ATM Inhibitor 1

ATM Inhibitor-1 is a highly potent, selective, and orally active ATM inhibitor (IC50: 0.7 nM) with anti-tumor activity. It exhibits weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM), and PI3Kδ (IC50, 0.73 μM).

Tuvusertib (M1774) is an orally available ataxia telangiectasia and Rad3-related (ATR) kinase inhibitor (Ki< 1 µΜ) with selective and potentially antitumor activity.Tuvusertib selectively inhibits ATR activity and blocks downstream phosphorylation of serine threonine protein kinase checkpoint kinase 1 (CHK1), thereby inhibits DNA damage checkpoint activation, disrupting DNA damage repair and inducing apoptosis in tumor cells.

Tyrphostin AG1433 (AG1433) is an inhibitor of tyrosine kinases and also a dual inhibitor of PDGFRβ(IC50s = 5.0 μM) and VEGFR-2 (Flk-1 KDR)(IC50s = 9.3 μM).

ATMInhibitor-11 (Compound 1) is an inhibitor of ATM with an IC50 of 0.32 nM. It also inhibits KAP1 phosphorylation with an IC50 of 0.97 nM. This compound exhibits high exposure in the brain, heart, and plasma of ICR mice. Furthermore, ATMInhibitor-11 demonstrates antitumor activity in the NCI-H441 xenograft mouse model.

Potent and selective ATM kinase inhibitor (IC50 = 0.6 nM in an enzyme inhibition assay). Exhibits > 600-fold selectivity for ATM over other kinases. Inhibits ATM kinase in an in vitro cellular assay (IC50 = 0.33 μM). Potentiates the antitumor effects of the topoisomerase 1 inhibitor irinotecan in tumor bearing, immunocompromised mice. Orally bioavailable. Degorce et al (2016) Discovery of novel 3-quinoline carboxamides as potent, selective and orally bioavailable inhibitors of ataxia telangiectasia mutated (ATM) kinase. J.Med.Chem. 59 6281 PMID:27259031

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK ATM Chk1 2 pathway, leading to inactivation of the Cd

AIM-100 is a Ack1 inhibitor (IC50: 24 nM).

ATM Inhibitor -2 is a potent and selective inhibitor of ATM (IC50<1 nM).

ATM Inhibitor -4 is a selective and potent ATM inhibitor (IC50: 0.32 nM) that strongly inhibits the activity of the PI3K kinase family and exhibits good metabolic stability. ATM Inhibitor -4 completely inhibits mTOR at 1 μM.

ATM-IN-1, a potent inhibitor of ATM, has demonstrated research potential in cancer and neurological diseases.

A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2 M phase cell cycle arrest when combined with CPT-11, displaying notable antitumor activity [1].

ATM Inhibitor-8 (Compound 10r) is a potent, selective, and orally active ATM inhibitor with anti-tumor activity, characterized by an IC50 value of 1.15 nM [1].

ATM Inhibitor-9 (Compd 7a) is a potent ATM kinase inhibitor with an IC50 of 5 nM, used in cancer research [1].

ATM inhibitor-6 (A-193), a selective inhibitor of ATM kinase, is utilized in cancer research [1].

WSD0628 is a brain-penetrant and potent ATM inhibitor with a significant radiosensitizing effect [1].

XRD-0394 is a highly effective and selective dual inhibitor of ATM and DNA-PKcs, exhibiting oral bioactivity. It notably increases tumor cell destruction both in vitro and in vivo when combined with therapeutic ionizing radiation. Furthermore, XRD-0394 enhances the efficacy of PARP and topoisomerase I inhibitors in vitro [1].