(CC9)C(NC9=O)=O)=O)=O)=O.O=C(O)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Liu C, et al. Re-Evaluating PIN1 as a Therapeutic Target in Oncology Using Neutral Inhibitors and PROTACs. J Med Chem. 2024;67(17):15780-15795. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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