PROTAC PIN1 degrader-1
Based on 1 Customer Validation
PROTAC PIN1 degrader-1 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.
- Purity: 97.39%
- CAS No.: 3038591-59-9
- Formula: C51H52N10O7
- Molecular Weight:917.02
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
PIN1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | GI50 |
>30 μM
Compound: D4
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Antiproliferative activity against human Huh-7 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human Huh-7 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
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[PMID: 39229909] |
| MDA-MB-468 | GI50 |
>30 μM
Compound: D4
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Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
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[PMID: 39229909] |
| PANC-1 | GI50 |
>30 μM
Compound: D4
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Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
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[PMID: 39229909] |
PROTAC PIN1 degrader-1 (compound D4) (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) 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.
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Cell Line:MDA-MB-468, PANC-1, and Huh-7 human cancer cells
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Concentration:serial concentrations
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Incubation Time:96 h
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Result:Exhibited no meaningful antiproliferative activity, with a GI50 > 30 μM in all three tested cancer cell lines.
Chemical Information
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CAS No. 3038591-59-9
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Appearance Solid
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Molecular Weight 917.02
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Formula C51H52N10O7
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (109.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0905 mL | 5.4524 mL | 10.9049 mL | 27.2622 mL |
| 5 mM | 0.2181 mL | 1.0905 mL | 2.1810 mL | 5.4524 mL | |
| 10 mM | 0.1090 mL | 0.5452 mL | 1.0905 mL | 2.7262 mL | |
| 15 mM | 0.0727 mL | 0.3635 mL | 0.7270 mL | 1.8175 mL | |
| 20 mM | 0.0545 mL | 0.2726 mL | 0.5452 mL | 1.3631 mL | |
| 25 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0905 mL | |
| 30 mM | 0.0363 mL | 0.1817 mL | 0.3635 mL | 0.9087 mL | |
| 40 mM | 0.0273 mL | 0.1363 mL | 0.2726 mL | 0.6816 mL | |
| 50 mM | 0.0218 mL | 0.1090 mL | 0.2181 mL | 0.5452 mL | |
| 60 mM | 0.0182 mL | 0.0909 mL | 0.1817 mL | 0.4544 mL | |
| 80 mM | 0.0136 mL | 0.0682 mL | 0.1363 mL | 0.3408 mL | |
| 100 mM | 0.0109 mL | 0.0545 mL | 0.1090 mL | 0.2726 mL |
PROTAC PIN1 degrader-1 Related Classifications
HY-168037 Related Classifications
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