PARP

Olaparib (KU0059436) is a small molecule inhibitor of PARP1 PARP2 (IC50=5 1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP, exhibiting anticancer activity. It is utilized in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine, and pancreatic cancers.

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8 2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1 2 (Kis: 1.2 0.85 nM).

XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription.

Fucosterol is isolated from E. stolonifera with anti-diabetic, anti-adipogenic and anti-cancer activities. It regulates adipogenesis via modulation of PPARα and C EBPα expression.

RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.

Paris saponin VII (Dioscini) shows inhibitory effects on cell proliferation.

RBN012759 inhibits PARP14 protein with an IC50 value of 0.003 μM and is more than 300-fold selective over all PARP family members.[2]

AZD5305 is a potent, selective and oral active PARP inhibitor.

Rucaparib (PF-01367338) is a PARP protein inhibitor (PARP-1 Ki=1.4 nM) and hexose hexose-6-phosphate dehydrogenase (H6PD) inhibitor with oral activity. Rucaparib exhibits antitumor activity, with activity against desmoplasia-resistant prostate cancer (CRPC).

Fluzoparib (SHR3162) is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours.

Veliparib (ABT-888) (ABT-888) is an orally bioavailable inhibitor of PARP (Kis: 5.2 2.9 nM for PARP1 2). It enhances apoptosis and autophagy.

RBN-3143 is a potent inhibitor of NAD+-competitive catalytic PARP14 (IC50= 4 nM), which inhibits ADP-ribosylation mediated by PARP14 and stabilizes PARP14 in cell lines, demonstrating research potential for lung inflammation.

Lasiodin (Lasiokaurin) is a diterpene compound from the plant Camellia sinensis that inhibits the proliferation of NPC cells. Lasiodin has antioxidant, antitumor and antibacterial activities, induces cell cycle length and apoptosis, induces cell migration and invasion, and can be used in the study of nasopharyngeal carcinoma.

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

Verbascoside (Kusaginin) is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.

E7016 (GPI 21016) is an orally available PARP inhibitor that inhibits DNA repair and enhances tumor cell radiosensitivity both in vitro and in vivo.

AZD-9574 is a selective inhibitor of PARP1 at the sites of SSBs. AZD-9574 exhibits anti-cancer activities and can be used in studies about HRD+ breast cancer and advanced solid malignancies.

Nesuparib (JPI-547/OCN-201) is a potent PARP inhibitor with inhibitory effects on PARP and TNKS1.Nesuparib has antitumor activity and can be used in the treatment of tumors, endocrine and metabolic disorders, genitourinary disorders, and can be used in the study of neuropathic pain, neurodegenerative disorders, and cardiovascular diseases.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax Bcl-2, activating caspases as well as cleaving PARP.

Zingiberen newsaponin is a steroidal saponin from Dioscorea zingiberensis.

Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM 2.1 nM) is a selective PARP1 PARP2 inhibitor.

PJ34 hydrochloride (PJ34 HCl) is a potent specific inhibitor of PARPl 2.

Venadaparib (NOV140101) (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib is insensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSBs) and can be used in solid tumor research.

AG14361 is an effective inhibitor of PARP1 (Ki<5 nM).

Senaparib (IMP4297) is a novel highly potent and selective oral PARP1/2 inhibitor with strong antitumor activity.

EB-47 mimics the substrate NAD+ and extends from the nicotinamide to the adenosine subsite.EB-47, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM.

Simmiparib (SMOCL-9112) is a novel and potent PARP1 and PARP2 inhibitor, a derivative of Olaparib.Simmiparib induces DNA double-strand breaks (DSBs) and cell cycle arrest in homologous recombination repair (HR)-deficient cells, thereby contributing to apoptosis.Simmiparib has been used for study Parkinson's disease, Alzheimer's disease, breast cancer, and melanoma.

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.

Polyporenic acid C shows inhibitory activity against human collagenase.

NVP-TNKS656 (TNKS656) is a highly potent, selective, and orally active TNKS2 inhibitor.

E7449 (UNII-9X5A2QIA7C) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ～50 and ～50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.

Myristicin (Myristicine) is a natural product found in spices and umbelliferous plants. Myristicin has anti-cholinergic, Antibacterial, and hepatoprotective effects, it also has anti-inflammatory properties related with its inhibition of NO, cytokines,chemokines, and growth factors in dsRNA-stimulated macrophages via the calcium pathway. Myristicin can induce Apoptosis as characterised by alterations in the mitochondrial membrane potential, cytochrome c release, Caspase-3 activation, PARP-cleavage and DNA fragmentation.

3',4'-Dimethoxyflavone is a standard flavonoid compound with numerous medicinal activities.

Rucaparib Phosphate (PF-01367338 phosphate) is an inhibitor of PARP (Ki: 1.4 nM for PARP1) that is used in clinical therapy to sensitize cancer cells to chemotherapy.

ME0328 is a potent, selective PARP inhibitor with an IC50 of 0.89 μM for PARP3, showing approximately 7-fold selectivity over PARP1.

Ayanin has vasorelaxant activity, it also may have the potential for use in treating allergic asthma.The IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethylether) is 2.2microM for inhibiting interleukin (IL)-4 production from purified basophils.

RK-287107 is an effective and specific inhibitor of tankyrase (IC50s: 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively).

Phytic acid dipotassium salt is an endogenous metabolite that inhibits β-secretase 1 (BACE1).

Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor with IC50 values of 0.9 nM for PARP1 and 0.5 nM for PARP2. It exhibits strong PARP trapping, has the capability to penetrate the brain, and is used for researching various cancers, including solid tumors.

AZ9482 is a selective and potent inhibitor of PARP featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine. AZ9482 exhibits very potent activity of centrosome declustering with EC50 of < 18 nM in HeLa cells.

WIKI4 is a potent inhibitor of Wnt β-catenin signaling and tankyrase 2 (TNKS2).

Iniparib (BSI-201) (BSI-201) , a PARP1 inhibitor, exhibits potency in triple-negative breast Y (TNBC).

5,7,4'-Trimethoxyflavone (4',5,7-Trimethoxyflavone) is isolated from Kaempferia parviflora (KP) which is a medicinal plant from Thailand.

AZD2461 is a novel PARP inhibitor.

SK-575 is a degradation agent targeting protein-hydrolyzed PARP1 chimera with anticancer and antitumor activity.SK-575 effectively inhibits the growth of cancer cells harboring BRCA1/2 mutations and selectively induces PARP1 degradation in cancer cells.

PARP1-IN-5 dihydrochloride is an orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.