PARP Inhibitor

Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors.

PJ34 is a potent specific inhibitor of PARPl/2 with IC₅₀ of 110 nM and 86 nM, respectively.

Fucosterol is a sterol isolated from algae, seaweed or diatoms. Fucosterol exhibits various biological activities, including antioxidant, anti-adipogenic, blood cholesterol reducing, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via inhibition of PPARα and C/EBPα expression and can be used for anti-obesity agents development research.

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.

Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline shows strong anti-malarial effects (IC₅₀=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.

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.

Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC₅₀ of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC₅₀ of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors.

FeTMPyP is an orally active poly (ADP-ribose) polymerase (PARP) inhibitor. FeTMPyP inhibits cell death, nitrotyrosine formation, and depolarization of mitochondrial transmembrane potential. FeTMPyP reduces homocysteine-induced nitrosative stress and partially restores TFEB protein and mRNA levels. FeTMPyP improves functional and behavioral deficits caused by chronic constriction injury in rats. FeTMPyP alleviates acute cerebral infarction in a rat model of middle cerebral artery occlusion with mild hyperglycemia. FeTMPyP can be used in studies related to neuropathic pain, renal aging, ischemic penumbra, and hyperglycemic stroke.

Olaparib (Standard) is the analytical standard of Olaparib. This product is intended for research and analytical applications. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC₅₀s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.

Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC₅₀ of 0.57 nM for PARP1.

BGP-15 is a PARP inhibitor, with an IC₅₀ and a K_i of 120 and 57 μM, respectively.

PARP11 inhibitor ITK7 (ITK7) is a potent and selective PARP11 inhibitor. PARP11 inhibitor ITK7 can potently inhibit PARP11 with an IC₅₀ value of 14 nM. PARP11 inhibitor ITK7 can be used for the research of cellular localization.

Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling.

PJ34 hydrochloride is an inhibitor of PARP1/2 with IC₅₀ of 110 nM and 86 nM, respectively.

Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models.

N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib (HY-10162) containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a PARP inhibitor used for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4 (HY-141481). N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled with F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor.

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.

NSC 146109 hydrochloride (XI-011 hydrochloride) is a p53 activator and MDMX inhibitor. NSC 146109 hydrochloride inhibits MDMX gene transcription, downregulates MDMX mRNA and protein levels, stabilizes p53 and activates the transcriptional activity of p53. NSC 146109 hydrochloride induces cancer cell apoptosis (apoptosis) and inhibits the growth of transformed cells. NSC 146109 hydrochloride inhibits the growth of xenograft tumors. NSC 146109 hydrochloride can be used in research related to breast cancer and cervical cancer.

PARPi-FL (Olaparib-bodipy FL) is a small-molecule fluorescent inhibitor of PARP1 that can specifically bind to PARP1. PARPi-FL can be used as a fluorescent imaging agent for tumor detection, diagnosis, and surgical guidance.

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.