ATM Kinase Inhibitor

KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.

Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.RP-3500 is 30-fold more selective for ATR than mTOR (IC50: 120 nM) and more than 2,000-fold more potent than ATM, DNA-PK and PI3Kα kinases. RP-3500 is 30 times more selective for ATR than mTOR (IC50: 120 nM), and 2,000 times more selective than ATM, DNA-PK and PI3Kα kinases.

ART0380 is a potent, selective, orally available, ATP-competitive ATR kinase inhibitor (IC50=51.7 nM) with antitumor activity for the study of ataxia telangiectasia mutated (ATM) cancer.

AZ31 is an ATM inhibitor with potency, high selectivity, and oral activity.AZ31 inhibits ATM enzymes, intracellular ATM, with IC50 values of <1.2 nM and 46 nM, respectively.AZ31 exhibits excellent ATR selectivity, PIKK family selectivity, and pan-kinase selectivity.AZ31 is a potent in vitro radiosensitizer that can be used for cancer research.

Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50: 6.3 nM). It is much less effective or without effect against a panel of 229 other kinases.

ATM-IN-2 is a selective, orally active ATM inhibitor with an IC50 of 4 nM. It demonstrates high kinase selectivity, being over 700 times more selective relative to PIKK family members. ATM-IN-2 exerts its anti-tumor effects and promotes apoptosis by inhibiting ATM phosphorylation and downstream signaling pathways (p53, H2AX). It is applicable for research in solid tumors, such as colon cancer.

ATM-IN-12 (example 1.1) is an ATM kinase inhibitor with an IC50 of 1.26 μM. It is useful for investigating diseases mediated by ATM kinase, such as cancer.

ATR-IN-31 is a selective ATR kinase inhibitor with an IC50 of 7 nM. It does not significantly inhibit ATM kinase activity and can suppress ATR kinase activity at the functional level. ATR-IN-31 is capable of inhibiting the viability of prostate cancer cells and is applicable for research related to prostate cancer.

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

Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110α, 5 nM for p110γ, 7 nM for p110δ, 75 nM for p110β, and 20.7 nM for mTOR.

NU 7026 (DNA-PK Inhibitor II) is an effective DNA-PK inhibitor (IC50: 0.23 μM, in cell-free assays), 60-fold selective for DNA-PK than PI3K and no inhibition against both ATM and ATR.

PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.

AZ 5704 (compound 74) is a selective and orally active ATM inhibitor (IC50 = 0.6 nM), which can enhance the anti-tumor activity of irinotecan in the SW620 xenograft model.

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

Mirin is a Mre11-Rad50-Nbs1 (MRN) complex inhibitor that inhibits MRN-dependent ATM activation without affecting ATM protein kinase activity. It also inhibits Mre11-associated exonuclease activity, thereby disrupting DNA double-strand break repair.Mirin induces cell cycle arrest in G1 phase.

SKLB-197 is a potent and highly selective inhibitor of ataxia telangiectasia and Rad3-related kinase (ATR) with an IC50 value of 0.013 μM and minimal activity against more than 402 other kinases. SKLB-197 shows strong antitumor efficacy in ATM-deficient tumors both in vitro and in vivo, while also exhibiting favorable pharmacokinetic properties for oncology research.

Lartesertib (ATM Inhibitor-5) is an inhibitor of serine/threonine protein kinase ATM with potential anticancer activity for the study of lung cancer.

Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8/48 nM) that blocks autophagy.

ATM Inhibitor-3 is a potent and selective inhibitor of ATM (IC50: 0.71 nM). ATM Inhibitor-3 inhibits the PI3K kinase family and exhibits good metabolic stability.

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.

NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.

SU-11752 is a potent and selective DNA-PK inhibitor. Inhibition kinetics and a direct assay for ATP binding showed that SU11752 inhibited DNA-PK by competing with ATP. SU11752 inhibited DNA double-strand break repair in cells and gave rise to a five-fold sensitization to ionizing radiation. At concentrations of SU11752 that inhibited DNA repair, cell cycle progression was still normal and ATM kinase activity was not inhibited.

M3541 is a selectively potent and orally active ATM inhibitor with potential antitumor activity.M-3541 inhibits ATM kinase activity and ATM-mediated signaling by binding to ATM.M3541 prevents activation of DNA damage checkpoints, inhibits DNA damage repair, contributes to apoptosis, and induces death of ATM overexpressing tumor cells.

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.