PARP1 PROTAC 180055
Based on 1 publication(s) in Google Scholar
PARP1 PROTAC 180055 is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells.
(Pink: PARP-1 ligand (HY-10617A); Blue: VHL ligand (HY-125845); Black: linker (HY-W014787)).
For research use only. We do not sell to patients.
- Purity: 98.90%
- Formula: C51H62FN7O6S
- Molecular Weight:920.14
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
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HY-L004
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Epigenetics Compound Library
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Anti-Cancer Compound Library
HY-L025
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Anti-Breast Cancer Compound Library
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Anti-Pancreatic Cancer Compound Library
HY-L077
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PROTAC Library
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Anti-Ovarian Cancer Compound Library
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Publications Citing Use of MedChemExpress (MCE) PARP1 PROTAC 180055
MoreAll PROTACs Isoforms
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Biological Activity
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PARP1 |
PARP1 PROTAC 180055 (1-10 μM, 24-48 h) protects T47D and MOLT4 cells from gene toxicity-induced cell death[1].
PARP1 PROTAC 180055 (10 μM, 3-6 days) induces substantial cytotoxic effects in MOLT4 cells with BRCA1 mutation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cardiomyocyte cell lines lacking BRCA1 mutations and MOLT4 cells
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Concentration:1, 5, 10 μM
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Incubation Time:144 h
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Result:Showed minimal cytotoxicity in cardiomyocyte cell lines lacking BRCA1 mutations.
Induced substantial cytotoxic effects in MOLT4 cells with BRCA1 mutation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-week-old NSG mice (injected 8 × 106 MOLT4 cells or 4 × 106 A2780)[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection (i.p.), 16 days
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Result:Exhibited a noticeable reduction in tumor size compared to the control group.
Effectively degraded PARP1 in tumors derived from MOLT4-xenografted mice.
Showed no significant alterations in neutrophil count, lymphocyte count or glutamic-pyruvic transaminase levels.
Chemical Information
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Appearance Solid
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Molecular Weight 920.14
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Formula C51H62FN7O6S
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Color Light yellow to yellow
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SMILES
O=C1NCCC2=C(C3=CC=C(CN(C)C(CCCCCCCCC(N[C@H](C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)C(C)(C)C)=O)=O)C=C3)NC7=CC(F)=CC1=C72
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 100 mg/mL (108.68 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 (protect from light). 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 (protect from light). 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 (protect from light). 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 | 1.0868 mL | 5.4340 mL | 10.8679 mL | 27.1698 mL |
| 5 mM | 0.2174 mL | 1.0868 mL | 2.1736 mL | 5.4340 mL | |
| 10 mM | 0.1087 mL | 0.5434 mL | 1.0868 mL | 2.7170 mL | |
| 15 mM | 0.0725 mL | 0.3623 mL | 0.7245 mL | 1.8113 mL | |
| 20 mM | 0.0543 mL | 0.2717 mL | 0.5434 mL | 1.3585 mL | |
| 25 mM | 0.0435 mL | 0.2174 mL | 0.4347 mL | 1.0868 mL | |
| 30 mM | 0.0362 mL | 0.1811 mL | 0.3623 mL | 0.9057 mL | |
| 40 mM | 0.0272 mL | 0.1358 mL | 0.2717 mL | 0.6792 mL | |
| 50 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5434 mL | |
| 60 mM | 0.0181 mL | 0.0906 mL | 0.1811 mL | 0.4528 mL | |
| 80 mM | 0.0136 mL | 0.0679 mL | 0.1358 mL | 0.3396 mL | |
| 100 mM | 0.0109 mL | 0.0543 mL | 0.1087 mL | 0.2717 mL |
PARP1 PROTAC 180055 Related Classifications
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