2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Epigenetics
  4. PARP
  5. PARP1 Isoform
  6. PARP1 Degrader

PARP1 Degrader

PARP1 Degraders (12):

Cat. No. Product Name Effect Purity
  • HY-130646
    iVeliparib-AP6
    		Degrader
    iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) molecule designed based on Veliparib (HY-10129), which targets PARP1/2. The DC50s of iVeliparib-AP6 for inducing the degradation of PARP1 and PARP2 are 36 nM and 63 nM, respectively, and its IC50s are 69 nM and 21 nM, respectively. iVeliparib-AP6 contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder; it uses Thalidomide (HY-14658) as a ligand to recruit CRBN E3 ubiquitin ligase and exerts the PARP2 degradation mechanism.
  • HY-W973851
    2H-Indazole-7-carboxamide
    		Degrader
    2H-Indazole-7-carboxamide is a PARP1 ligand and can be used for the synthesis of PROTACs, such as PROTAC PARP1 degrader-1 (HY-158045).
  • HY-130644
    iRucaparib-AP6
    		Degrader 99.03%
    iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1.
  • HY-158045
    PROTAC PARP1 degrader-1
    		Degrader 99.86%
    PROTAC PARP1 degrader-1 is a PARP1 PROTAC degrader with a DC50 value of 252.5 nM. PROTAC PARP1 degrader-1, combined with Daunorubicin (HY-13062A), induces the accumulation of cytoplasmic DNA fragments, activates the cGAS/STING innate immune pathway, and remodels the tumor microenvironment. PROTAC PARP1 degrader-1 can be used in research related to breast cancer.
  • HY-130645
    iRucaparib-TP3
    		Degrader
    iRucaparib-TP3 is a selective PARP1 degrader (DC50=36 nM). iRucaparib-TP3 is promising for research of oncology (e.g., BRCA-mutated cancers) and neurodegenerative diseases.
  • HY-181720
    Antitumor agent-214
    		Degrader
    Antitumor agent-214 is a chalcone analogue with anti-tumor activity. Antitumor agent-214 induces cell cycle arrest and apoptosis in tumor cells, disrupts mitochondrial metabolism, and upregulates the expression of caspase 3, caspase 7 and caspase 9, downregulates PARP1. Antitumor agent-214 can be used for anti-tumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer.
  • HY-130647
    Vrucaparib-TP4
    		Degrader
    Vrucaparib-TP4 (Compound 9) is a PARP1 PROTAC-type degrader. Vrucaparib-TP4 promotes the ubiquitination and degradation of PARP1. Vrucaparib-TP4 can be used in the research of tumors.
  • HY-181967
    PROTAC PARP1 degrader-5
    		Degrader
    PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma.
  • HY-180276
    PARP1 degrader 1
    		Degrader
    PARP1 degrader 1 (Compound 2c) is a comparatively potent PARP1 HyT degrader (DC50: 618 nM for intracellular PARP-1). PARP1 degrader 1 is also a HyT-Olaparib (HY-10162) conjugate. PARP1 degrader 1 induces UPR/autophagy, thus facilitating the degradation of PARP-1. PARP1 Degrader 1 can be used in the research of cancer.
  • HY-181460
    PARP1 degrader-2
    		Degrader
    PARP1 degrader-2 (Compound 11e) is a potent, selective PARP1 HYT degrader (DC50: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)).
  • HY-168722
    PROTAC PARP1 degrader-3
    		Degrader
    PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader for PARP1 with a DC50 of 58.14 nM. PROTAC PARP1 degrader-3 exhibits cytotoxicity in cancer cell SW-620 and LOVO with IC50 of 1.63 μM and 2.84 μM. PROTAC PARP1 degrader-3 exhibits a synergistic effect with SN-38 (HY-13704) in BRCA-mutated colon cancer cell with a combination index (CI) of 0.487. (Blue: Ligand for E3 ligase Cereblon (HY-23095); Pink: Ligand for target protein (HY-10619); Black: Linker (HY-16872))
  • HY-178496
    DDO3602
    		Degrader
    DDO3602 is a PARP1 HEMTAC degradation agent mediated by HSP90. DDO3602 has good anti-tumor activity and tumor selectivity. DDO3602 induces G2/M phase arrest, DNA damage, and inhibits cell migration by degrading PARP1 in MCF-7 cells (IC50 = 187 nM). DDO3602 can be used for research on cancer such as breast cancer. (Pink: PARP1 Ligand (HY-75706); Blue: HSP90 Ligand (HY-179203); Black: Linker (HY-W015300))