SML1788
LJI308
≥98% (HPLC)
别名:
2,6-Difluoro-4-(4-(4-morpholinophenyl)pyridin-3-yl)phenol, 2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]phenol
登录 查看组织和合同定价。
选择规格
变更视图
关于此项目
经验公式（希尔记法）:
C21H18F2N2O2
化学文摘社编号:
分子量:
368.38
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 5 mg/mL, clear (warmed)
storage temp.
−20°C
SMILES string
OC1=C(C=C(C=C1F)C2=C(C=CN=C2)C3=CC=C(C=C3)N4CCOCC4)F
InChI
1S/C21H18F2N2O2/c22-19-11-15(12-20(23)21(19)26)18-13-24-6-5-17(18)14-1-3-16(4-2-14)25-7-9-27-10-8-25/h1-6,11-13,26H,7-10H2
InChI key
YUYJEQHNWKQNBT-UHFFFAOYSA-N
Biochem/physiol Actions
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).
LJI308 is potent pan-RSK inhibitor that targets RSK N-terminal kinase domain ATP-binding site and inhibits YB1-dependent growth of cncer cells.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable