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Pathways Recommended: MAPK/ERK Pathway
Results for "

ERK phosphorylation

" in MedChemExpress (MCE) Product Catalog:

121

Inhibitors & Agonists

1

Biochemical Assay Reagents

14

Peptides

3

Inhibitory Antibodies

18

Natural
Products

2

Isotope-Labeled Compounds

4

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P3751
    [Tyr8] Bradykinin

    		Bradykinin Receptor ERK Cardiovascular Disease Endocrinology
    [Tyr8] Bradykinin is a B2 kinin receptor agonist. [Tyr8] Bradykinin also stimulates ERK1/2 phosphorylation. [Tyr8] Bradykinin can be used as an internal standard .
    [Tyr8] Bradykinin
  • HY-114436
    MRTX-1257
    3 Publications Verification

    		 Ras Cancer
    MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
    MRTX-1257
  • HY-124097
    HNMPA-(AM)3

    		Insulin Receptor Metabolic Disease
    HNMPA-(AM)3 is a cell-permeable and selective insulin receptor tyrosine kinase inhibitor analog of HNMPA. HNMPA-(AM)3 greatly inhibits the ability of prothoracicotropic hormone (PTTH) to activate ERK phosphorylation and stimulate ecdysteroidogenesis. HNMPA-(AM)3 is also effective in inhibiting ecdysteroid production (IC50=14.2 μM) and insulin receptor activity (IC50 is 14.2 μM and 200 μM in mosquitoes and mammals, respectively) .
    HNMPA-(AM)3
  • HY-157787
    Ginkgolic acid 2-phosphate

    		LPL Receptor Neurological Disease
    Ginkgolic acid 2-phosphate is a potent sphingosine 1-phosphate agonist. Ginkgolic acid 2-phosphate induces ERK phosphorylation. Ginkgolic acid 2-phosphate interactes with S1P1 .
    Ginkgolic acid 2-phosphate
  • HY-146319
    MIF-IN-6

    		Macrophage migration inhibitory factor (MIF) Metabolic Disease Inflammation/Immunology Cancer
    MIF-IN-6 (compound 2d) is a potent macrophage migration inhibitory factor (MIF) inhibitor with an IC50 of 1.4 μM and a Ki value of 0.96 μM, respectively. MIF-IN-6 attenuates MIF-induced ERK phosphorylation and inhibits proliferation of A549 cells .
    MIF-IN-6
  • HY-114436S
    MRTX-1257-d6

    		Isotope-Labeled Compounds Cancer
    MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
    MRTX-1257-d6
  • HY-113592
    ERK-IN-4

    		ERK Cancer
    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 .
    ERK-IN-4
  • HY-123938
    Risovalisib

    CYH33

    		 PI3K Cancer
    Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors .
    Risovalisib
  • HY-123938A
    CYH33 methanesulfonate

    		PI3K Cancer
    CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors .
    CYH33 methanesulfonate
  • HY-18849
    ERK2-IN-3

    ERK2-IN-3 (compound 2) is a inhibitor of ERK2, and inhibits Erk2 WT and Erk2 DS1 activation loop phosphorylation, with IC50 of 5 μM and 42 nM, respectively .
    ERK2-IN-3
  • HY-P5977
    STE-MEK1(13)

    Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide

    		 ERK Cancer
    STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH?) is a cell permeable ERK1/2 inhibitor (IC50: 13-30?μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
    STE-MEK1(13)
  • HY-122246
    ML192

    		GPR55 PKC ERK Arrestin Metabolic Disease
    ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation .
    ML192
  • HY-124740
    ML00253764

    		Melanocortin Receptor Cancer
    ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity .
    ML00253764
  • HY-N9725
    16-Hydroxycleroda-3,13-dien-15,16-olide

    16ξ-Hydroxycleroda-3,13-dien-15,16-olide

    		 Dipeptidyl Peptidase Metabolic Disease
    16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy .
    16-Hydroxycleroda-3,13-dien-15,16-olide
  • HY-50706
    Selumetinib
    Maximum Cited Publications
    57 Publications Verification

    AZD6244; ARRY-142886

    		 MEK Apoptosis Cancer
    Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
    Selumetinib
  • HY-108330
    AG126
    2 Publications Verification

    Tyrphostin AG126

    		 ERK Inflammation/Immunology
    AG126 is a tyrosine kinase inhibitor, can inhibit the phosphorylation of ERK1 and ERK2 at 25-50 μM. AG126 can be used in meiosis, mitosis, and postmitotic research .
    AG126
  • HY-50706A
    Selumetinib sulfate
    Maximum Cited Publications
    57 Publications Verification

    AZD6244 sulfate; ARRY-142886 sulfate

    		 MEK Apoptosis Cancer
    Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
    Selumetinib sulfate
  • HY-N2858
    Alpinumisoflavone acetate

    		Apoptosis Cancer
    Alpinumisoflavone acetate is a anticancer agent. Alpinumisoflavone acetate shows antiproliferative activity. Alpinumisoflavone acetate decreases the expression of phosphorylation of ERK1/2. Alpinumisoflavone acetate induces mitochondrial dysfunction and mitochondria-mediated Apoptosis. Alpinumisoflavone acetate has the potential for the research of HCC .
    Alpinumisoflavone acetate
  • HY-13241
    Ralimetinib dimesylate
    10+ Cited Publications

    LY2228820 dimesylate

    		 p38 MAPK Autophagy Apoptosis Inflammation/Immunology Cancer
    Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
    Ralimetinib dimesylate
  • HY-N1987
    Cucurbitacin IIb

    Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
    Cucurbitacin IIb
  • HY-150700
    RLX-33

    		ERK Metabolic Disease
    RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
    RLX-33
  • HY-13241A
    Ralimetinib

    LY2228820

    		 p38 MAPK Autophagy Inflammation/Immunology Cancer
    Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .
    Ralimetinib
  • HY-12960
    SKLB4771

    FLT3-​IN-​1

    		 FLT3 c-Kit Apoptosis Cancer
    SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .
    SKLB4771
  • HY-153445
    MEK-IN-6

    		ERK MEK Cancer
    MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). MEK-IN-6 can be used for research of cancer .
    MEK-IN-6
  • HY-76474
    BAY 61-3606

    		Syk Apoptosis Inflammation/Immunology Cancer
    BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
    BAY 61-3606
  • HY-14985
    BAY 61-3606 dihydrochloride
    5 Publications Verification

    		 Syk Apoptosis Inflammation/Immunology Cancer
    BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
    BAY 61-3606 dihydrochloride
  • HY-N2270
    Chicanine

    		p38 MAPK ERK IKK Inflammation/Immunology
    Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity .
    Chicanine
  • HY-N1966
    (E)-Osmundacetone
    2 Publications Verification
    (E)-Osmundacetone is the isomer of Osmundacetone. Osmundacetone significantly suppresses the phosphorylation of MAPKs, including JNK, ERK, and p38 kinases. Osmundacetone has a neuroprotective effect against oxidative stress .
    (E)-Osmundacetone
  • HY-147301
    Resomelagon

    AP1189

    		 Melanocortin Receptor Metabolic Disease Inflammation/Immunology
    Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research .
    Resomelagon
  • HY-147301A
    Resomelagon acetate

    AP1189 acetate

    		 Melanocortin Receptor Metabolic Disease Inflammation/Immunology
    Resomelagon (AP1189) acetate is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon acetate induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon acetate has anti-inflammatory activity. Resomelagon acetate can be used for obesity and chronic inflammation research .
    Resomelagon acetate
  • HY-155533
    YF704

    		SHP2 Cancer
    YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC50=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells .
    YF704
  • HY-100403
    Ro 67-7476
    5+ Cited Publications

    		 mGluR Cancer
    Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
    Ro 67-7476
  • HY-110318
    VUF11207 fumarate
    1 Publications Verification

    		 CXCR Inflammation/Immunology Cancer
    VUF11207 fumarate is a CXCR7 agonist that binds specifically to CXCR7. VUF11207 fumarate reduces CXCL12-mediated osteoclastogenesis and bone resorption by inhibiting ERK phosphorylation .
    VUF11207 fumarate
  • HY-107640
    WAY-170523

    		MMP Cancer
    WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC50 of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research .
    WAY-170523
  • HY-124404A
    12(S)-HETE

    		ERK DNA/RNA Synthesis p38 MAPK Cancer
    12(S)-HETE is the 12-lipoxygenase metabolite of arachidonic acid and has a mitogenic effect on cancer cell proliferation. 12(S)-HETE induces tyrosine phosphorylation of cellular proteins, promotes ERK and P38 MAPK phosphorylation, increases DNA synthesis, and stimulates the proliferation of pancreatic cancer cells .
    12(S)-HETE
  • HY-113599
    Isoprocurcumenol

    		EGFR ERK Akt Others
    Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate EGFR signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes .
    Isoprocurcumenol
  • HY-146672
    ITK inhibitor 6

    		Itk Cancer
    ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
    ITK inhibitor 6
  • HY-126477
    NNK

    		Endogenous Metabolite Cancer
    NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
    NNK
  • HY-15496
    E6201

    ER-806201

    		 MEK FLT3 Cancer
    E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
    E6201
  • HY-P3750
    Methionyl-Lysyl-Bradykinin

    Met-Lys-Bradykinin

    		 Bradykinin Receptor Cardiovascular Disease Endocrinology
    Methionyl-Lysyl-Bradykinin (Met-Lys-Bradykinin), a Bradykinin (HY-P0206) analogue, is a kinin .
    Methionyl-Lysyl-Bradykinin
  • HY-163283
    6′-Methyl paeonol

    		Amyloid-β Neurological Disease
    6’-Methyl paeonol is a paeonol derivative, which inihibits abnormal depolarizations and reduces the Amyloid β-induced ERK phosphorylation. 6’-Methyl paeonol exhibits alleviating activity against Alzheimer’s Disease .
    6′-Methyl paeonol
  • HY-13905
    Flumatinib mesylate

    HHGV678 mesylate

    		 Bcr-Abl c-Kit PDGFR Cancer
    Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .
    Flumatinib mesylate
  • HY-16697
    CID 16020046
    1 Publications Verification

    		 GPR55 Cancer
    CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
    CID 16020046
  • HY-P0178
    LXW7

    		Integrin Inflammation/Immunology
    LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
    LXW7
  • HY-N10047
    7,8-Didehydrocimigenol

    		NF-κB PPAR Cardiovascular Disease
    7,8-Didehydrocimigenol is an active triterpenoid that can be isolated from Cimicifugae rhizoma. 7,8-Didehydrocimigenol inhibits TNF-α-induced VCAM-1 expression, inhibits NF-kB activity and phosphorylation of ERK1/2 and Akt, increases PPAR-γ expression. 7,8-Didehydrocimigenol can be used for the research of cardiovascular disorders such as atherosclerosis .
    7,8-Didehydrocimigenol
  • HY-154985
    DSO-5a

    		PPAR Bombesin Receptor ERK Metabolic Disease
    DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research .
    DSO-5a
  • HY-155417
    GPR34 receptor antagonist 3

    		Others Neurological Disease
    GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
    GPR34 receptor antagonist 3
  • HY-P99183
    Abituzumab

    EMD 525797; DI17E6

    		 Integrin Cancer
    Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer .
    Abituzumab
  • HY-N0774
    Isofraxidin
    1 Publications Verification

    		 COX MMP Toll-like Receptor (TLR) Inflammation/Immunology
    Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
    Isofraxidin
  • HY-P0178A
    LXW7 TFA

    		Integrin Inflammation/Immunology
    LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
    LXW7 TFA

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