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S6 Kinase Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S2163 | PF-4708671 | PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. This compound induces autophagy. It is the first S6K1-specific inhibitor to be reported. |
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| S2843 | BI-D1870 | BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. This compound exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy. |
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| S7698 | LY2584702 | LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. |
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| S7704 | LY2584702 Tosylate | LY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1. |
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| S7870 | LJH685 | LJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively. |
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| S7871 | LJI308 | LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. |
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| S0385 | S6K-18 | S6K-18 is a highly selective inhibitor of ribosomal protein S6 kinase beta-1 (S6K1, p70S6K, p70-S6K). |
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| S3940 | 3'-Hydroxypterostilbene | 3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies. This compound, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. It inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways. |
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| E1754 | BRD7389 | BRD7389 is an inhibitor of RSK family kinases with IC50 of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. This compound also increases β-cell–specific gene expression in primary human islet cells. | ||
| E4345 | L-Norvaline | L-Norvaline is a non-proteinogenic amino acid, an isomer of valine, and an inhibitor of arginase and p70 ribosomal S6 kinase 1 (p70S6K1) kinase. L-norvaline enhances NO production from activated macrophages. | ||
| E4690New | Gingerenone A | Gingerenone A is a a polyphenol present in ginger, an inhibitor of p70 S6 (S6K1) and an activator of Nrf2-Gpx4 signaling pathway to alleviate ferroptosis in secondary liver injury in colitis. It exhibits anti-adipogenic, anti-lipogenic, anti-hyperglycemic, anti-obesity, and anti-inflammatory effects, and holds promise for research into anti-diabetic and anti-obesity drug development. | ||
| S1582 | H-89 Dihydrochloride | H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy. |
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| S1421 | Staurosporine (STS) | Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. This compound also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. |
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| S1014 | SKI-606 (Bosutinib) | Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy. |
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| S1558 | AT7867 | AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM in cell-free assays, respectively; this compound shows little activity outside the AGC kinase family. |
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| S6385 | Prexasertib (LY2606368) |
Prexasertib (LY2606368, ACR 368) is a selective ATP competitor inhibitor of Chk1 and Chk2 with IC50s of 1 nM and 8 nM in cell-free assays, respectively. It also inhibits RSK1 with an IC50 of 9 nM in cell-free assay. |
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| S7563 | AT13148 | AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1. |
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| S8518 | AD80 | AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but was much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM. |
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| S7752 | Pluripotin (SC1) | Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP that maintains embryonic stem cell (ESC) self-renewal. It also inhibits RSK1, RSK2, RSK3 and RSK4 with IC50 of 0.5 µM, 2.5 µM, 3.3 µM and 10.0 µM, respectively. |
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