LJI308

产品名称：

1627709-94-7
LJI308
2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]phenol
2,6-Difluoro-4-(4-(4-morpholinophenyl)pyridin-3-yl)phenol

产品介绍：

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