| S3224 |
Cinobufagin |
Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis. |
Selective |
|
| S8375 |
AZD0156 |
AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. |
Selective |
|
| S8680 |
AZD1390 |
AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases. |
Selective |
ATM, IC50: 0.78 nM |
| S8729 |
AZ32 |
AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability. |
Selective |
ATM, IC50: <0.0062 μM |
| S1570 |
KU-60019 |
KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer. |
Selective |
ATM, IC50: 6.3 nM |
| S1092 |
KU-55933 |
KU-55933 is a potent and specific ATM 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. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy. |
Selective |
ATM, IC50: 12.9 nM |
| S2758 |
Wortmannin |
Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity. |
Selective |
ATM, IC50: 150 nM |
| S2245 |
CP-466722 |
CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells. |
Selective |
ATM, IC50: 410 nM |
| S8556 |
AZ31 |
AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ). |
Selective |
|
| S4157 |
Chloroquine diphosphate |
Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). |
Selective |
|
| S8096 |
Mirin |
Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. Mirin inhibits MRN-dependent activation of ATM. |
Selective |
|
| S2817 |
Torin 2 |
Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis. |
Pan |
ATM, EC50: 28 nM |
| S7136 |
CGK 733 |
CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM. |
Pan |
ATM, IC50: 200 nM |
| S8050 |
ETP-46464 |
ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. |
Pan |
ATM, IC50: 545 nM |
