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S6 Kinase

In molecular biology, 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.

  • BI-D1870
    T6171501437-28-1
    BI-D1870 is a cell-permeable, ATP-competitive inhibitor of ribosomal S6 kinases (RSKs; IC50s: 31/24/18/15 nM for RSK1/2/3/4).
    • $48
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  • Lenaldekar
    T24398418800-15-4
    Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase/AKT/mTOR pathway and delays sensitive cells in late mitosis.
    • $148
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  • MBM-55S
    T119612083624-07-9In house
    MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.
    • $195
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  • FMK
    TQ0310821794-92-7In house
    FMK is an irreversible inhibitor of RSK2 kinase.
    • $68
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  • GSK-25
    T4488874119-56-9
    GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).
    • $39
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  • AD80
    T43011384071-99-1
    AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
    • $39
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  • H-89 dihydrochloride
    T6250130964-39-5
    H-89 dihydrochloride (5-Isoquinolinesulfonamide) is a potent inhibitor of protein kinase A (PKA; IC50: 0.14 μM, Ki: 48 nM).
    • $33
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  • BIX 02565
    T54281311367-27-7
    BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM).
    • $56
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  • Eudesmin
    T3836526-06-7
    Eudesmin shows antiinflammatory, neuritogenic, anticonvulsant and sedative effects, the mechanism of eudesmin may be related to up-regulation of GABAA and GAD65 expressions, and anti-apoptosis of neuron the in brain.50 microM (+)-eudesmin can induce neurite outgrowth and enhance nerve growth factor (NGF)-mediated neurite outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways.
    • $142
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  • LY-2584702 tosylate salt
    T17461082949-68-5
    LY-2584702 tosylate salt is a selective, ATP-competitive p70S6K inhibitor, used in trials studying the treatment of cancer.
    • $31
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  • Carnosol
    T6S13025957-80-2
    Carnosol is an Nrf2 activator, increasing Nrf2 levels and promoting heme oxygenase 1 (HMOX1) expression. It is a ribosomal S6 kinase (RSK2) inhibitor and can be used in gastric cancer-related research with an IC50 value of approximately 5.5 μM.
    • $39
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  • Quercitrin
    T2871522-12-3
    Quercitrin (3-rhamnosyl quercetin) is a plant-derived flavonoid compound, displays antioxidant and anti-inflammatory activities. Quercitrin can be found in a number of food items such as garden tomato (var. ), German camomile, endive, and kiwi, which makes quercitrin a potential biomarker for the consumption of these food products.
    • $42
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  • GSK269962A
    T3518850664-21-0
    GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
    • $36
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  • SL 0101-1
    T1689677307-50-7
    SL 0101-1 (SL0101) is a selective, efficient, reversible and ATP-competitive inhibitor of p90 ribosomal S6 kinase (RSK) that can permeate cell membranes, with an IC50 value of 89 nM for RSK.SL 0101-1 (SL0101) is also a potent RSK1/2 inhibitor with a Ki value of 1 μM. SL 0101-1 (SL0101) is also a potent RSK1/2 inhibitor with a Ki value of 1 μM.
    • $143
    35 days
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  • Bisindolylmaleimide V
    T7790113963-68-1
    Bisindolylmaleimide V, a bisindolylmaleimide derivative, is an inactive of a kinase inhibitor.
    • $68
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  • LJI308
    T68781627709-94-7
    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.
    • $38
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  • CHIR 98024
    T3074556813-39-9
    CHIR 98024 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.
    • $37
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  • Gossypin
    TN1712652-78-8
    Gossypin has antidiabetic, antioxdiant, anticonvulsant, anti-allergic, antiinflammatory, antinociceptive, cytotoxic and antibacterial activities; it inhibits the NF-kappaB activation pathway, which may explain its role in the suppression of inflammation,
    • $139
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  • Bimiralisib
    T22651225037-39-7
    Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.
    • $36
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  • Prexasertib dihydrochloride
    T43271234015-54-3
    Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.
    • $38
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  • Sodium salicylate
    T033554-21-7
    Sodium salicylate (2-Hydroxybenzoic acid sodium salt), a metabolite of acetylsalicylic acid, can inhibit NF-kB and reduce oxidative stress.
    • $45
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  • CHIR-98014
    T2608252935-94-7
    CHIR-98014 (CT98014) is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
    • $68
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  • LY-2584702 free base
    T61591082949-67-4
    LY2584702 is a selective, ATP-competitive p70S6K inhibitor(IC50: 4 nM).
    • $39
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  • AT13148
    T24821056901-62-2
    AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
    • $41
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  • BRD7389
    T14779376382-11-5
    BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.
    • $77
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  • PF-4708671
    T20021255517-76-0
    PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) .In cell-free assays, PF-4708671(PF4708671) is potent for S6K1(Ki50=20 nM, IC50=160 nM).
    • $47
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  • CYC-116
    T6458693228-63-6
    CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
    • $33
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  • CCT128930
    T6303885499-61-6
    CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.
    • $47
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  • GSK1838705A
    T30791116235-97-2
    GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases.
    • $34
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  • S6K-18
    T224221265789-88-5
    S6K-18, a highly selective S6K1 inhibitor, inhibits S6K1 with IC50 of 52nM.
    • $59
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  • CKI-7
    T199131177141-67-1
    CKI-7 is a potent and ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.
    • $193
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  • AT7867
    T6304857531-00-1
    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, respectively; little activity outside the AGC kinase family.
    • $44
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  • LJH685
    T68771627710-50-2
    LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 nM).
    • $33
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  • Vistusertib
    T19611009298-59-2
    Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
    • $43
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  • LY-2584702 hydrochloride
    T119001082948-81-9
    Ly-2584702 hydrochloride is a p70S6K selective ATP competitive inhibitor with IC50 of 4 nM.In the S6K1 enzyme assay, the IC50 of LY-2584702 was 2 nM.
    • $1,520
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  • Pluripotin
    T6948839707-37-8
    Pluripotin (SC1) (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.
    • $30
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  • A-443654
    T14072552325-16-3
    A-443654 is a pan-Akt inhibitor. A-443654 has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
    • $84
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  • MBM-55
    T119602083622-09-5
    MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
    • $187
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