PROTAC PARP1 degrader
Based on 1 Customer Validation
PROTAC PARP1 degrader is a PROTAC PARP1 degrader. PROTAC PARP1 degrader mediates the interaction between PARP1 and MDM2 E3 ubiquitin ligase, thereby inducing ubiquitination of PARP1 and subsequent proteasome-mediated degradation. PROTAC PARP1 degrader selectively inhibits the growth of breast cancer cells. PROTAC PARP1 degrader induces cell apoptosis by activating caspase-3 and phosphatidylserine externalization. PROTAC PARP1 degrader can be used in the research of triple-negative breast cancer.
(Pink: PARP1 ligand (HY-171543); Blue: MDM2 ligand (HY-128836); Black: linker (HY-128834)).
For research use only. We do not sell to patients.
- Purity: 99.74%
- CAS No.: 2369022-68-2
- Formula: C58H63Cl2N11O10
- Molecular Weight:1145.09
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Storage:
-20°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
All PROTACs Isoforms
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Biological Activity
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PARP1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
8.45 μM
Compound: 56
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
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[PMID: 36512711] |
PROTAC PARP1 degrader (compound 3) (4-10 μM; 24 h) induces concentration-dependent cleavage of PARP1 in MDA-MB-231 cells, and this effect depends on specific binding to PARP1 and MDM2 as well as proteasome function[1].
PROTAC PARP1 degrader (10 μM; 24 h) induces apoptosis in MDA-MB-231 cells, which is evidenced by increased phosphatidylserine externalization and production of cleaved caspase-3 after treatment with 10 μM for 24 h[1].
PROTAC PARP1 degrader (10 μM; 24-48 h) potently inhibits the viability of MDA-MB-231 cells, with an IC50 of 8.45 μM at 24 h and 6.12 μM at 48 h. Its potency in this cell line is 5-fold higher than that of the PARP1 inhibitors niraparib, olaparib and veliparib[1].
PROTAC PARP1 degrader (100 μM; 48 h) shows high selectivity toward MDA-MB-231 cells; even after treatment at 100 μM for 48 h, it exhibits only extremely low or no cytotoxicity, with no PARP1 degradation, in MCF10A, BEAS-2B, HeLa and HepG2 cells[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-231 triple negative breast cancer cells
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Concentration:4, 6, 8, 10 μM (main assay); 10 μM (competition experiments)
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Incubation Time:24 h (main assay; competition experiments); 4 h (MLN4924 pre-treatment)
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Result:Reduced PARP1 protein levels to 98%, 38%, 30%, and 20% of control levels respectively.
Induced PARP1 cleavage that was abolished by pre-treatment with 50 μM niraparib.
Induced PARP1 cleavage that was partially blocked by pre-treatment with 20 μM nutlin-3.
Induced PARP1 cleavage that was effectively blocked by pre-treatment with 1 μM MLN4924 for 4 h.
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Cell Line:MDA-MB-231 triple negative breast cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Increased annexin V-positive cells, showing elevated dot intensity in the Q2 region of the annexin V/PI dot plot, indicating enhanced phosphatidylserine externalization.
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Cell Line:MDA-MB-231 triple negative breast cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced detectable cleavage of caspase-3, a key effector of apoptotic cell death.
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Cell Line:MCF10A breast epithelial cells, BEAS-2B bronchial epithelial cells, HeLa cells, HepG2 cells
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Concentration:100 μM
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Incubation Time:48 h
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Result:Resulted in 40% inhibition or no toxic effect on cell viability in MCF10A, BEAS-2B, HeLa, and HepG2 cells after 48 h treatment.
Caused no significant change in PARP1 protein levels detected via immunoblot in these cell lines after treatment.
Chemical Information
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CAS No. 2369022-68-2
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Appearance Solid
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Molecular Weight 1145.09
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Formula C58H63Cl2N11O10
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Color White to off-white
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SMILES
O=C(CN(C(N1C(C2=CC=C(OC)C=C2OC(C)C)=N[C@H](C3=CC=C(Cl)C=C3)[C@@H]1C4=CC=C(Cl)C=C4)=O)CC5)N5CC(NCCOCCOCCOCCOCCN6N=NC(C7=CC=C(N8N=C(C(C(N)=O)=CC=C9)C9=C8)C=C7)=C6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (87.33 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 (275 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 | 0.8733 mL | 4.3665 mL | 8.7329 mL | 21.8323 mL |
| 5 mM | 0.1747 mL | 0.8733 mL | 1.7466 mL | 4.3665 mL | |
| 10 mM | 0.0873 mL | 0.4366 mL | 0.8733 mL | 2.1832 mL | |
| 15 mM | 0.0582 mL | 0.2911 mL | 0.5822 mL | 1.4555 mL | |
| 20 mM | 0.0437 mL | 0.2183 mL | 0.4366 mL | 1.0916 mL | |
| 25 mM | 0.0349 mL | 0.1747 mL | 0.3493 mL | 0.8733 mL | |
| 30 mM | 0.0291 mL | 0.1455 mL | 0.2911 mL | 0.7277 mL | |
| 40 mM | 0.0218 mL | 0.1092 mL | 0.2183 mL | 0.5458 mL | |
| 50 mM | 0.0175 mL | 0.0873 mL | 0.1747 mL | 0.4366 mL | |
| 60 mM | 0.0146 mL | 0.0728 mL | 0.1455 mL | 0.3639 mL | |
| 80 mM | 0.0109 mL | 0.0546 mL | 0.1092 mL | 0.2729 mL |
PROTAC PARP1 degrader Related Classifications
HY-114324 Related Classifications
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