LJI308

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LJI308 是一种有效的泛 RSK（p90 核糖体 S6 激酶）抑制剂，对 RSK1、RSK2 和 RSK3 的 IC50 分别为 6 nM、4 nM 和 13 nM。

LJI308 is a RSK inhibitor. LJI308 overcomes chemoresistance by eliminating cancer stem cells. LJI308 targets the CSC population and repress TNBC growth and dissemination. LJI308 specifically targeted transformed cells as it had little effect on the non-tumorigenic parental HMECs. Targeting RSK using specific and potent inhibitors, such as LJI308, delivers the promise of inhibiting the growth of TNBC.

LJI308 inhibits S6K1 with an IC50 of 0.8 μM.LJI308 inhibits YB-1 phosphorylation in CRC cells at concentrations of 5 to 25 μM. In a dose kinetics experiment, LJI308, starting at 2.5 μM, inhibits YB-1 phosphorylation in the KRAS mutated TNBC cell line MDA-MB-231 by approximately 86%. LJI308 effectively blocks RSK and YB-1 phosphorylation after EGF stimulation and after irradiation in KRAS wild-type HBL-100 cells.LJI308 (1-10 μM; 96 hours) decreases cell viability by up to 90%. Cell Viability Assay Cell Line:HTRY-LT cell lines Concentration:1-10 μM Incubation Time:96 hours Result:Decreased cell viability by up to 90%.

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LJI308 | LJI-308 | LJI 308 | NVP-LJI308 | NVP-LJI-308

Angiogenesis

PDE

RSK1|RSK2|RSK3

Cancer

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1627709-94-7

368.38

C21H18F2N2O2

>98% (HPLC)

DMSO : ≥ 32 mg/mL 86.87 mM

Oc1c(F)cc(cc1F)-c1cnccc1-c1ccc(cc1)N1CCOCC1

2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]-phenol

(-20℃)

With Ice Pack

≥ 2 years