Home MAPK S6 Kinase

S6 Kinase inhibidores (S6 Kinase Inhibitors)

The 70 kDa ribosomal protein S6 kinase (p70 S6K) is a serine/threonine kinase. Two members of S6K family are named as S6K1 and S6K2, respectively. As the downstream target of PI3K/Akt/mTOR signaling pateway, S6K could be activated in response to many stimulus such as growth factors, cytokines and nutrients.  [show the full text]

Otro MAPK Inhibidores

MEK p38 MAPK Raf JNK ERK MNK TOPK Mixed Lineage Kinase TAK1 KLF

Productos selectivos de isoformas

Nº Cat. Nombre del producto Información Citas de uso del producto Validaciones del producto
S1421 Staurosporine (STS) Staurosporine (STS) es un potente inhibidor de PKC para PKCα, PKCγ y PKCη con IC50 de 2 nM, 5 nM y 4 nM, menos potente para PKCδ (20 nM), PKCε (73 nM) y poco activo para PKCζ (1086 nM) en ensayos libres de células. Este compuesto también muestra actividades inhibidoras en otras quinasas, como PKA, PKG, S6K, CaMKII, etc. Fase 3.
Oncotarget, November 13, 2018, 35962-35973
Biochemical Journal, May 1, 2014, 513-524
Acta Pharmacologica Sinica, July 23, 2018, 1902-1912
Verified customer review of Staurosporine (STS)
S2163 PF-4708671 PF-4708671 es un inhibidor permeable a las células de la p70 ribosomal S6 kinase (isoforma S6K1) con un Ki/IC50 de 20 nM/160 nM en ensayos sin células, una selectividad 400 veces mayor para S6K1 que para S6K2, y una selectividad 4 y >20 veces mayor para S6K1 que para MSK1 y RSK1/2, respectivamente. Este compuesto induce Autophagy. Es el primer inhibidor específico de S6K1 en ser reportado.
Nutrition & Metabolism, May 2, 2018, 31
Frontiers in Physiology, March 29, 2019, 250
Molecular Cancer Therapeutics, March 2015, 799-809
Verified customer review of PF-4708671
S2843 BI-D1870 BI-D1870 es un inhibidor ATP-competitivo de la S6 quinasa ribosomal para RSK1/2/3/4 con una IC50 de 31 nM/24 nM/18 nM/15 nM en ensayos libres de células, respectivamente; 10 a 100 veces mayor selectividad para RSK que MST2, GSK-3β, MARK3, CK1 y Aurora B. Este compuesto exhibe atributos anticancerígenos incluyendo la generación de especies reactivas de oxígeno (ROS) y el aumento del estrés del retículo endoplásmico (RE) y la Autophagy.
J Biol Chem, 2025, 301(10):110643
Cells, 2024, 13(18)1546
Sci Rep, 2024, 14(1):9440
Verified customer review of BI-D1870
S7698 LY2584702 LY2584702 es un inhibidor selectivo de p70S6K, competitivo de ATP, con una IC50 de 4 nM.
Journal of Virology, June 1, 2020, e00387-20
Cancer Cell International, December 19, 2024, 409
PLoS One, August 9, 2017, e0182891
Verified customer review of LY2584702
S7704 LY2584702 Tosylate LY2584702 Tosylate es un inhibidor selectivo de p70S6K, competitivo de ATP, con una IC50 de 4 nM. Fase 1.
Blood Adv, 2024, 8(15):3880-3892
Cell, 2023, 186(24):5328-5346.e26
Cell, 2023, 10.1016/j.cell.2023.09.027
Verified customer review of LY2584702 Tosylate
S7870 LJH685 LJH685 es un potente inhibidor pan-RSK con IC50 de 6 nM, 5 nM y 4 nM para RSK1, RSK2 y RSK3, respectivamente.
Biol Pharm Bull, 2025, 48(2):172-176
Sci Adv, 2025, 11(36):eadw2568
Biological & Pharmaceutical Bulletin, 2025, 172-176
Verified customer review of LJH685
S7871 LJI308 LJI308 es un potente inhibidor pan-RSK (p90 ribosomal S6 quinasa) con IC50 de 6 nM, 4 nM y 13 nM para RSK1, RSK2 y RSK3, respectivamente.
Nat Commun, 2024, 15(1):2089
J Exp Clin Cancer Res, 2022, 41-1:256
Cell Rep, 2022, 41(11):111827
S0385 S6K-18 S6K-18 es un inhibidor altamente selectivo de la proteína ribosomal S6 quinasa beta-1 (S6K1, p70S6K, p70-S6K).
Nature Communications, 2024, 5292
Elife, 2024, 13RP92925
Item – Theses Canada, 2016,
S3940 3'-Hydroxypterostilbene El 3'-Hydroxypterostilbene (3'-HPT) es uno de los componentes activos de Sphaerophysa salsula y Pterocarpus marsupium que puede ser útil en el tratamiento de diferentes tipos de neoplasias hematológicas. Este compuesto, un análogo natural del pterostilbeno, inhibe eficazmente el crecimiento de las células de cáncer de colon humano (IC50s de 9.0, 40.2 y 70.9 µM para las células COLO 205, HCT-116 y HT-29, respectivamente) al inducir la apoptosis y la autofagia. Inhibe las vías PI3K/Akt/mTOR/p70S6K y p38 MAPK y activa las vías ERK1/2, JNK1/2 MAPK.
Int J Mol Sci, 2024, 25(18)9990
International Journal of Molecular Sciences, 2024, 9990
Human Molecular Genetics, 2024, 2133–2144
E1754 BRD7389 BRD7389 es un inhibidor de las quinasas de la familia RSK con CI50 de 1,5 μM, 2,4 μM y 1,2 μM para RSK1, RSK2 y RSK3, respectivamente. Este compuesto también aumenta la expresión génica específica de las células β en las células de islotes humanos primarios.

The 70 kDa ribosomal protein S6 kinase (p70 S6K) is a serine/threonine kinase. There are two highly homologous members in S6K family, which are named as S6K1 and S6K2, respectively. Both S6Ks belong to the AGC family of serine/threonine kinases and they could be activated in response to many stimulus, like growth factors, insulin and cytokines. In turn, S6Ks phosphorylate its substrates including the ribosomal protein S6, elF4B, and SKAR. It was found that the activity of S6Ks could be controlled by mammalian target of rapamycin (mTOR) [2]. And then, direct phosphorylation of S6K1 by mTOR was confirmed [3; 4]. Therefore, the activity of S6K presented sensitive to rapamycin [8]. However, the sensitivity of S6Ks to rapamycin was found always changing. S6Ks became insensitive to rapamycin when the site T412 was phosphorylated [9]. Until recently, raptor has been proved to be responsible for T412 phosphorylation [6]. Besides, S6K−/− animals showed short-lived and were much smaller than wild type animals. A study suggested that this phenomenon was due to the control of S6K on cell growth rather than proliferation [5]. To date, S6Ks are also related to many serious diseases. For example, S6K1 showed overexpression in breast cancer patients [1]. With the understanding of the importance of S6K in human diseases, the demand for S6K-specific inhibitors increased rapidly. Fortunately, a novel inhibitor specific for S6K1, PF-4708671, was developed to facilitate the study of the functions of S6K1, at the same time, and S6K2 [7].