LJI308
SIGMA/SML1788 - ≥98% (HPLC)
Synonym: 2,6-
CAS Number: 1627709-94-7
Empirical Formula (Hill Notation): C21H18F2N2O2
Molecular Weight: 368.38
MDL Number: MFCD29905461
Linear Formula: C21H18F2N2O2
Product Type: Chemical
| assay | ≥98% (HPLC) |
| color | white to beige |
| form | powder |
| Quality Level | 100  |
| SMILES string | OC1=C(C=C(C=C1F)C2=C(C=CN |
| solubility | DMSO: 5 mg/mL, clear (warmed) |
| storage temp. | −20°C |
| 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). |
| Packaging: | 5, 25 mg in glass bottle |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | −20°C |
| UNSPSC | 12352200 |