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关于此项目
经验公式(希尔记法):
C22H21F2N3O
化学文摘社编号:
分子量:
381.42
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
LJH685, ≥98% (HPLC)
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Dewei Jiang et al.
Cell death and differentiation, 29(6), 1283-1295 (2022-01-14)
Y-box binding protein 1 (YB-1) is a well-known oncogene highly expressed in various cancers, including basal-like breast cancer (BLBC). Beyond its role as a transcription factor, YB-1 is newly defined as an epigenetic regulator involving RNA 5-methylcytosine. However, its specific
Ida Aronchik et al.
Molecular cancer research : MCR, 12(5), 803-812 (2014-02-21)
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
Xiaolin Guan et al.
Cell death discovery, 8(1), 84-84 (2022-02-27)
Breast cancer is one of the leading causes of mortality among women. Triple-negative breast cancer (TNBC) is responsible for a large percentage of all breast cancer deaths in women. This study demonstrated the function of Myb-like, SWIRM, and MPN domains
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