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MAPK Filter
MAPKS6 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.
Carnosol
Cited
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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CitedMBM-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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Vistusertib
Cited
T19611009298-59-2
Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
- $31
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CitedGossypin
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,
- $30
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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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BI-D1870 Cited
T6171501437-28-1
BI-D1870 is a highly specific, blood-brain-permeable, and ATP-competitive inhibitor of the N-terminal AGC kinase domain of RSK, with IC50 values of 31 nM, 24 nM, 18 nM, and 15 nM for RSK1, RSK2, RSK3, and RSK4.
- $48
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CitedH-89 dihydrochloride Cited
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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CitedQuercitrin Cited
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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CitedGSK269962A Cited
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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CitedAT13148
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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A-443654
T14072552325-16-3
A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).
- $84
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AD80 Cited
T43011384071-99-1
AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.
- $39
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Citedcct128930
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.
- $35
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BIX 02565 Cited
T54281311367-27-7In house
BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM).
- $76
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CitedCYC-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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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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AT7867
T6304857531-00-1
AT7867 is a potent ATP-competitive inhibitor of Akt1 2 3 and p70S6K PKA with IC50 values of 32 nM, 17 nM, 47 nM, 85 nM, and 20 nM, respectively, exhibiting little activity outside the AGC kinase family.
- $37
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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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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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LY-2584702 free base
T61591082949-67-4
LY2584702 is a selective, ATP-competitive p70S6K inhibitor(IC50: 4 nM).
- $39
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gsk-25 Cited
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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CitedCHIR-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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LJH685
T68771627710-50-2
LJH685 is an effective pan-RSK inhibitor for RSK1 2 3 (IC50: 6 5 4 nM).
- $31
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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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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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Eudesmin Cited
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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CitedSodium 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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LY-2584702 tosylate salt Cited
T17461082949-68-5
LY-2584702 tosylate salt, a selective ATP-competitive p70S6K inhibitor, is being used in clinical trials for cancer treatment.
- $31
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Citedchir 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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s6k-18
T224221265789-88-5
S6K-18, a highly selective S6K1 inhibitor, inhibits S6K1 with IC50 of 52nM.
- $35
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BRD7389 Cited
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.
- $29
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CitedLJI308 Cited
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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CitedBimiralisib
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.
- $30
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CKI-7
T199131177141-67-1
CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. It also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.
- $116
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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.
- $89
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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.
- $198
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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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