parp

PARP1-IN-8 (N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide) is an effective inhibito of PARP1 (IC50 = 97 nM).

PARP/PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

PARP-1/HDAC-IN-1 is an effective dual inhibitor of PARP-1 and HDAC6, with IC50 values of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 exhibits anti-cancer, anti-migration, and anti-angiogenesis activities.

ARTD10/PARP10-IN-1 is a potent PARP inhibitor of the mono-ADP ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly ADP-ribose polymerase-1 (ARTD1/PARP1), with potential anticancer and antitumour activity for the study of prostate and breast cancers.

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.

BGP-15 (BGP-15 2HCl) is a PARP inhibitor with protecting effect after ischemia-reperfusion injury.

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, 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.

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

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.

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.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

MN-64 is a tankyrases inhibitor, showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition.

UPF 1069 is a specific PARP2 inhibitor ( IC50: 0.3 μM). It is ~27-fold selective against PARP1.

1, 5-Isoquinolinediol is an inhibitor of poly(ADP-ribose) synthetase (PARP1; IC50: 0.39 μM). The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis. 1, 5-Isoquinolinediol has been used to study the role of

Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid exhibiting anti-inflammatory and anti-cancer activities and can enhance the activation of p38 MAPK.