poly(adp-ribose)

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.

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.

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).

Niraparib metabolite M1 (Niraparib carboxylic acid metabolite M1) is the carboxylic acid metabolite of Niraparib. Niraparib is a novel poly (ADP-ribose) polymerase (PARP) inhibitor used in cancer research.

CEP-9722 is an orally active, selective and potent inhibitor of poly (ADP-ribose) polymerase-1 PARP-1 and poly (ADP-ribose) polymerase-12 PARP-2, with anticancer activity, and can be used for the study of ovarian cancer.

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

4-Aminobenzamide is an inhibitor of poly (ADP-ribose) polymerase (PADPRP) and has been studied for cytotoxic effects.

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.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Vanillyl Alcohol (3-Methoxy-4-hydroxybenzyl alcohol) possesses anti-angiogenic, anticonvulsive, anti-inflammatory, anti-oxidant, neuroprotective, and anti-nociceptive activities. Vanillyl alcohol can effectively inhibit the cytotoxicity and improved cell viability in 1-methyl-4-phenylpyridinium (MPP+)-induced MN9D dopaminergic cells, it also can attenuate the elevation of reactive oxygen species (ROS) levels, decrease in the Bax Bcl-2 ratio and poly (ADP-ribose) polymerase proteolysis.

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.

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).

3-Aminobenzamide (PARP-IN-1) is a potent PARP inhibitor (IC50 < 50 nM in CHO cells) and mediates oxidant-induced myocyte dysfunction during reperfusion.

Benzamide (Amid kyseliny benzoove), an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid.

Picolinamide (Picolinoylamide) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.

3-Methoxybenzamide (3-MBA) is a competitive inhibitor of poly(ADP-ribose) synthetase.

4'-Methoxychalcone with a variety of pharmacological activities, such as anti-tumor and anti-inflammatory activities.

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.

Niraparib metabolite M1 HCl is the active metabolite of Niraparib, as a novel targeted ADP ribose polymerase (PARP) inhibitor, it can competitively inhibit PARP1 and PARP2 to block the DNA repair mechanism of tumor cells and thus effectively inhibit the growth and proliferation, which is commonly used in the study of ovarian cancer, fallopian tube cancer and primary peritoneal cancer, and is commonly used in the study of ovarian, fallopian tube and primary peritoneal cancers.

PARPYnD is a potent photoaffinity probe for poly(ADP-ribose) polymerase (PARP) (IC50 values for PARP2, PARP1 and PARP6 are 6, 38 and 230 nM, respectively). PARPYnD labels PARP1 and PARP2 in the cell when an N3 functionalized fluorescent probe is attached and can inhibit isolated PARP6.

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.

AZD2461 is a novel PARP inhibitor.

COH29 (RNR Inhibitor COH29) is an orally available, aromatically substituted thiazole and human ribonucleotide reductase (RNR) inhibitor with potential antineoplastic activity. COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail, decreasing the pool of deoxyribonucleotide triphosphates needed for DNA synthesis, leading to cell cycle arrest and growth inhibition. It may also inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, preventing DNA repair, causing accumulation of DNA breaks, and inducing apoptosis.

Ethacridine lactate (Acrinol) is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor.