产品说明
包装
5, 25 mg in glass bottle
生化/生理作用
LJI308 is potent pan-RSK inhibitor that targets RSK N-terminal kinase domain (NTKD) ATP-binding site (IC50/[ATP] = 6 nM/5 μM/RSK1, 4 nM/20 μM/RSK2, 13 nM/10 μM/RSK3), exhibiting similary binding affinity toward RSK1-4, but much reduced inhibitory potency against S6K1 (IC50 = 0.8 μM), MEK4 (IC50 >10 μM), and HIP kinase 1 (IC50 >1 μM). LJI308 effectivelfy reduces cellular Y-box binding protein-1 (YB1) Ser102 (EC50 = 0.2-0.3 μM; MDA-MB-231 and H358 cells), but not ribosomal S6 protein (S6RP) S235/236, phosphorylation level and selectively inhibits the growth of YB1-overpressing HTRY-LT triple-negative breast cancer (TNBC) cells, but not the parental non-tumorigenic human mammary epithelial cell (HMEC) line HTRZ (% inhibition = 6.8%/HTRZ, 88%/HTRY-LT1, 66%/HTRY-LT2 in 8 days; 5 μM at 0 and 96 hr).
基本信息
| 经验(实验)分子式 | C21H18F2N2O2 |
| 分子量 | 368.38 |
| MDL编号 | MFCD29905461 |
| PubChem化学物质编号 | 329826065 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 5 mg/mL, clear (warmed) |
| 储存温度 | −20℃ |
| SMILES string | OC1=C(C=C(C=C1F)C2=C(C=CN=C2)C3=CC=C(C=C3)N4CCOCC4)F |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
