PARP Inhibitor

AZD5335 is an ADC targeting FRα, with an IC₅₀ of 10.6 nM against human FRα. AZD5335 specifically binds to FRα, mediates internalization and trafficking to lysosomal compartments, while delivering a topoisomerase I inhibitor payload that traps TOP1-DNA cleavage complexes. AZD5335 induces DNA damage response via the ATR, ATM, Chk1 and Chk2 signaling pathways, and increases the levels of phosphorylated KAP1, phosphorylated RPA, phosphorylated γH2AX, as well as PARP cleavage. AZD5335 exhibits bystander cytotoxicity against FRα-negative cells co-cultured with FRα-expressing cells. AZD5335 induces potent and durable responses and complete regression in ovarian cancer models, including models with low FRα expression and models resistant to Elahere, with enhanced efficacy when combined with Carboplatin, Bevacizumab or poly (ADP-ribose) polymerase inhibitors. AZD5335 can be used for ovarian cancer research.

PJ34 (Standard) is the analytical standard of PJ34. This product is intended for research and analytical applications. PJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.

Talazoparib tosylate (Standard) is the analytical standard of Talazoparib tosylate (HY-108413). This product is intended for research and analytical applications. Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC₅₀ of 0.57 nM for PARP1.

Niraparib Tosylate (Standard) is the analytical standard of Niraparib Tosylate (HY-10619B). This product is intended for research and analytical applications. Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC₅₀ of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

Homoeriodictyol (Standard) is the analytical standard of Homoeriodictyol (HY-N8210). This product is intended for research and analytical applications. Homoeriodictyol is an orally active, bitter-tasting flavanone that can penetrate the blood-brain barrier. Homoeriodictyol enhances synaptic-related protein expression through NCOA4-mediated ferritin autophagy. Homoeriodictyol improves memory impairment in mice by inhibiting the NLRP3 inflammasome. Homoeriodictyol protects human endothelial cells from oxidative damage by activating Nrf2 and inhibiting mitochondrial dysfunction. Homoeriodictyol enhances ROS activity and induces apoptosis, exhibiting anticancer effects. Homoeriodictyol inhibits the survival and migration of androgen-resistant prostate cancer cells in vitro. Homoeriodictyol exerts antinociceptive activity in mice in vivo.

INO-1001 mesylate is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 mesylate is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death. INO-1001 mesylate has anti-tumor effects.

Saruparib (Standard) is the analytical standard of Saruparib (HY-132167). This product is intended for research and analytical applications. Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC₅₀ values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair.

CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC₅₀: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560).

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.

ST7710AA1 (compound 1l) is a potent PARP-1 inhibitor with an IC₅₀ value of 0.07 µM. ST7710AA1 shows an antiproliferative activity. ST7710AA1 shows anticancer activity.

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).

Orsellinic acid (Standard) is an analytical standard of Orsellinic acid (HY-N3126). This product is intended for research and analytical applications. Orsellinic acid is a Benzoic acid (HY-N0216) derivative. Orsellinic acid can be isolated from Chaetomium globosum endophytic on Ephedra fasciculata (Mormon tea). Orsellinic acid blocks PAF-mediated Apoptosis, inhibits caspase-3/7 activation, and PARP cleavage. Orsellinic acid can be used in research of neurons and various tumors (non-small cell lung cancer, breast cancer, neuroblastoma, pancreatic cancer).

8-Chloroquinazolin-4-ol is a poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor with an IC₅₀ value of 5.65 μM. 8-Chloroquinazolin-4-ol can be used in cancer-related research.

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.

Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A₁ and hA_2A, with K_i of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC₅₀ of 0.311 and 5.5 μM.

Sorafenib (tosylate) (Standard) (Bay 43-9006 (tosylate) (Standard)) is the analytical standard of Sorafenib (tosylate) (HY-10201A). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.