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. |
-
Nat Commun, 2024, 15(1):8887
-
J Extracell Vesicles, 2024, 13(4):e12426
-
J Extracell Vesicles, 2024, 13(4):e12426
|
|
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):3816
-
Nat Commun, 2024, 15(1):3816
|
|
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. |
-
Elife, 2024, 12RP92324
-
Front Immunol, 2024, 15:1425670
-
PLoS Pathog, 2024, 20(7):e1012170
|
|
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. |
-
Cells, 2024, 13(18)1546
-
Sci Rep, 2024, 14(1):9440
-
BMC Cancer, 2024, 24(1):233
|
|
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. |
-
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
-
Int J Mol Sci, 2024, 25(7)3944
-
Am J Cancer Res, 2024, 14(3):1087-1100
|
|
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
-
Oncoimmunology, 2021, 10(1):1943234
|
|
S7698 |
LY2584702
|
LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
|
-
Mol Cell, 2024, S1097-2765(24)00832-3
-
Am J Cancer Res, 2024, 14(3):1087-1100
-
ACS Bio Med Chem Au, 2023, 3(3):283-294
|
|
S7704 |
LY2584702 Tosylate
|
LY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
|
-
Blood Adv, 2024, 8(15):3880-3892
-
Cell, 2023, 186(24):5328-5346.e26
-
Cell, 2023, 10.1016/j.cell.2023.09.027
|
|
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. |
-
Nat Commun, 2024, 15(1):2089
-
Cell Death Dis, 2024, 15(4):274
-
Cell Death Discov, 2024, 10(1):278
|
|
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.
|
-
Nat Commun, 2024, 15(1):2089
-
J Exp Clin Cancer Res, 2022, 41-1:256
-
Cell Rep, 2022, 41(11):111827
|
|
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. |
-
J Clin Biochem Nutr, 2024, 74(2):97-107
-
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. |
-
Int J Mol Sci, 2024, 25(18)9990
|
|
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). |
-
Elife, 2024, 13RP92925
-
Item – Theses Canada, 2016,
|
|
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. |
|
|
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. |
- Nat Commun, 2024, 15(1):8887
- J Extracell Vesicles, 2024, 13(4):e12426
- J Extracell Vesicles, 2024, 13(4):e12426
|
|
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):3816
- Nat Commun, 2024, 15(1):3816
|
|
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. |
- Elife, 2024, 12RP92324
- Front Immunol, 2024, 15:1425670
- PLoS Pathog, 2024, 20(7):e1012170
|
|
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. |
- Cells, 2024, 13(18)1546
- Sci Rep, 2024, 14(1):9440
- BMC Cancer, 2024, 24(1):233
|
|
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. |
- Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
- Int J Mol Sci, 2024, 25(7)3944
- Am J Cancer Res, 2024, 14(3):1087-1100
|
|
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
- Oncoimmunology, 2021, 10(1):1943234
|
|
S7698 |
LY2584702
|
LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
|
- Mol Cell, 2024, S1097-2765(24)00832-3
- Am J Cancer Res, 2024, 14(3):1087-1100
- ACS Bio Med Chem Au, 2023, 3(3):283-294
|
|
S7704 |
LY2584702 Tosylate
|
LY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
|
- Blood Adv, 2024, 8(15):3880-3892
- Cell, 2023, 186(24):5328-5346.e26
- Cell, 2023, 10.1016/j.cell.2023.09.027
|
|
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. |
- Nat Commun, 2024, 15(1):2089
- Cell Death Dis, 2024, 15(4):274
- Cell Death Discov, 2024, 10(1):278
|
|
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.
|
- Nat Commun, 2024, 15(1):2089
- J Exp Clin Cancer Res, 2022, 41-1:256
- Cell Rep, 2022, 41(11):111827
|
|
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. |
- J Clin Biochem Nutr, 2024, 74(2):97-107
- 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. |
- Int J Mol Sci, 2024, 25(18)9990
|
|
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). |
- Elife, 2024, 13RP92925
- Item – Theses Canada, 2016,
|
|
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. |
|
|