PARP Inhibitor

MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC₅₀s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity.

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.

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.

ME0328 is a potent and selective ARTD3/PARP3 inhibitor with an IC₅₀ of 0.89±0.28 μM.

Sorafenib (Standard) (Bay 43-9006 (Standard)) is the analytical standard of Sorafenib (HY-10201). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) 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 induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with K_is of 5.2 nM and 2.9 nM in cell-free assays, respectively.

AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC₅₀s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC₅₀s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.

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.

Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer.

Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC₅₀ values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity.

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.

PARP7-IN-15 is an orally active and selective PARP7 inhibitor with an IC₅₀ of 0.56 nM. PARP7-IN-15 inhibits the enzymatic activity of PARP7 and induces anti-tumor activity against lung cancer in vivo. PARP7-IN-15 can be used for the research of lung cancer.

Nesuparib (JPI-547) is the orally active inhibitor for PARP 1/2 and Tankyrase 1/2 that inhibits tankyrases 1, tankyrases 2, and PARP 1 with IC₅₀s of 5, 1 and 2 nM, respectively. Nesuparib exhibits antitumor activity and can be used in research of advanced solid tumor.

7-Methylguanine is an orally active and competitive PARP-1 inhibitor with a K_i value of 61 μM. 7-Methylguanine is a metabolite of nucleic acids. 7-Methylguanine has anticancer activity against uterine sarcoma and colon adenocarcinoma. 7-Methylguanine is used as a probe for protein-DNA interactions.

MN-64 is a potent tankyrase 1 inhibitor, with IC₅₀s of 6 nM, 72 nM, 19.1 μM, and 39.4 μM for TNKS1, TNKS2, ARTD1 and ARTD2, respectively.

(8R,9S)-Talazoparib ((8R,9S)-BMN-673) is an enantiomer of Talazoparib. (8R,9S)-Talazoparib is an PARP1 inhibitor, with an IC₅₀ of 144 nM.

NU1025 is a potent PARP inhibitor with an IC₅₀ of 400 nM and a K_i of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer agents. NU1025 has anti-cancer and neuroprotective activity.