1879887-96-3
1879887-96-3 structure
- Name: LTURM 34
- Chemical Name: LTURM34
- CAS Number: 1879887-96-3
- Molecular Formula: C24H18N2O3S
- Molecular Weight: 414.476
- Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA-PK
- Create Date: 2018-06-30 11:32:43
- Modify Date: 2024-01-13 18:26:41
-
LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 μM.
| Name | LTURM34 |
|---|---|
| Synonyms |
8-(Dibenzo[b,d]thiophen-4-yl)-2-(4-morpholinyl)-4H-1,3-benzoxazin-4-one
4H-1,3-Benzoxazin-4-one, 8-(dibenzo[b,d]thien-4-yl)-2-(4-morpholinyl)- |
| Description | LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 μM. |
|---|---|
| Related Catalog | |
| Target |
DNA-PK:34 nM (IC50) PI3Kβ:5.8 μM (IC50) PI4Kδ:8.5 μM (IC50) |
| In Vitro | LTURM34 shows potent inhibition of DNA-PK with excellent selectivity over the Class I PI3K isoforms. The IC50s are 5.8 and 8.5 μM for PI3K β and δ, respectively. LTURM34 shows potent and broad ranging antiproliferative activity. LTURM34 is more consistently active against the selected cell lines (11 of 16), but at best shows 54% inhibition against the HOP-92 non-small cell lung cancer line[1]. |
| Kinase Assay | LTURM34 is dissolved at 10 mM in DMSO and stored at -20°C until use. PI3K enzyme activity is determined in 50 μL of 20 mM HEPES pH 7.5, 5 mM MgCl2 with 180 μM PI and 10 μM ATP. After a 60 min incubation at room temperature the reaction is stopped by the addition of 50 μl of Kinase-Glo followed by a further 15 min incubation. Luminescence is then read using a luostar plate reader. LTURM34 is diluted in 20% (v/v) DMSO at the ndicated concentrations in order to generate a concentration versus inhibition of enzyme activity curve which is then analysed using GraphPad Prism version 5.00 for Windows, in order to calculate the IC50[1]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 657.8±65.0 °C at 760 mmHg |
| Molecular Formula | C24H18N2O3S |
| Molecular Weight | 414.476 |
| Flash Point | 351.6±34.3 °C |
| Exact Mass | 414.103821 |
| LogP | 3.97 |
| Vapour Pressure | 0.0±2.0 mmHg at 25°C |
| Index of Refraction | 1.742 |
| Storage condition | -20℃ |