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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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