SML3645
LJH685
≥98% (HPLC)
Synonyme(s) :
2,6-Difluoro-4-(4-(4-(4-methylpiperazin-1-yl)phenyl)pyridin-3-yl)phenol, 2,6-Difluoro-4-[4-[4-(4-methyl-1-piperazinyl)phenyl]-3-pyridinyl]phenol, LJH 685, LJH-685, NVP-LJH685
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A propos de cet article
Formule empirique (notation de Hill) :
C22H21F2N3O
Numéro CAS:
Poids moléculaire :
381.42
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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Laissez-nous vous aiderQuality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
SMILES string
Fc1c(c(cc(c1)c2cnccc2c3ccc(cc3)N4CCN(CC4)C)F)O
InChI
1S/C22H21F2N3O/c1-26-8-10-27(11-9-26)17-4-2-15(3-5-17)18-6-7-25-14-19(18)16-12-20(23)22(28)21(24)13-16/h2-7,12-14,28H,8-11H2,1H3
InChI key
IKUFKDGKRLMXEX-UHFFFAOYSA-N
Biochem/physiol Actions
LJH685 is potent pan-RSK inhibitor that targets RSK N-terminal kinase domain (NTKD) ATP-binding site (IC50/[ATP] = 6 nM/5 μM/RSK1, 5 nM/20 μM/RSK2, 4 nM/10 μM/RSK3). LJI308 effectivelfy inhibits MAPK pathway-dependent cancer growth (EC50 values of 0.73 μM/MDA-MB-231 and 0.79 μM/H358) by reducing the phosphorylation level of cellular Y-box binding protein-1 (YB1) Ser102 (EC50 = 0.2-0.3 μM; MDA-MB-231 and H358), but not that of ribosomal S6 protein (S6RP) S235/236.
Potent pan-RSK inhibitor that targets RSK N-terminal kinase domain (NTKD) ATP-binding site.
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Ida Aronchik et al.
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The p90 ribosomal S6 kinase (RSK) family of serine/threonine kinases is expressed in a variety of cancers and its substrate phosphorylation has been implicated in direct regulation of cell survival, proliferation, and cell polarity. This study characterizes and presents the