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ERK-IN-2

" in MedChemExpress (MCE) Product Catalog:

428

Inhibitors & Agonists

1

Screening Libraries

2

Fluorescent Dyes

4

Biochemical Assay Reagents

40

Peptides

4

Inhibitory Antibodies

97

Natural
Products

19

Isotope-Labeled Compounds

2

Click Chemistry

3

Oligonucleotides

2

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19696
    Tauroursodeoxycholate
    Maximum Cited Publications
    104 Publications Verification

    Tauroursodeoxycholic acid; TUDCA; UR 906

    ERK Caspase Endogenous Metabolite Apoptosis Cancer
    Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an orally active endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK .
    Tauroursodeoxycholate
  • HY-N0431
    Astragaloside IV
    30+ Cited Publications

    MMP ERK JNK Cancer
    Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
    Astragaloside IV
  • HY-50706
    Selumetinib
    85+ Cited Publications

    AZD6244; ARRY-142886

    MEK Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology 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 can penetrate the blood brain barrier (BBB) [2] .
    Selumetinib
  • HY-15312
    WP1066
    35+ Cited Publications

    STAT JAK Apoptosis Cancer
    WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. WP1066 can cross the blood-brain barrier[1][2][3][4].
    WP1066
  • HY-14463
    Onalespib
    10+ Cited Publications

    AT13387

    HSP Cancer
    Onalespib (AT13387) is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor. Onalespib inhibits the proliferation, survival and migration. Onalespib decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib shows antitumor activity. Onalespib has the potential for the research of non-small cell lung cancer (NSCLC) [2] .
    Onalespib
  • HY-100403
    Ro 67-7476
    20+ 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 [2]. 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-111407
    MK-8353
    5 Publications Verification

    SCH900353

    ERK Cancer
    MK-8353 (SCH900353) is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.
    MK-8353
  • HY-126288
    ASTX029
    5+ Cited Publications

    ERK Apoptosis Cancer
    ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity [2].
    ASTX029
  • HY-10520
    CGP 57380
    3 Publications Verification

    MNK Apoptosis Cancer
    CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
    CGP 57380
  • HY-50706A
    Selumetinib sulfate
    85+ Cited Publications

    AZD6244 sulfate; ARRY-142886 sulfate

    MEK Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Selumetinib (AZD6244) sulfate is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) sulfate inhibits ERK1/2 phosphorylation. Selumetinib sulfate can penetrate the blood brain barrier (BBB) [2] .
    Selumetinib sulfate
  • HY-112287
    ERK1/2 inhibitor 1
    5+ Cited Publications

    ERK Cancer
    ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively .
    ERK1/2 inhibitor 1
  • HY-P5985
    mSIRK
    2 Publications Verification

    ERK Others
    mSIRK (G-Protein βγ Binding Peptide) is an cell-permeable activator of ERK1/2, with EC50 of 2.5-5 μM. mSIRK disrupts the interaction between α and βγ subunits and promotes α subunit dissociation without stimulating nucleotide exchange .
    mSIRK
  • HY-129566

    ERK Wnt β-catenin RUNX Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Withanolide B is an active component of W. somnifera Dunal. Withanolide B promotes osteogenic differentiation of hBMSCs via ERK1/2 and Wnt/β-catenin signaling pathways. Withanolide B exhibits neuroprotective, anti-arthritic, anti-aging and anti-cancer effects [2] .
    Withanolide B
  • HY-107753

    Ras Inflammation/Immunology Cancer
    XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2 . XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules [2].
    XRP44X
  • HY-N2450
    Sulforaphene
    1 Publications Verification

    Apoptosis EGFR ERK NF-κB Microtubule/Tubulin Cancer
    Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals [2] .
    Sulforaphene
  • HY-112570
    CC-90003
    1 Publications Verification

    ERK Cancer
    CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
    CC-90003
  • HY-112181
    KO-947
    4 Publications Verification

    ERK Cancer
    KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
    KO-947
  • HY-B0513
    Methylthiouracil
    1 Publications Verification

    MTU

    NF-κB TNF Receptor Interleukin Related ERK Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
    Methylthiouracil
  • HY-N2283
    Deltonin
    1 Publications Verification

    ERK Akt Endogenous Metabolite Cancer
    Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
    Deltonin
  • HY-N2312
    Mogrol
    2 Publications Verification

    ERK STAT Cancer
    Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
    Mogrol
  • HY-16642A
    LY2828360
    1 Publications Verification

    Cannabinoid Receptor Neurological Disease
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
    LY2828360
  • HY-122246

    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-N1374
    Magnolin
    2 Publications Verification

    ERK Inflammation/Immunology
    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.
    Magnolin
  • HY-B0916

    Environmental Pollutants MMP Insecticide Cholinesterase (ChE) ERK Keap1-Nrf2 Reactive Oxygen Species (ROS) Infection Neurological Disease Cancer
    Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests [2] .
    Propoxur
  • HY-147301A

    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 [2].
    Resomelagon acetate
  • HY-137977
    DMU-212
    2 Publications Verification

    ERK Apoptosis Cancer
    DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active [2].
    DMU-212
  • HY-147301

    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 [2].
    Resomelagon
  • HY-W010907
    Pamoic acid disodium
    4 Publications Verification

    GPR35 ERK Neurological Disease
    Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect .
    Pamoic acid disodium
  • HY-153738

    ERK Cancer
    ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .
    ERK1/2 inhibitor 9
  • HY-133084A

    ERK Cancer
    ERK-IN-2 free base is a ERK2 inhibitor with an IC50 value of 1.8 nM. ERK-IN-2 free base might lead to off-target toxicity and/or off-target activity at dose >10 μM .
    ERK-IN-2 free base
  • HY-124740

    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-W001174

    ERK NF-κB Inflammation/Immunology
    2,5-Dihydroxyacetophenone, isolated from Rehmannia glutinosa, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways .
    2,5-Dihydroxyacetophenone
  • HY-P3513

    ERK MMP Neurological Disease
    β-Neo-Endorphin is an endogenous opioid peptide. β-Neo-Endorphin is a hypothalamic “big” Leu-enkephalin of porcine origin. β-Neo-Endorphin shows activation of the Erk1/2, MMP-2 and MMP-9 [2].
    β-Neo-Endorphin
  • HY-N2156

    ERK TGF-beta/Smad Wnt β-catenin JNK p38 MAPK Metabolic Disease Inflammation/Immunology
    Paeonolide, found in Paeonia suffruticosa, is an ERK1/2 activator. Paeonolide promotes early and late osteoblast differentiation, stimulates pre-osteoblast transmigration, and activates the BMP-Smad1/5/8, Wnt-β-catenin, JNK and p38 pathways. Paeonolide can be used for the research of osteoporosis, periodontitis .
    Paeonolide
  • HY-120006A
    (rel)-AR234960
    1 Publications Verification

    ERK Cardiovascular Disease
    (rel)-AR234960 is a selective and competitive agonist of the G protein-coupled receptor MAS. (rel)-AR234960 binds to the MAS receptor to activate the downstream ERK1/2 signaling pathway, inducing the expression of connective tissue growth factor (CTGF) and its downstream collagen subtype genes (such as COL1A1, COL3A1). (rel)-AR234960 promotes collagen synthesis in cardiac fibroblasts through the MAS-ERK1/2-CTGF pathway and aggravates extracellular matrix remodeling. (rel)-AR234960's in vitro effect can be blocked by the MAS inverse agonist AR244555 and MEK1 inhibitor. (rel)-AR234960 regulates the expression of cardiac fibrosis-related genes and can be used in the study of heart failure [2].
    (rel)-AR234960
  • HY-133084

    ERK Cancer
    ERK-IN-2 is a ERK2 inhibitor with an IC50 value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM .
    ERK-IN-2
  • HY-N1507

    Estrogen Receptor/ERR Cancer
    Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing .
    Tracheloside
  • HY-N2270
    Chicanine
    1 Publications Verification

    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-N6007
    Chrysosplenol D
    1 Publications Verification

    Apoptosis Infection Inflammation/Immunology Cancer
    Chrysosplenol D is a methoxy flavonoid that induces ERK1/2-mediated apoptosis in triple negative human breast cancer cells. Chrysosplenol D also exhibits anti-inflammatory and moderate antitrypanosomal activities [2] .
    Chrysosplenol D
  • HY-153445
    Polfurmetinib
    1 Publications Verification

    MEK-IN-6

    ERK MEK Cancer
    Polfurmetinib (MEK-IN-6) (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). Polfurmetinib can be used for research of cancer .
    Polfurmetinib
  • HY-142433

    ERK Cancer
    ERK1/2 inhibitor 7 is a potent ERK inhibitor with an IC50 of 0.94 nM for ERK2 (WO2021110168A1, WX006) .
    ERK1/2 inhibitor 7
  • HY-P3751

    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-113916

    AT13387 lactate

    HSP Cancer
    Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) [2] .
    Onalespib lactate
  • HY-145025

    ERK Inflammation/Immunology Cancer
    ERK1/2 inhibitor 3 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1) .
    ERK1/2 inhibitor 3
  • HY-153735

    PROTACs ERK Cancer
    ERK-CLIPTAC is a ERK CLIPTAC (click chemistry-synthesized proteolysis-targeting chimera) degrader. ERK-CLIPTAC forms intracellularly via click chemistry from ERK1/2-IN-14 (HY-175578) and Tz-thalidomide (HY-101460). The formed ERK-CLIPTAC recruits the E3 ubiquitin ligase CRBN to ERK1/2, thereby inducing ubiquitination and subsequent degradation of ERK1/2. Due to its lack of cell permeability, ERK-CLIPTAC cannot induce ERK1/2 degradation in cells. ERK-CLIPTAC can be used in research related to melanoma and colorectal cancer .
    ERK-CLIPTAC
  • HY-162460

    ERK Cancer
    ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations .
    ERK1/2 inhibitor 10
  • HY-145026

    ERK Inflammation/Immunology Cancer
    ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .
    ERK1/2 inhibitor 4
  • HY-145027

    ERK Cancer
    ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .
    ERK1/2 inhibitor 5
  • HY-P5977

    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 [2].
    STE-MEK1(13)
  • HY-142437

    ERK Cancer
    ERK1/2 inhibitor 8 is a potent ERK inhibitor with an IC50 of 0.48 nM for ERK2 (WO2021110168A1, WX007) .
    ERK1/2 inhibitor 8

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