ATM/ATR Inhibitor

Berzosertib (Standard) is the analytical standard of Berzosertib (HY-13902). This product is intended for research and analytical applications. Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR K_inase inhibitor. Berzosertib blocks ATR K_inase activity, abrogates G₂/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer.

CBP-93872 is a G2 checkpoint inhibitor and a chemosensitizer. CBP-93872 specifically inhibits DNA double-strand break (DSB)-dependent, Nbs1-mediated ATR activation, without directly inhibiting ATR kinase activity or affecting ATR activation induced by other types of DNA damage; meanwhile, it suppresses the pathway between ATM and ATR activation, thereby reducing the autophosphorylation of ATR and the subsequent phosphorylation of Chk1. CBP-93872 does not inhibit DNA end resection at DSB sites. CBP-93872 induces cell death and enhances the cytotoxic effects of platinum-containing compounds and pyrimidine antimetabolites on cancer cells. CBP-93872 can be used in related research on p53-mutant cancers, colorectal cancer, and pancreatic cancer.

Elimusertib (Standard) is the analytical standard of Elimusertib (HY-101566). This product is intended for research and analytical applications. Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity. Elimusertib can be used for the research of solid tumors and lymphomas.

AZD0156 (Standard) is the analytical standard of AZD0156 (HY-100016). This product is intended for research and analytical applications. AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.

VE-821 (Standard) is the analytical standard of VE-821 (HY-14731). This product is intended for research and analytical applications. VE-821 is a potent ATP-competitive inhibitor of ATR with K_i/IC₅₀ of 13 nM/26 nM.

Ro 90-7501 (Standard) is the analytical standard of Ro 90-7501 (HY-103241). This product is intended for research and analytical applications. Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC₅₀ of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.

AZD-7648 (Standard) is the analytical standard of AZD-7648 (HY-111783). This product is intended for research and analytical applications. AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC₅₀ of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.

Gavapsertib (compound A) is a ATR kinase inhibitor that can be used in tumor research.

Ceralasertib formate is a potent, selective and orally active ATR inhibitor with an IC₅₀ value of 1 nM. Ceralasertib formate inhibits cell viability and induces DNA damage. Ceralasertib formate induces cell senescence. Ceralasertib formate shows antitumor activity.

KU-55933 (Standard) is the analytical standard of KU-55933 (HY-12016). This product is intended for research and analytical applications. KU-55933 is a potent ATM inhibitor with an IC₅₀ and K_i of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

CP-466722 (Standard) is the analytical standard of CP-466722 (HY-11002). This product is intended for research and analytical applications. CP-466722 is a rapidly reversible inhibitor of ATM, with an IC₅₀ of 0.41 μM, and has no effects on PI3K or closely related PI3K-like protein K_inase (PIKK) family members.

Tuvusertib (Standard) is the analytical standard of Tuvusertib (HY-111451). This product is intended for research and analytical applications. Tuvusertib (M1774; ATR inhibitor 1) is a selective and orally active ATR inhibitor extracted from patent WO2015187451A1, compound I-l, with a K_i value below 1 μΜ.

Elrelesertib (Standard) (AZD1390 (Standard)) is the analytical standard of Elrelesertib (AZD1390) (HY-109566). This product is intended for research and analytical applications. Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC₅₀ values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer.