ATM/ATR Inhibitor

ATR-IN-22 (Compound 34) is an orally active ATR inhibitor. ATR-IN-22 inhibits MIAPaCa-2 proliferation (IC₅₀ <1 μM). ATR-IN-22 shows anti-tumor activity in colon cancer.

(Rac)-Lartesertib ((Rac)-M4076) is an isoform of Lartesertib (HY-150617). Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity.

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.

ATR-IN-12 (Compound 5g) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase with an IC₅₀ value of 0.007 μM. ATR-IN-12 displays good anti-tumor activity and significantly reduces the phosphorylation level of ATR and its downstream signaling protein. ATR-IN-12 is a promising lead compound for subsequent agent discovery targeting ATR kinase.

ATR-IN-8 is a potent inhibitor of ATR. ATR is a key enzyme in the homologous recombination repair pathway and belongs to the PIKK family. ATR-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021143821A1, compound 3).

ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. ATR kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing replication stress (RS). ATR-IN-11 is a promising lead compound for subsequent agent discovery targeting ATR kinase. ATR-IN-11 has the potential for the research of cancer disease.

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

ATM-IN-12 (example 1.1) is an ATM kinase inhibitor with an IC₅₀ of 1.26 μM. ATM-IN-12 can be used for the study of ATM kinase mediated disease, including cancer.

ATR-IN-29 is a potent and orally active ATR kinase inhibitor with an IC₅₀ value of 1 nM. ATR-IN-29 shows antiproliferative activity.

ATR-IN-13 (compound A9) is a potent ATR kinase inhibitor, with an IC₅₀ of 2 nM. ATR-IN-13 can be used for ATR kinase mediated diseases research, such as proliferative diseases and cancer.

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.

ATM-IN-13 (A36) is an orally active, selective ATM kinase inhibitor with a human IC₅₀ of 0.3 nM. ATM-IN-13 blocks the ATM-mediated DNA double-strand break repair signaling pathway, reduces the phosphorylation levels of ATM and p53, and inhibits ATM-dependent DNA damage response. ATM-IN-13 can be used in the research of colorectal cancer.

ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC₅₀ of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC₅₀ of 37.34 nM. ATR-IN-18 has anti-tumor activity.

ATR kinase-IN-2 (Compound I-G-27) is a ATR protein kinase inhibitor with the K_i of 0.01 ~ 1 μΜ and can be used for study of cancer.

ATR-IN-5 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-5 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent CN112047938A, compound D24).

ATM Inhibitor-9 (Compd 7a) is a potent ATM inhibitor with IC₅₀5 nM for ATM kinase, useful in cancer research.

ATR kinase-IN-3 (Compound I-G-28) is a ATR protein kinase inhibitor with the K_i of 0.01 ~ 1 μΜ and can be used for study of cancer.

ATR-IN-16 (compound 46) is a potent ATR kinase inhibitor. ATR-IN-16 shows good anticancer activity in LoVo cells, with an IC₅₀ of 410 nM.