2. Signaling Pathways
  3. MAPK/ERK Pathway
    Stem Cell/Wnt
  4. ERK
  5. ERK2 Isoform
  6. ERK2 Inhibitor

ERK2 Inhibitor

ERK2 Inhibitors (53):

Cat. No. Product Name Effect Purity
  • HY-12028
    PD98059
    		Inhibitor 99.96%
    PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.
  • HY-50846
    SCH772984
    		Inhibitor 98.82%
    SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
  • HY-15816
    Ulixertinib
    		Inhibitor 99.95%
    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.
  • HY-164151
    ERK-IN-8
    		Inhibitor
    ERK-IN-8 (compound I-1) is an aniline pyrimidine derivative that acts as an ERK inhibitor. ERK-IN-8 has a strong inhibitory effect on ERK2 in vitro (IC50≤50 nM). ERK-IN-8 can be used in cancer research.
  • HY-162460
    ERK1/2 inhibitor 10
    		Inhibitor
    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.
  • HY-N0431
    Astragaloside IV
    		Inhibitor ≥98.0%
    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.
  • HY-101494
    Temuterkib
    		Inhibitor 99.94%
    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.
  • HY-N2329
    Piperlongumine
    		Inhibitor 99.87%
    Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.
  • HY-15947
    Ravoxertinib
    		Inhibitor 99.75%
    Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
  • HY-12275
    FR 180204
    		Inhibitor 99.64%
    FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively.
  • HY-N7140
    Gamma-Linolenic acid
    		Inhibitor 99.74%
    Gamma-linolenic acid (γ-Linolenic acid) is an orally active unsaturated fatty acid. Gamma-linolenic acid exerts anti-inflammatory effects by inhibiting the NF-κB pathway and the phosphorylation of ERK1/2 and JNK. At the same time, it exerts anticancer effects by inducing apoptosis (Apoptosis) in cancer cells. Additionally, Gamma-linolenic acid also has antioxidant and memory-improving effects. It holds promise for research in the fields of inflammation, neurology, and cancer diseases.
  • HY-136579
    ASN007
    		Inhibitor 99.70%
    ASN007 (ERK-IN-3) is a potent and orally active inhibitor of ERK. ASN007 inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 can be used for the research of cancers driven by RAS mutations.
  • HY-111407
    MK-8353
    		Inhibitor
    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.
  • HY-14178
    VX-11e
    		Inhibitor 99.17%
    VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
  • HY-108330
    AG126
    		Inhibitor ≥98.0%
    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.
  • HY-126288
    ASTX029
    		Inhibitor 99.82%
    ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity.
  • HY-111483
    Tizaterkib
    		Inhibitor 99.31%
    Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.
  • HY-18932
    DEL-22379
    		Inhibitor 99.69%
    DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.
  • HY-15947A
    Ravoxertinib hydrochloride
    		Inhibitor 99.93%
    Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
  • HY-114491
    Rineterkib
    		Inhibitor 99.83%
    Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.