ATM Inhibitor

ATM Inhibitor-7 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC₅₀ value of 1.0 nM. ATM Inhibitor-7 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). ATM Inhibitor-7 combines with CPT-11 shows antitumor activity.

ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC₅₀ of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability.

AZD-7648 (GMP) is AZD-7648 (HY-111783) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.

ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC₅₀ of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC₅₀ of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model.

ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC₅₀ of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC₅₀ values of 47, 663 and 5131 nM, respectively.

ATM Inhibitor-2 (compound 7) is a potent and selective ATM inhibitor, with an IC₅₀ of <1 nM.

ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC₅₀ of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC₅₀ of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects.

Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity.

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

ATM-IN-2 is a selective and orally active ATM inhibitor with an IC₅₀ of 4 nM. ATM-IN-2 exhibits excellent kinase selectivity (>700-fold over PIKK family members). ATM-IN-2 exerts its anti-tumor effect by inhibiting ATM phosphorylation and the downstream signaling pathways (p53, H2AX), and promotes cell apoptosis. ATM-IN-2 can be used for the study of chemosensitizer candidate such as colon cancer.

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.