PROTAC PARP1 degrader-3
PROTAC PARP1 degrader-3 is a PARP1 PROTAC degrader with a DC50 of 58.14 nM. PROTAC PARP1 degrader-3 promotes the ubiquitination and degradation of PARP1 via the ubiquitin-proteasome system. PROTAC PARP1 degrader-3 acts synergistically with SN-38 (HY-13704) to inhibit colorectal cancer. PROTAC PARP1 degrader-3 can be used in studies related to colorectal cancer.
(Pink: PARP-1 ligand (HY-10619); Blue: Cereblon ligand (HY-23095); Black: linker (HY-168723)).
For research use only. We do not sell to patients.
- Formula: C52H65N9O5
- Molecular Weight:896.13
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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PARP-1 58.14 nM (DC50) |
Cereblon |
PROTAC PARP1 degrader-3 (Compound C6) (0.01-10 μM; 0-48 h) efficiently and selectively degrades PARP1 in HCT-116 colorectal cancer cells via the ubiquitin-proteasome system, with a DC50 of 58.14 nM and a maximum degradation rate of 96.55%[1].
PROTAC PARP1 degrader-3 (0.01-10 μM; 24 h) potently degrades PARP1 in RKO colorectal cancer cells, with a DC50 of 160.56 nM and a maximum degradation rate of 95.87%[1].
PROTAC PARP1 degrader-3 potently inhibits the activity of colorectal cancer cells SW-620 and LOVO, with IC50 values of 1.63 μM and 2.84 μM, respectively[1].
PROTAC PARP1 degrader-3 (4 μM) acts synergistically with SN-38 (HY-13704) to inhibit the viability of HCT-116 colorectal cancer cells, with a maximum combination index of 0.487[1].
PROTAC PARP1 degrader-3 forms a stable PARP1-C6-CRBN ternary complex through multiple favorable binding interactions, which supports its potent PARP1 degradation activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 colorectal cancer cells
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Concentration:1 μM; 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; 1 μM (with inhibitor pretreatment)
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Incubation Time:0, 4, 8, 12, 24, 48 h; 24 h
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Result:Induced rapid PARP1 degradation, with protein levels starting to decline at 4 hours post-treatment.
Achieved a DC50 of 58.14 nM and a maximum degradation rate (Dmax) of 96.55% in HCT-116 cells.
Showed a "hook effect" at 10 μM and 50 μM concentrations.
Induced much weaker degradation of PARP2, with a DC50 of 19.10 μM and Dmax of 84.84%.
Had its PARP1 degradation activity effectively inhibited by pretreatment with MG132, MLN4924, or Thalidomide.
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Cell Line:RKO colorectal cancer cells
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
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Incubation Time:24 h
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Result:Degraded PARP1 in RKO cells with a DC50 of 160.56 nM and a Dmax of 95.87%.
Chemical Information
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Molecular Weight 896.13
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Formula C52H65N9O5
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SMILES
NC(C1=CC=CC2=CN(C3=CC=C([C@H]4CN(CCC5CCN(CCC6CCN(CC7CCN(C8=CC9=C(C(N(C%10CCC(NC%10=O)=O)C9=O)=O)C=C8)CC7)CC6)CC5)CCC4)C=C3)N=C21)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC PARP1 degrader-3 Related Classifications
HY-168722 Related Classifications
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