PARP Inhibitor

Niraparib hydrochloride (Standard) is the analytical standard of Niraparib hydrochloride (HY-10619A). This product is intended for research and analytical applications. Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

Rucaparib monocamsylate (Standard) is the analytical standard of Rucaparib monocamsylate (HY-102003). This product is intended for research and analytical applications. Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research.

Schisandronic acid is a triterpenoid antioxidant and anticancer agent extracted from Schisandra chinensis, which has potent cytotoxicity against human breast cancer cells, especially MCF-7. Schisandronic acid induces apoptosis and reduces cell viability in a time-dependent manner (MCF-7, IC50=8.06 μM). Schisandronic acid can upregulate active caspase-3 expression and cleave PARP, reduce the generation of reactive oxygen species and exhibit antioxidant effects.

3-Methoxybenzamide (Standard) is the analytical standard of 3-Methoxybenzamide. This product is intended for research and analytical applications. 3-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells. 3-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum).

Talazoparib (Standard) is the analytical standard of Talazoparib (HY-16106). This product is intended for research and analytical applications. Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with K_is of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity.

PJ34 (hydrochloride) (Standard) is the analytical standard of PJ34 (hydrochloride). This product is intended for research and analytical applications. PJ34 hydrochloride is an inhibitor of PARP1/2 with IC50 of 110 nM and 86 nM, respectively.

Niraparib (Standard) is the analytical standard of Niraparib. This product is intended for research and analytical applications. Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

1,5-Isoquinolinediol is a potent PARP inhibitor, with an IC50 of 0.18-0.37 μM. 1,5-Isoquinolinediol attenuates diabetes-induced NADPH oxidase-derived oxidative stress in retina.

Talazoparib-d₄ (BMN-673-d₄) is deuterium labeled Talazoparib. Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with K_is of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity.

Benzamide-d₅ (Benzenecarboxamide-d₅) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature.

BRCA1-IN-2 (Standard) is the analytical standard of BRCA1-IN-2 (HY-100862). This product is intended for research and analytical applications. BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions.

Benadrostin is a Poly(ADP-ribose) synthetase inhibitor with an IC₅₀ of 35 μM.

Rucaparib-d₈ (AG014699-d₈ ) is deuterium labeled Rucaparib. Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research.

3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects.

EB-47 dihydrochloride (Standard) is the analytical standard of EB-47 (dihydrochloride) (HY-108631). This product is intended for research and analytical applications. EB-47 dihydrochloride, 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. EB-47 mimics the substrate NAD+ and extends from the nicotinamide to the adenosine subsite.

Tankyrase-IN-5 (Compound 30f), an analogue of MSC2504877 (HY-123851), is a tankyrase TNKS1 and TNKS2 inhibitor with IC₅₀s of 2.3 nM and 7.9 nM, respectively.

PARP1-IN-19 is a PARP1 inhibitor with antitumor effects (CN107955001A; Embodiment 3).

NU1064 (dihydrochloride) is an inhibitor of PARP. NU1064 (dihydrochloride) potentiates the cytotoxicity of DNA-methylating agent (MTIC) in a concentration-dependent manner.

3-Aminobenzamide (Standard) is the analytical standard of 3-Aminobenzamide. This product is intended for research and analytical applications. 3-Aminobenzamide (PARP-IN-1) is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.

Pamiparib (Standard) is the analytical standard of Pamiparib. This product is intended for research and analytical applications. Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC₅₀ values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor.