1627709-94-7

1627709-94-7 structure

Name: LJI308
Chemical Name: 2,6-Difluoro-4-{4-[4-(4-morpholinyl)phenyl]-3-pyridinyl}phenol
CAS Number: 1627709-94-7
Molecular Formula: C₂₁H₁₈F₂N₂O₂
Molecular Weight: 368.377
Catalog: Signaling Pathways MAPK/ERK Pathway Ribosomal S6 Kinase (RSK)
Create Date: 2016-08-07 18:23:33
Modify Date: 2024-01-18 19:02:22
LJI308 is a new and potent pan-RSK inhibitor, with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.IC50 value: 6/4/13 nMTarget: RSK1/2/3in vitro: LJI308 efficiently inhibits RSK activity. LJI308 inhibites S6K1 with an IC50 of 0.8 μM, representing a 200-fold lower inhibition than that of RSK2. LJI308 inhibits MEK4 less than 50% at 10 μMand HIP kinase 1 less than 50% at 1 μM. [1] LJI308 inhibits the growth and survival of TNBC. LJI308 also suppresses the growth of HTRY-LT cells in 3-dimensional soft agar cultures. LJI308 is one of the first potent and effective targeted therapies for TNBC that, unlike currently utilized drugs, exhibits efficacy in eliminating the CSC population. [2]

Name	2,6-Difluoro-4-{4-[4-(4-morpholinyl)phenyl]-3-pyridinyl}phenol
Synonyms	2,6-Difluoro-4-{4-[4-(4-morpholinyl)phenyl]-3-pyridinyl}phenol Phenol, 2,6-difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]- LJI308 LJI-308

Description	LJI308 is a new and potent pan-RSK inhibitor, with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.IC50 value: 6/4/13 nMTarget: RSK1/2/3in vitro: LJI308 efficiently inhibits RSK activity. LJI308 inhibites S6K1 with an IC50 of 0.8 μM, representing a 200-fold lower inhibition than that of RSK2. LJI308 inhibits MEK4 less than 50% at 10 μMand HIP kinase 1 less than 50% at 1 μM. [1] LJI308 inhibits the growth and survival of TNBC. LJI308 also suppresses the growth of HTRY-LT cells in 3-dimensional soft agar cultures. LJI308 is one of the first potent and effective targeted therapies for TNBC that, unlike currently utilized drugs, exhibits efficacy in eliminating the CSC population. [2]
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> Ribosomal S6 Kinase (RSK) Research Areas >> Cancer
References	[1]. Aronchik I, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12. [2]. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7. [3]. Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.