ERK
Extracellular signal regulated kinases
ERKs (Extracellular-signal-regulated kinases) are widely expressed protein kinase intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions in differentiated cells. Many different stimuli, including growth factors, cytokines, virus infection, ligands for heterotrimeric G protein-coupled receptors, transforming agents, and carcinogens, activate the ERK pathway. In the MAPK/ERK pathway, Ras activates c-Raf, followed by mitogen-activated protein kinase kinase (abbreviated as MKK, MEK, or MAP2K) and then MAPK1/2 (below). Ras is typically activated by growth hormones through receptor tyrosine kinases and GRB2/SOS, but may also receive other signals. ERKs are known to activate many transcription factors, such as ELK1, and some downstream protein kinases. Disruption of the ERK pathway is common in cancers, especially Ras, c-Raf and receptors such as HER2.
ERK Isoform Specific Products
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ERK Inhibitors
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ERK Agonists
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ERK Activators
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ERK Modulators
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ERK Chemical
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ERK Inducers
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ERK Degraders
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ERK Controls
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ERK Ligands
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ERK Related Products (1144)
Related Products (1144)
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Antibodies (22)
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ERK Isoform Comparison
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Zoniporide hydrochloride
0 ImagesCat. No.: HY-105064BCAS No.: 241800-97-5Synonyms: CP-597396 hydrochlorideZoniporide hydrochloride (CP-597396 hydrochloride) is a selective Na+/H+ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC50 values of 67 nM and 73 nM against rat NHE1. Zoniporide hydrochloride reduces intracellular Na+ and Ca2+ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide hydrochloride is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.
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αMβ2 integrin agonist-1
0 ImagesCat. No.: HY-175288αMβ2 integrin agonist-1 (Compound 8) is a highly selective αMβ2 integrin agonist with anti-inflammatory activity (EC50=1.4 nM). αMβ2 integrin agonist-1 activates integrin-mediated cell adhesion and JNK/ERK signaling. αMβ2 integrin agonist-1 induces tumor-associated macrophage repolarization and enhances antitumor T-cell immune responses. αMβ2 integrin agonist-1 is promising for research of cancers and chronic inflammatory diseases (e.g., pancreatic cancer, rheumatoid arthritis).
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MAPK-IN-3
0 ImagesCat. No.: HY-169412CAS No.: 2848599-79-9MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK.
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Sargachromanol E
0 ImagesCat. No.: HY-123364CAS No.: 856414-54-5Sargachromanol E is an apoptosis inducer, anti-inflammatory agent, and anti-aging agent. Sargachromanol E activates caspase-3, mediates PARP cleavage, downregulates Bcl-xL and upregulates Bax levels, and drives sub-G1 phase cell cycle arrest, inhibits LPS-induced COX-2 and iNOS transcription and expression (NO: IC50 = 6.99 μg/mL), reduces p38 MAPK and ERK1/2 phosphorylation levels, and suppresses the release of pro-inflammatory mediators such as TNF-α, IL-1β, and prostaglandin E2 (PGE2). Sargachromanol E can be used for research on skin aging, leukemia, oral squamous cell carcinoma, and inflammation-related studies.
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ZSH-2117
0 ImagesCat. No.: HY-174415ZSH-2117 is an NEDD4-recruiting EGFR PROTAC degrader. ZSH-2117 shows an IC50 of 13 nM against EGFRL858R/T790M/C797S, induces EGFR proteasome-dependent degradation, inhibits the downstream signaling pathways of EGFR, including the phosphorylation of AKT and ERK, suppresses cancer cell proliferation, and exhibits in vivo anti-tumor activity. ZSH-2117 can be used in research related to non-small cell lung cancer.
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Hordenine-d6 hydrochloride
0 ImagesCat. No.: HY-N0113BSSynonyms: Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochlorideHordenine-d6 hydrochloride (Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochloride) is the deuterated-labeled Hordenine hydrochloride (HY-N0113B). Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride inhibits melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.
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RK-682 hemicalcium
0 ImagesCat. No.: HY-135564CAS No.: 332131-32-5RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 hemicalcium inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24[2].
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DZX19
0 ImagesCat. No.: HY-181871DZX19 (Compound C02) is an orally active, selective TRK inhibitor with a TRKA IC50 value of 1.32 nM, a TRKB IC50 of 2.28 nM, and a TRKC IC50 of 4.05 nM. DZX19 inhibits the kinase activities of wild-type TRKA, TRKA mutants (G595R, F589L, G667C), wild-type TRKB, and wild-type TRKC, and suppresses the phosphorylation of TRKA as well as its downstream AKT and ERK signaling pathways. DZX19 induces apoptosis. DZX19 inhibits tumor growth in a colorectal cancer xenograft mouse model. DZX19 is applicable for the research of colorectal cancer.
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α4β1 antagonist-1
0 ImagesCat. No.: HY-175286α4β1 antagonist-1 (Compound 4) is a highly selective α4β1 integrin antagonist (IC50=15 nM). α4β1 antagonist-1 inhibits integrin-mediated cell adhesion and ERK1/2 signaling activation. α4β1 antagonist-1 also exhibits partial agonism toward αMβ2 integrin (EC50=23 nM). α4β1 antagonist-1 is promising for research of chronic inflammatory diseases (e.g., rheumatoid arthritis, multiple sclerosis) and cancers.
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ABD56
0 ImagesCat. No.: HY-122019CAS No.: 521294-19-9
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Aloisine A
0 ImagesCat. No.: HY-112363CAS No.: 496864-16-5Synonyms: RP107Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.
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Dabogratinib (GMP)
0 ImagesCat. No.: HY-159642GCAS No.: 2800223-30-5Synonyms: TYRA-300 (GMP)Dabogratinib (GMP) is the GMP-grade version of Dabogratinib (HY-159642). Dabogratinib (TYRA-300) is an orally active, selective FGFR3 inhibitor with an IC50 of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia.
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BRSD-143
0 ImagesCat. No.: HY-184010CAS No.: 3101973-42-3BRSD-143 is an orally active KRASG12D inhibitor, with a Kd value of 0.003 nM for KRASG12D and 0.024 nM for KRASG12V. BRSD-143 inhibits the activity of phosphorylated ERK in KRAS-mutated cells. BRSD-143 induces tumor regression in ovarian cancer xenograft mouse models. BRSD-143 can be used for the research of KRAS-mutated cancers.
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BSI-001
0 ImagesCat. No.: HY-P991977Synonyms: 5G9BSI-001 (5G9) is a HER2-targeting antibody. BSI-001 inhibits cell proliferation and migration, induces apoptosis and PARP cleavage, and suppresses HER2-mediated downstream signaling pathways (including the phosphorylation of EGFR, HER3, AKT and ERK) when combined with Trastuzumab (HY-P9907) in HER2-positive cancer cells. BSI-001 exhibits synergistic anti-tumor efficacy in animal models of gastric cancer and breast cancer when combined with Trastuzumab. BSI-001 can be used for the research of HER2-positive breast cancer and HER2-overexpressing gastric cancer.
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Nrf2/HO-1 activator 1
0 ImagesCat. No.: HY-151430Nrf2/HO-1 activator 1 (Compound 24) is a potent Nrf2/HO-1 activator, neuroprotective agent. Nrf2/HO-1 activator 1 shows neuroprotective and antioxidant activities. Nrf2/HO-1 activator 1 can be used in Parkinson's disease (PD) research.
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Deltafluorine
0 ImagesCat. No.: HY-181020Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma.
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Kuwanon H (Standard)
0 ImagesCat. No.: HY-N2600RCAS No.: 76472-87-2Kuwanon H (Standard) is the analytical standard of Kuwanon H. This product is intended for research and analytical applications. Kuwanon H is a selective non-peptide bombesin receptor antagonist and platelet activation inhibitor. Kuwanon H also acts as a specific antagonist of GRP-preferring receptors, with a Ki value of 290 nM for mouse GRP-R and 6500 nM for rat NMB-R. Kuwanon H inhibits the phosphorylation of AKT, mTOR, ERK, cPLA2 and p38, and upregulates TRIB3. It induces endoplasmic reticulum stress, apoptosis and autophagosome formation. Kuwanon H blocks calcium mobilization, mitogenic signaling, DNA synthesis, dense granule secretion, thromboxane A2 generation and integrin αIIb/β3 activity. It inhibits collagen-induced platelet aggregation and fibronectin adhesion, and delays clot retraction. Kuwanon H inhibits melanoma cell growth in vitro and in vivo, and enhances the sensitivity of melanoma cells to CDDP. It can be used in research related to melanoma, small cell lung cancer and thrombosis.
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HTL-9936
0 ImagesCat. No.: HY-148961CAS No.: 1438242-59-1HTL-9936 is an orally active partial agonist of muscarinic M1 receptor. HTL-9936 has an EC50 of 32 nM for human M1 receptor and an EC50 of 224 nM for human M4 receptor. HTL-9936 activates Gq/11 coupling, promotes inositol phosphate accumulation, ERK1/2 phosphorylation, β-arrestin recruitment and receptor internalization. HTL-9936 can be used in the research of Alzheimer's disease and schizophrenia.
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Myrislignan-13C,d2
0 ImagesCat. No.: HY-N0608SMyrislignan-13C,d2 is the 13C, d2 deuterated-labeled Myrislignan (HY-N0608). Myrislignan is a PI3K/AKT/NF-κB inhibitor that can cross the blood-brain barrier. Myrislignan exerts anticancer activity by inducing apoptosis and ferroptosis. Myrislignan inhibits the replication and invasion of Toxoplasma gondii; it induces reactive oxygen species (ROS) imbalance, autophagy, and the death of Toxoplasma gondii tachyzoites. Myrislignan inhibits mitochondrial function and ERK1/2 phosphorylation to improve ovariectomy-induced osteoporosis. Myrislignan can be used in studies related to gastric cancer, glioblastoma, osteoporosis, and toxoplasmosis.
