| LJH685RSK (p90 ribosomal S6 kinase) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 1627710-50-2 | SDF | Download SDF |
| Chemical Name | 2,6-difluoro-4-(4-(4-(4-methylpiperazin-1-yl)phenyl)pyridin-3-yl)phenol | ||
| Canonical SMILES | OC1=C(F)C=C(C2=C(C3=CC=C(N4CCN(C)CC4)C=C3)C=CN=C2)C=C1F | ||
| Formula | C22H21F2N3O | M.Wt | 381.42 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 6 nM, 5 nM and 4 nM for the biochemical activities of RSK1, RSK2, and RSK3, respectively
LJH685 is a RSK (p90 ribosomal S6 kinase) inhibitor.
The p90 ribosomal S6 kinase (RSK) family of serine/threonine kinases is found to be expressed in a variety of cancers and its substrate phosphorylation has been implicated in direct regulation of cell proliferation, cell survival, as well as cell polarity.
In vitro: In a previous study, the structural analysis results confirmed the binding of LJH685 to the RSK2 N-terminal kinase ATP-binding site, which suggested that the inhibitor LJH685 adopted an unusual nonplanar conformation that explained its excellent selectivity for RSK family kinases. In addition, LJH685 and it analog LJI308 could efficiently inhibit RSK activity in vitro and in cells. Moreover, in a subset of examined cell lines, the cellular inhibition of RSK and its phosphorylation of YB1 on Ser102 were found to be closely associate with the inhibition of cell growth in an anchorage-independent growth setting [1].
In vivo: So far, there is no animal in vivo data reported for LJH685.
Clinical trial: Up to now, LJH685 is still in the preclinical development stage.
Reference:[1] Aronchik I, Appleton BA,Basham SE,Crawford K,Del Rosario M,Doyle LV,Estacio WF,Lan J,Lindvall MK,Luu CA,Ornelas E,Venetsanakos E,Shafer CM,Jefferson AB. 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.
