PARP

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.

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.

RBN-3143 is a potent inhibitor of NAD+-competitive catalytic PARP14 (IC50= 4 nM), which inhibits ADP-ribosylation mediated by PARP14 and stabilizes PARP14 in cell lines, demonstrating research potential for lung inflammation.

AZ9482 is a selective and potent inhibitor of PARP featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine. AZ9482 exhibits very potent activity of centrosome declustering with EC50 of < 18 nM in HeLa cells.

RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.

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.

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.

KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP, exhibiting anticancer activity. It is utilized in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine, and pancreatic cancers.

AZD5305 is a potent, selective and oral active PARP inhibitor.

RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.

Fluzoparib (SHR3162) is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours.

Lasiodin (Lasiokaurin) is a diterpene compound from the plant Camellia sinensis that inhibits the proliferation of NPC cells. Lasiodin has antioxidant, antitumor and antibacterial activities, induces cell cycle length and apoptosis, induces cell migration and invasion, and can be used in the study of nasopharyngeal carcinoma.

AZD-9574 is a selective inhibitor of PARP1 at the sites of SSBs. AZD-9574 exhibits anti-cancer activities and can be used in studies about HRD+ breast cancer and advanced solid malignancies.

Fucosterol is isolated from E. stolonifera with anti-diabetic, anti-adipogenic and anti-cancer activities. It regulates adipogenesis via modulation of PPARα and C EBPα expression.

Chlorin E6 (CE6) is a second-generation photosensitizer with antitumor activity when used in combination with irradiation. In a mouse model of implanted fibrosarcoma, Chlorin E6 (2.5-10 mg/kg, i.v., 50-200 J/cm2 irradiation) resulted in complete tumor disappearance after varying degrees of irradiation. Agents including Chlorin E6 were tested in a Phase I clinical study in patients with early superficial squamous cell carcinoma of bronchial origin with favorable results (40 mg/m2, IV, 100 J/cm2 laser irradiation). In a Phase II clinical trial in patients with early stage lung cancer, the same mode of administration resulted in a complete response in 82.9% of patients. Chlorin E6 has been investigated as a nanotechnology drug delivery tool.

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.

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.

Venadaparib (NOV140101) (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib is insensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSBs) and can be used in solid tumor research.

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.

Verbascoside (Kusaginin) is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.

Patritumab (U3-1287) is an anti-HER3 monoclonal antibody with potential antitumor activity and inhibits phosphorylation of EGFR, HER2, HER3, ERK, and AKT.Patritumab promotes apoptosis and inhibits proliferation in non-small cell lung cancer.

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).

PARPi-FL (PARPiFL) is a fluorescent PARP1 inhibitor used for imaging glioblastoma and detecting oral cancer.