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BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells .
BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively .
Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 µM, respectively.
LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation .
LJH685 is a potent, ATP-competitive and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively .
SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM . SL 0101-1 (SL0101) is a selective RSK1/2 inhibitor, with a Ki of 1 μM .
S6 Kinase Substrate Peptide 32 is a substrate of Ribosomal S6 Kinase (RSK). S6 Kinase Substrate Peptide 32 can be used to measure the activity of RSKs which phosphorylate ribosomal protein S6 .
ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2 .
Magnolin, a major component of Magnolia liliiflora, inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
PV1115 is a potent and highly selective Chk2 inhibitor with an IC50 of 0.14 nM, 66000 nM, >100000 nM for Chk2, Chk1 and RSK2, respectively. PV1115 is situated within the ATP-binding pocket of Chk2 .
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM . Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1) .
Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
SB-747651A is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A can be used for inflammation research .
SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research .
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research .
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis .
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity .
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity .
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity .
Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity .
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity .
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice .
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells .
SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines .
MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers.
MCE designs a unique collection of 510 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.
S6 Kinase Substrate Peptide 32 is a substrate of Ribosomal S6 Kinase (RSK). S6 Kinase Substrate Peptide 32 can be used to measure the activity of RSKs which phosphorylate ribosomal protein S6 .
SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM . SL 0101-1 (SL0101) is a selective RSK1/2 inhibitor, with a Ki of 1 μM .
Magnolin, a major component of Magnolia liliiflora, inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM . Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1) .
RSK4 protein, a constitutively active serine/threonine-protein kinase, demonstrates growth-factor-independent kinase activity and is implicated in p53/TP53-dependent cell growth arrest signaling. It may play an inhibitory role during embryogenesis. RSK4 Protein, Human (sf9, GST) is the recombinant human-derived RSK4 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of RSK4 Protein, Human (sf9, GST) is 745 a.a., with molecular weight of ~110 kDa.
RSK3, a kinase downstream of ERK signaling, crucially mediates mitogenic and stress-induced transcription factor activation. It regulates translation, impacting proliferation, survival, and differentiation. In epithelial ovarian cancer cells, RSK3 may act as a tumor suppressor, highlighting its diverse roles in cellular homeostasis and potential implications in cancer biology. RSK3 Protein, Human (sf9, GST) is the recombinant human-derived RSK3 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of RSK3 Protein, Human (sf9, GST) is 733 a.a., with molecular weight of ~110 kDa.
RSK2 is a kinase downstream of ERK signaling and plays a critical role in mediating mitosis and stress responses. It activates transcription factors (CREB1, ETV1, NR4A1), affecting proliferation, survival and differentiation. RSK2 Protein, Human is the recombinant human-derived RSK2 protein, expressed by E. coli , with tag free. The total length of RSK2 Protein, Human is 341 a.a., .
RSK2 is a kinase downstream of ERK signaling and plays a critical role in mediating mitosis and stress responses. It activates transcription factors (CREB1, ETV1, NR4A1), affecting proliferation, survival and differentiation. RSK2 Protein, Human (His) is the recombinant human-derived RSK2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of RSK2 Protein, Human (His) is 341 a.a., .
RSK1 is a kinase downstream of ERK signaling and is critical for mitosis and stress-induced responses. It activates transcription factors (CREB1, ETV1, NR4A1), affecting proliferation, survival and differentiation. RSK1 Protein, Human (Sf9) is the recombinant human-derived RSK1 protein, expressed by Sf9 insect cells , with tag free. The total length of RSK1 Protein, Human (Sf9) is 321 a.a., .
RSK1 is a kinase downstream of ERK signaling and is critical for mitosis and stress-induced responses. It activates transcription factors (CREB1, ETV1, NR4A1), affecting proliferation, survival and differentiation. RSK1 Protein, Human (Sf9, His) is the recombinant human-derived RSK1 protein, expressed by Sf9 insect cells , with N-8*His labeled tag. The total length of RSK1 Protein, Human (Sf9, His) is 321 a.a., .
RPS6KA5; Ribosomal protein S6 kinase alpha-5; S6K-alpha-5; 90 kDa ribosomal protein S6 kinase 5; Nuclear mitogen- and stress-activated protein kinase 1; RSK-like protein kinase; RSKL
MSK1 is a serine/threonine protein kinase that centralizes multiple cellular processes by phosphorylating key transcription factors. In response to stimuli such as UV-C irradiation, EGF, and anisomycin, MSK1 activates CREB1 and ATF1, affecting gene expression through histone phosphorylation. MSK1 Protein, Human (Sf9, GST) is the recombinant human-derived MSK1 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of MSK1 Protein, Human (Sf9, GST) is 801 a.a., .
RSK1 p90 Antibody (YA088) is a non-conjugated and Rabbit origined monoclonal antibody about 83 kDa, targeting to RSK1 p90. It can be used for WB,ICC,IHC-P,FC assays with tag free, in the background of Human, Mouse, Rat.
Phospho-RSK4 (Ser232) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 84 kDa, targeting to Phospho-RSK4 (Ser232). It can be used for WB,ICC/IF assays with tag free, in the background of Human.
RPS6KA3; ISPK1; MAPKAPK1B; RSK2; Ribosomal protein S6 kinase alpha-3; S6K-alpha-3; 90 kDa ribosomal protein S6 kinase 3; p90-RSK 3; p90RSK3; Insulin-stimulated protein kinase 1; ISPK-1; MAP kinase-activated protein kinase 1b; MAPK-activated
WB, IP
Human, Mouse, Rat
Phospho-RSK2 (Ser227) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 84 kDa, targeting to Phospho-RSK2 (Ser227). It can be used for WB,IP assays with tag free, in the background of Human, Mouse, Rat.
RPS6KA2; MAPKAPK1C; RSK3; Ribosomal protein S6 kinase alpha-2; S6K-alpha-2; 90 kDa ribosomal protein S6 kinase 2; p90-RSK 2; p90RSK2; MAP kinase-activated protein kinase 1c; MAPK-activated protein kinase 1c; MAPKAP kinase 1c; MAPKAPK-1c; Ri
WB, IHC-F, IHC-P, ICC/IF, IP
Human, Hamster
RSK3 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 83 kDa, targeting to RSK3. It can be used for WB,IHC-F,IHC-P,ICC/IF,IP assays with tag free, in the background of Human, Hamster.
RPS6KA1; MAPKAPK1A; RSK1; Ribosomal protein S6 kinase alpha-1; S6K-alpha-1; 90 kDa ribosomal protein S6 kinase 1; p90-RSK 1; p90RSK1; p90S6K; MAP kinase-activated protein kinase 1a; MAPK-activated protein kinase 1a; MAPKAP kinase 1a; MAPKAP
WB, ICC/IF, IP
Human, Rat, Mouse
Phospho-RSK1 p90 (Ser380) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 83 kDa, targeting to Phospho-RSK1 p90 (Ser380). It can be used for WB, ICC/IF, IP assays with tag free, in the background of Human, Mouse and Rat.
RPS6KA1; MAPKAPK1A; RSK1; Ribosomal protein S6 kinase alpha-1; S6K-alpha-1; 90 kDa ribosomal protein S6 kinase 1; p90-RSK 1; p90RSK1; p90S6K; MAP kinase-activated protein kinase 1a; MAPK-activated protein kinase 1a; MAPKAP kinase 1a; MAPKAP
WB, IP
Human, Mouse, Monkey
RSK1 p90 Antibody (YA676) is a non-conjugated and Mouse origined monoclonal antibody about 83 kDa, targeting to RSK1 p90 (6B9). It can be used for WB,IP assays with tag free, in the background of Human, Mouse, Monkey.
RPS6KA1; MAPKAPK1A; RSK1; Ribosomal protein S6 kinase alpha-1; S6K-alpha-1; 90 kDa ribosomal protein S6 kinase 1; p90-RSK 1; p90RSK1; p90S6K; MAP kinase-activated protein kinase 1a; MAPK-activated protein kinase 1a; MAPKAP kinase 1a; MAPKAP
WB, IP
Human, Mouse, Rat
Phospho-RSK1 p90 (Thr359/Ser363) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 83 kDa, targeting to Phospho-RSK1 p90 (Thr359/Ser363). It can be used for WB,IP assays with tag free, in the background of Human, Mouse, Rat.
RPS6KA5; MSK1; Ribosomal protein S6 kinase alpha-5; S6K-alpha-5; 90 kDa ribosomal protein S6 kinase 5; Nuclear mitogen- and stress-activated protein kinase 1; RSK-like protein kinase; RSKL
WB, ICC/IF, IP
Human, Mouse, Rat, Hamster
Phospho-MSK1 (Ser360) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 90 kDa, targeting to Phospho-MSK1 (Ser360). It can be used for WB,ICC/IF,IP assays with tag free, in the background of Human, Mouse, Rat, Hamster.
RPS6KA5; MSK1; Ribosomal protein S6 kinase alpha-5; S6K-alpha-5; 90 kDa ribosomal protein S6 kinase 5; Nuclear mitogen- and stress-activated protein kinase 1; RSK-like protein kinase; RSKL
WB, IHC-P, IP
Human, Rat
Phospho-MSK1 (Ser376) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 90 kDa, targeting to Phospho-MSK1 (Ser376). It can be used for WB,IHC-P,IP assays with tag free, in the background of Human, Rat.
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