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

PARP Degrader

PARP Isoform Comparison

PARP Degraders (19):

Cat. No. Product Name Effect Purity
  • HY-183013
    PROTAC PARP2 degrader-1
    		Degrader
    PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer.
  • 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-173679
    RBN012811
    		Degrader 98.79%
    RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD+ site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections.
  • HY-114324A
    rel-PROTAC PARP1 degrader
    		Degrader 98.99%
    rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. rel-PROTAC PARP1 degrader induces significant PARP1 cleavage and programmed cell death.
  • 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-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-168724
    Thalidomide-piperidine-C-Pip-C2-Pip-C2-OH
    		Degrader
    Thalidomide-piperidine-C-Pip-C2-Pip-C2-OH (Compound C6) is a conjugate of the linker and E3 ligase ligand, that can be used in synthesis of PROTAC PARP1 degrader-30 (HY-168722).
  • 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-173437
    CW-2
    		Degrader
    CW-2 is a PARP1 PROTAC degrader. CW-2 has potent antiproliferative effects against MDA-MB-231 cells (IC50 = 0.72 μM) and CDDP-resistant cells (A549/CDDP: IC50 = 3.52 μM). CW-2 has synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts antitumor effects by inducing DNA damage, impairing DNA repair, and activating mitochondria-dependent apoptosis (Pink: PARP1 ligand (HY-173441); Blue: E3 CRBN ligand (HY-173439); Black: linker (HY-173440)).
  • 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-116692
    Apoptosis inducer 34
    		Degrader 99.9%
    Apoptosis inducer 34 (Compound 4) is a small molecule compound that induces apoptosis by directly activating the intrinsic apoptotic pathway. Apoptosis inducer 34 promotes Apaf-1 oligomerization to form mature apoptosomes, thereby activating caspase-9 and caspase-3. It significantly activates the apoptotic pathway in Jurkat cells by enhancing the cytochrome c-dependent apoptotic signaling pathway, inducing PARP cleavage and chromosomal DNA fragmentation. Furthermore, Apoptosis inducer 34 exhibits low toxicity to normal cells, demonstrating potential for selective targeting of cancer cells. Apoptosis inducer 34 is a promising candidate for studying cancer related to apoptotic pathways.
  • 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))
  • HY-164306
    PROTAC PARP1 degrader-2
    		Degrader
    PROTAC PARP1 degrader-2 (Compound 72) is a PROTAC degrader for PARP with a DC50<10 nM in MDA-MB-231 cell. PROTAC PARP1 degrader-2 inhibits the cell viability of MDA-MB-436 with an IC50 <100 nM. (Blue: ligand for target protein (HY-160937); Pink: ligand for E3 ligase (HY-W998262))