S6 Kinase

シグナル伝達経路

S6 Kinaseシグナル伝達経路

S6 Kinase製品

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  • S6 Kinase阻害剤 (18)
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S1582 H 89 2HCl 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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Commun Signal, 2024, 22(1):48
iScience, 2024, 27(3):109125
S1421 Staurosporine (STS) スタウロスポリン (Staurosporine (AM-2282、Antiviotic AM-2282、STS)) は、PKCα、PKCγ、および PKCη に対する強力な PKC 阻害剤であり、IC50 は 2 nM、5 nM、および 4 nM です。 無細胞アッセイでは、PKCδ (20 nM)、PKCε (73 nM) に対して効力が低く、PKCζ (1086 nM) に対してほとんど活性がありません。 また、PKA、PKG、S6K、CaMKII などの他のキナーゼに対しても阻害活性を示します。臨床フェーズ3。
Nat Commun, 2024, 15(1):489
Nat Commun, 2024, 15(1):1300
Mol Syst Biol, 2024, 20(1):28-55
S1014 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.
Heliyon, 2024, 10(1):e23690
Mol Cell, 2023, 83(5):803-818.e8
Cancer Res, 2023, 83(1):141-157
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. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
BMC Cancer, 2024, 24(1):233
Leukemia, 2023, 37(8):1611-1625
Leukemia, 2023, 37(8):1611-1625
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. First S6K1-specific inhibitor to be reported.
Adv Sci (Weinh), 2023, 10(3):e2203718
Nucleic Acids Res, 2023, 51(22):12076-12091
CNS Neurosci Ther, 2023, 10.1111/cns.14475
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; little activity outside the AGC kinase family.
Exp Gerontol, 2023, 173:112091
Cancers (Basel), 2022, 14(21)5215
Cancers (Basel), 2021, 13(6)1205
S7698 LY2584702 LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
ACS Bio Med Chem Au, 2023, 3(3):283-294
Nature, 2022, 609(7929):975-985
Nat Commun, 2022, 13(1):4848
S7704 LY2584702 Tosylate LY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
Cell, 2023, 10.1016/j.cell.2023.09.027
Nat Commun, 2022, 13(1):4848
Cancer Res, 2022, can.21.2908
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.
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Cancers (Basel), 2022, 14(23)5943
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
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. Prexasertib also inhibits RSK1 with an IC50 of 9 nM in cell-free assay.
EMBO Mol Med, 2023, e16431.
EBioMedicine, 2023, 95:104752
J Biol Chem, 2023, S0021-9258(23)01969-5
S8518 AD80 AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.
Nat Commun, 2022, 13(1):2500
Mol Cancer Res, 2020, 18(8):1176-1188
Mol Cancer Res, 2020, 1176-1188
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.
J Exp Clin Cancer Res, 2022, 41-1:256
Cell Rep, 2022, 41(11):111827
Transl Psychiatry, 2022, 12(1):458
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.
Cell Rep, 2022, 38(11):110522
Front Mol Biosci, 2022, 9:1030725
Mol Cell, 2021, S1097-2765(21)00736-X
S7752 Pluripotin (SC1) Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Maintains embryonic stem cell (ESC) self-renewal. Pluripotin also inhibits RSK1, RSK2, RSK3 and RSK4 with IC50 of 0.5 µM, 2.5 µM, 3.3 µM and 10.0 µM, respectively.
Antiviral Res, 2018, 157:57-67
Reprod Domest Anim, 2018, 53(5):1052-1059
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.
E1754New 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. BRD7389 also increases β-cell–specific gene expression in primary human islet cells. 
S0385 S6K-18 S6K-18 is a highly selective inhibitor of ribosomal protein S6 kinase beta-1 (S6K1, p70S6K, p70-S6K).
Item – Theses Canada, 2016,
E4345New 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.
S1582 H 89 2HCl 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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Commun Signal, 2024, 22(1):48
iScience, 2024, 27(3):109125
S1421 Staurosporine (STS) スタウロスポリン (Staurosporine (AM-2282、Antiviotic AM-2282、STS)) は、PKCα、PKCγ、および PKCη に対する強力な PKC 阻害剤であり、IC50 は 2 nM、5 nM、および 4 nM です。 無細胞アッセイでは、PKCδ (20 nM)、PKCε (73 nM) に対して効力が低く、PKCζ (1086 nM) に対してほとんど活性がありません。 また、PKA、PKG、S6K、CaMKII などの他のキナーゼに対しても阻害活性を示します。臨床フェーズ3。
Nat Commun, 2024, 15(1):489
Nat Commun, 2024, 15(1):1300
Mol Syst Biol, 2024, 20(1):28-55
S1014 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.
Heliyon, 2024, 10(1):e23690
Mol Cell, 2023, 83(5):803-818.e8
Cancer Res, 2023, 83(1):141-157
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. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
BMC Cancer, 2024, 24(1):233
Leukemia, 2023, 37(8):1611-1625
Leukemia, 2023, 37(8):1611-1625
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. First S6K1-specific inhibitor to be reported.
Adv Sci (Weinh), 2023, 10(3):e2203718
Nucleic Acids Res, 2023, 51(22):12076-12091
CNS Neurosci Ther, 2023, 10.1111/cns.14475
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; little activity outside the AGC kinase family.
Exp Gerontol, 2023, 173:112091
Cancers (Basel), 2022, 14(21)5215
Cancers (Basel), 2021, 13(6)1205
S7698 LY2584702 LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
ACS Bio Med Chem Au, 2023, 3(3):283-294
Nature, 2022, 609(7929):975-985
Nat Commun, 2022, 13(1):4848
S7704 LY2584702 Tosylate LY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
Cell, 2023, 10.1016/j.cell.2023.09.027
Nat Commun, 2022, 13(1):4848
Cancer Res, 2022, can.21.2908
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.
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Cancers (Basel), 2022, 14(23)5943
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
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. Prexasertib also inhibits RSK1 with an IC50 of 9 nM in cell-free assay.
EMBO Mol Med, 2023, e16431.
EBioMedicine, 2023, 95:104752
J Biol Chem, 2023, S0021-9258(23)01969-5
S8518 AD80 AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.
Nat Commun, 2022, 13(1):2500
Mol Cancer Res, 2020, 18(8):1176-1188
Mol Cancer Res, 2020, 1176-1188
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.
J Exp Clin Cancer Res, 2022, 41-1:256
Cell Rep, 2022, 41(11):111827
Transl Psychiatry, 2022, 12(1):458
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.
Cell Rep, 2022, 38(11):110522
Front Mol Biosci, 2022, 9:1030725
Mol Cell, 2021, S1097-2765(21)00736-X
S7752 Pluripotin (SC1) Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Maintains embryonic stem cell (ESC) self-renewal. Pluripotin also inhibits RSK1, RSK2, RSK3 and RSK4 with IC50 of 0.5 µM, 2.5 µM, 3.3 µM and 10.0 µM, respectively.
Antiviral Res, 2018, 157:57-67
Reprod Domest Anim, 2018, 53(5):1052-1059
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.
E1754New 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. BRD7389 also increases β-cell–specific gene expression in primary human islet cells. 
S0385 S6K-18 S6K-18 is a highly selective inhibitor of ribosomal protein S6 kinase beta-1 (S6K1, p70S6K, p70-S6K).
Item – Theses Canada, 2016,
E4345New 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.
E1754New 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. BRD7389 also increases β-cell–specific gene expression in primary human islet cells. 
E4345New 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.

S6 Kinase阻害剤の選択性比較

Tags: S6 Kinase inhibitor|S6 Kinase agonist|S6 Kinase activator|S6 Kinase inducer|S6 Kinase antagonist|S6 Kinase signaling pathway|S6 Kinase assay kit