ATM(ATR)

ATM(ATR)

Members of the phosphatidyl inositol 3-kinase-like family of serine/threonine protein kinases (PIKKs), ATM/ATR are well-known for being key players in the mounting responses to DNA double-strand breaks (DSBs) and single-stranded DNA (ssDNA) that occur during the mitotic DNA damage response (DDR). Ionizing radiation activates the signal transduction pathways that cause cell cycle arrest at G1/S, S, and G2/M by activating the ATM. In response to DNA-damaging agents like ultraviolet radiation that cause hefty lesions, ATR is necessary for cell cycle arrest.

In order to stabilize stalled replication forks, repair damaged DNA, and stop the cell cycle from continuing, ATM/ATR phosphorylate a wide range of targets upon activation. This helps to ensure cell survival and protect the integrity of the genome. The cell cycle checkpoints activated by ATM and ATR act as an active defense against tumorigenesis and genome instability in replicating cells.

ATM(ATR) related products

Structure Cat No. Product Name CAS No. Product Description
V0231 AZ20 1233339-22-4 AZ20 is a novel potent and selective inhibitor of ATR(ATM and Rad3-related) protein kinase with potential antitumor activity.
V3683 AZ31 2088113-98-6 AZ31 (AZ-31; AZ 31) is a novel, potent and orally bioavailable and BBB (blood-brain barrier)-penetreable ATM inhibitor with antitumor activity.
V3682 AZ32 2288709-96-4 AZ32 is a novel, potent and orally bioavailable and blood-brain barrier-penetreable ATM inhibitor (AZ32) that radiosensitizes intracranial gliomas in mice.
V0075 AZD1390 2089288-03-7 AZD1390 (AZD-1390) is a novel, potent, selective, first-in-class orally bioavailable and CNS penetrant inhibitor of Ataxia-telangiectasia mutated (ATM) kinase with potential anticancer activity.
V2529 Berzosertib (VE-822; VX-970) 1232416-25-9 This product is discontinued due to commercial reason,Berzosertib (VE-822; VX-970; M6620) is a specific ATR inhibitor with IC50 of 19 nM in HT29 cells.
V0181 CB-5083 1542705-92-9 CB-5083 is a novel, potent, selective, first in class and orally bioavailable p97 AAA ATPase inhibitor with potential anticancer activity.
V0233 Ceralasertib (AZD-6738) 1352226-88-0 Ceralasertib (formerly AZD6738), amorpholino-pyrimidine-based DNA damage repair agent,is a potent, orally bioavailable and selective inhibitor of ATR (ataxia telangiectasia and rad3 related) kinase with potential antitumor activity.
V0230 CGK-733 905973-89-9 CGK 733 is a novel, potent and selective inhibitor of ATM (ataxia-telangiectasia mutated) and ATR (ATM and Rad3-related)with the potential to treat Hepatocellular carcinoma (HCC).
V2530 Chloroquine Phosphate 50-63-5 Chloroquine phosphate is reported to be highly effective in combating SARS-CoV-2 (COVID-19, CoronaVirus, or the COVID-19 pandemic) infection in vitro.
V2528 CP-466722 1080622-86-1 CP-466722 is a novel, specific and reversible ATM inhibitor with anIC50value of 4.1 μM, it does not affect ATR and inhibits PI3K or PIKK family members in cells.
V3122 Elimusertib (BAY-1895344) HCl Elimusertib (BAY1895344) HCl, the hydrochloride salt of BAY 1895344, is a selective and orally bioavailable ATR (ataxia telangiectasia and Rad3-related) inhibitor with potential antitumor activity.
V0204 ETP-46464 1345675-02-6 ETP-46464 (ETP46464) is a novel, potent and selective inhibitor of ATR (Ataxia-telangiectasia mutated) and mTOR (mammalian target of rapamycin) with potential anticancer activity.
V2525 KU-55933 587871-26-9 KU-55933 is a potent and specific ATM (Ataxia-telangiectasia mutated) kinase inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
V2526 KU-60019 925701-49-1 KU-60019 is an improved analogue of KU-55933 with 10-fold higher activity than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells.
V0232 Schisandrin B (γ-Schisandrin; Sch B) 61281-37-6 Schisandrin B (γ-Schisandrin; Sch B) is a naturally occuring and the most abundant dibenzocyclooctadiene lignan isolated from traditional Chinese medicinal herb Schisandra chinensis (Turcz.) with antioxidant effect on rodent liver and heart. Baill.
V4459 SKLB-197 2713577-16-1 SKLB 197 is a novel and potent ATR inhibitor (IC50 =0.013 μM).
V0196 Torin 2 1223001-51-1 Torin 2 is a novel, potent and selective ATP-competitive inhibitor of mTOR (mammalian target of rapamycin) with potential antitumor activity.
V2527 VE-821 1232410-49-9 VE-821 is a novel potent and highly selective ATP competitive protein kinase inhibitor of ATR (ataxia telangiectasia mutated and Rad3 related) with Ki and IC50 of 13 nM and 26 nM in cell-free assays, it shows inhibition of H2AX phosphorylation, and had minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
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