All AbMole products are for research use only, cannot be used for human consumption.
Compound 401 is a potent inhibitor of DNA-PK (IC50=0.28 μM). Compound 401 is reported to be a poor inhibitor of PI3K, ATM, and ATR in vitro, but it is active against mTOR. Compound 401 shows activity against mTOR (IC50=5.3 μM) but not p110α/p85α PI3K (IC50>100 μM). Treatment of cells with Compound 401 blocks the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr389 and Akt Ser473, respectively). By contrast, there is no direct inhibition of Akt Thr308 phosphorylation, which is dependent on PI3K. Similar effects are also observed in cells that lack DNA-PK. Compound 401 inhibits immunoprecipitated epitope-tagged mTOR or endogenous mTOR in Raptor immunoprecipitates. In both cases, inhibition of 67% or 78% is obtained at 5 μM or 10 μM Compound 401, respectively. By contrast, dose response curves show that the p110α/p85α or p110β/p85α PI3K complexes are poorly inhibited by Compound 401 at these concentrations. The proliferation of TSC1-/- fibroblasts is inhibited in the presence of Compound 401, but TSC1+/+ cells are resistant.
| Cell Experiment | |
|---|---|
| Cell lines | COS7 cells |
| Preparation method | Twenty-two hours later the cells were preincubated for 20 min with 0.1% dimethyl sulfoxide (Con) or the indicated concentrations of 401 (in μM). |
| Concentrations | 25 μM |
| Incubation time | 22 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 281.31 |
| Formula | C16H15N3O2 |
| CAS Number | 168425-64-7 |
| Solubility (25°C) | 6 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related DNA-PK Products |
|---|
| Nedisertib
Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. |
| BAY-8400
BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). |
| ZL-2201
ZL-2201 is a potent DNA-PK inhibitor with an IC50 of 1 nM. |
| AMA-37
AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively. |
| PIK-75
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis. |
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