PARP Inhibitor

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.

UPF-1035 is a selective PARP-2 inhibitor with an IC₅₀ value of 0.15 μM. UPF-1035 increases CA1 pyramidal cell loss in hippocampal and has neuroprotective activity.

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.

Veliparib (dihydrochloride) (Standard) is the analytical standard of Veliparib (dihydrochloride) (HY-10130). This product is intended for research and analytical applications. Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.

BYK204165 (Standard) is the analytical standard of BYK204165 (HY-108632). This product is intended for research and analytical applications. BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC₅₀ of 7.35 (pK_i=7.05), and murine PARP-2 (mPARP-2) with a pIC₅₀ of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1.

Benzamide (Standard) is the analytical standard of Benzamide. This product is intended for research and analytical applications. 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.

TNKS-IN-3 (Compound 6) is a TNKS2 inhibitor (K_i: 8.5 nM). TNKS-IN-3 has good activity (IC₅₀: 71 nM) and can effectively inhibit the WNT/β-catenin signaling pathway. TNKS-IN-3 can be used in the research of diseases such as cancer and fibrosis.

EXQ-2d is the inhibitor for tankyrase and inhibits TNKS1 and TNKS2 with an IC₅₀ of 48.8 nM and 13.8 nM (pIC₅₀=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC₅₀ of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI₅₀ of 4.9 μM and 77 μM.

5-AIQ (5-Aminoisoquinolin-1-one) is a PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver.

Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC₅₀s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase.

BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC₅₀ and K_i of 0.53 μM and 0.71 μM, respecrively.