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KU55933 (ATM Kinase Inhibitor)
| Product Name | KU55933 (ATM Kinase Inhibitor) |
| Price: | Inquiry |
| Catalog No.: | CN00525 |
| CAS No.: | 587871-26-9 |
| Molecular Formula: | C21H17NO3S2 |
| Molecular Weight: | 395.49 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=c1cc(oc(c1)c1cccc2c1Sc1ccccc1S2)N1CCOCC1 |
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| Description | KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. |
| Target | ATM:12.9 nM (IC50) DNA-PK:2500 nM (IC50) mTOR:9300 nM (IC50) PI3K:16600 nM (IC50) |
| In Vitro | KU-55933 (10 μM) blocks the ionizing radiation-induced p53 serine 15 phosphorylation. KU-55933 has a dose-dependent effect in inhibiting this ATM-dependent phosphorylation event with an estimated IC50 of 300 nM. KU-55933 ablates the ionizing radiation-induced phosphorylation of these ATM substrates. KU-55933 specifically inhibits ATM but not the other DNA damage-activated PIKKs, ATR, and DNA-PK[1]. KU-55933 induces pATM, p53, E2F1 and pATR, noticeably upregulates the nuclear fraction of E2F1 at the 0.5 h time point[2]. Metformin increases ATM and AMPK phosphorylation, as well as SHP protein level in primary hepatocytes, and this stimulatory effect of metformin is repressed by a specific ATM kinase inhibitor KU-55933[3]. |
| Cell Assay | 1BR or AT4 cells are seeded in 10-cm Petri dishes and treated on day 2 (80 to 90% confluence). Cells are preincubated for 1 hour with KU-55933 or vehicle control and then exposed to 5 Gy of ionizing radiation. Time courses of cell cycle distribution are performed, and the optimal time for discrimination of populations is selected as 16 hours. All subsequent experiments are performed at the 16-hour time point. Cells are stained with propidium iodide according to standard protocols and analyzed by FACS with a FACScalibur. Exponentially growing (50-70% confluent) SW620 cells in 60 mm dishes are exposed to KU-55933 or DMSO for 1 h before addition of etoposide (final concentration of 0.1 and 1 μM) for 16 h before harvesting, propidium iodide staining and analysis as above. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 628.0±55.0 °C at 760 mmHg |
| Flash Point | 333.6±31.5 °C |
| Exact Mass | 395.064972 |
| PSA | 93.28000 |
| LogP | 6.13 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Storage condition | Desiccate at -20°C |