Ribosomal S6 Kinase (RSK)|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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Ribosomal S6 Kinase (RSK) is a family of protein kinases involved in signal transduction. There are two subfamilies of rsk, p90rsk, also known as MAPK-activated protein kinase-1 (MAPKAP-K1), and p70rsk, also known as S6-H1 Kinase or simply S6 Kinase. There are three variants of p90rsk in humans, rsk 1-3. Rsks are serine/threonine kinases and are activated by the MAPK/ERK pathway. There are two known mammalian homologues of S6 Kinase: S6K1 and S6K2. Rsk is named for ribosomal protein s6, part of the translational machinery, but several other substrates have been identified, including other ribosomal proteins. Cytosolic substrates of p90rsk include protein phosphatase 1; glycogen synthase kinase 3 (GSK3); L1 CAM, a neural cell adhesion molecule, the Ras exchange factor; and Myt1, an inhibitor of cdc2. p90rsk also regulates transcription factors including cAMP response element-binding protein (CREB); estrogen receptor-α (ERα); IκBα/NF-κB; and c-Fos

Cat. No.	Product Name	CAS No.	Information
H7551	SL-0101	77307-50-7	The first specific inhibitor of RSK (p90 ribosomal S6 kinase) with IC50 of 89 nM for RSK2; does not inhibit upstream kinases such as MEK, Raf and PKC; inhibits the growth of MCF-7 human breast cancer cells with no effect on the normal breast cell line.
H7550	RSK2-IN-20	1627136-55-3	RSK2-IN-20 is a potent, selective, and durable inhibitpr of RSK2 with IC50 of 47 nM; shows high selectivity over NEK2, PLK1; potently inhibits MSK1 autophosphorylation in cells, and has no significant effect on a panel of 18 additional kinases.
H7549	Pluripotin	839707-37-8	A small molecule that can maintain the self-renewal of mESC (murine embryonic stem cells) in the absence of feeder cells and exogenous factors; works through dual inhibition of RasGAP and ERK1; maintains the undifferentiated phenotype of mES cells with EC50 of 1 uM, and shows low cellular toxicity (>30 uM).
H7548	M-2698	1379545-95-5	A potent, selective, ATP-competitive, orally bioavailable and brain penetrant dual inhibitor of p70S6K and Akt1/3 with IC50 of 1 nM and 17 nM, respectively; displays relative selectivity against a panel of 264 kinases (only 6 kinases within 10-fold IC50 of p70S6K); inhibits the phosphorylation of p70S6K1 and Akt substrates, S6 (IC50=11 nM) and GSK3β (IC50=17 nM) in MDA-MB-468 cells, show proliferation inhibition of 9 breast cancer cell lines (IC50
H7547	LY-2584702 tosylate salt	1082949-68-5	LY2584702 is a potent, selective, ATP-competitive inhibitor of P70 S6 kinase-1 (p70S6K1) with IC50 of 4 nM; blocks phosphorylation of p70S6K in primary rat hepatocytes without affecting the phosphorylation of other signaling kinases, including GSK-3β and ERK1/2; inhibits phosphorylation of p70S6K in HCT116 colon cancer cells with IC50 of 0.1-0.24 uM, demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.
H7546	LY-2584702 hydrochloride	1082948-81-9	LY2584702 is a potent, selective, ATP-competitive inhibitor of P70S6 kinase-1 (p70S6K1) with IC50 of 4 nM; blocks phosphorylation of p70S6K in primary rat hepatocytes without affecting the phosphorylation of other signaling kinases, including GSK-3β and ERK1/2; inhibits phosphorylation of p70S6K in HCT116 colon cancer cells with IC50 of 0.1-0.24 uM, demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.
H7545	LY-2584702 free base	1082949-67-4	LY2584702 is a potent, selective, ATP-competitive inhibitor of P70 S6 kinase-1 (p70S6K1) with IC50 of 4 nM; blocks phosphorylation of p70S6K in primary rat hepatocytes without affecting the phosphorylation of other signaling kinases, including GSK-3β and ERK1/2; inhibits phosphorylation of p70S6K in HCT116 colon cancer cells with IC50 of 0.1-0.24 uM, demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.
H7544	LJI-308	1627709-94-7	LJI-308 is a potent and specific pan-RSK inhibitor with IC50s of 6 nM,4 nM and 13 nM for RSK1,RSK2 and RSK3 respectively; inhibts Y-box binding protein-1 (YB-1) Ser102 phosphorylation (EC50= 0.2-0.3 uM) in MDA-MB-231 cancer cells.
H7543	LJH-685	1627710-50-2	LJH-685 is a potent and specific pan-RSK inhibitor with IC50s of 6 nM,5 nM and 4 nM for RSK1,RSK2 and RSK3 respectively; inhibts Y-box binding protein-1 (YB-1) Ser102 phosphorylation (EC50=0.2-0.3 uM) in MDA-MB-231 cancer cells.
H7542	FMK	821794-92-7	An irreversible inhibitor of the CTD of RSK1 and RSK2 with IC50 of 15 nM for wt RSK2; shows 600- and 200-fold selectivity over the C436V and T493M mutants, respectively; inhibits EGF-induced Ser386 phosphorylation of endogenous RSK2 in COS-7 cells (IC50=200 nM); also potently inhibits a Fyn mutant in which Val285 was replaced with Cys(IC50=100 nM), weakly inhibits WT Fyn with IC50 of 4 uM.

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