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ERK

ERK is a downstream component of an evolutionarily conserved signaling module that is activated by the Raf serine/threonine kinases. Raf activates the MAPK/ERK kinase (MEK)1/2 dual-specificity protein kinases, which then activate ERK1/2.

  • Beta-Tocopherol
    TN1441148-03-8
    Beta-Tocopherol shows effect on human erythroleukemia cell (HEL) adhesion induced by phorbol 12-myristate 13-acetate (PMA).
    • $54
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  • Notoginsenoside R1
    T296180418-24-2
    Notoginsenoside R1 (Sanchinoside R1) has been shown to exhibit antioxidant, antiapoptotic, anti-inflammatory, and immune-stimulatory properties.
    • $63
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  • SCH772984
    T6066942183-80-4
    SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases.
    • $48
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  • Allicin
    T3123539-86-6
    Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.
    • $40
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  • CK2/ERK8-IN-1
    T108271085822-09-8In house
    CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).
    • $30
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  • Farrerol
    T6S052524211-30-1
    1. Farrerol has antioxidative activity.2. Farrerol modulates TAP and BNBD5 gene expression in mammary gland, enhances bMEC defense against S. aureus infection and could be useful in protection against bovine mastitis. 3. Farrerol inactivates KEAP-1 or act
    • $110
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  • magnolin
    T385731008-18-1
    Magnolin reduces the renal oxidative stress, suppresses caspase-3 activity, and increases Bcl-2 expression in vivo and in vitro. Magnolin has anti-inflammatory and antioxidative effects.
    • $93
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  • Astragaloside IV
    T297384687-43-4
    Astragaloside IV (AS-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 is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.
    • $32
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  • Nothofagin
    TN199611023-94-2In house
    Nothofagin has antioxidant, and antithrombotic activities, it possesses anti-inflammatory activity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases.
    • $489
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  • CHPG hydrochloride
    T10809L In house
    CHPG hydrochloride is a selective agonist of mGluR5.
    • $85
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  • A-674563 2HCl(552325-73-2(fb-2hcl))
    T6139L
    A-674563 2HCl is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
    • $78
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  • ERK5-IN-6
    T777312734916-64-2
    ERK5-IN-6 is a potent inhibitor of ERK5 kinase.ERK5-IN-6 exhibits antiproliferative activity, anticonvulsant activity, and antitumor activity, and can be used in the study of central nervous system-related disorders.
    • $195
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  • A-674563 HCl (552325-73-2(free base))
    T44442070009-66-2
    A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16/46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th
    • $77
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  • ZINC12409120
    T611221010888-06-8In house
    ZINC12409120 (R-4584) is a selective ERK inhibitor.ZINC12409120 inhibits ERK with an IC50 of 5.0 μM.ZINC12409120 inhibits ERK activity by interfering with FGF23:α-Klotho interaction.
    • $350
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  • Prosaptide TX14(A) acetate
    TP1970L
    Prosaptide TX14(A) acetate is a potent GPR37L1 and GPR37 agonist. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.
    • $148
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  • Astragaloside
    T408217429-69-5
    Astragaloside, one of the main active ingredients in Astragalus membranaceus.
    • $50
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  • Gardenin A
    TN411421187-73-5
    Gardenin A shows neurotrophic effects via activating MAPK/ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.
    • $197
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  • AY 77
    T411901835734-92-3In house
    AY 77 (Unk-Cha-Chg-NH2) is a potent and selective PAR2 agonist. AY 77 showed selectivity for Ca2+ and ERK1/2 signaling (ec50 value of Ca2+ release was 40 nM and ec50 value of ERK1/2 phosphorylation was 2 μM). AY 77 can promote migration of human breast cancer cells in vitro.
    • $686
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  • Epieriocalyxin A
    TN3967191545-24-1
    Epieriocalyxin A can suppress Caco-2 colon cancer cell growth. It could be a potential drug for colon cancer therapy in the future.
    • $216
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  • EF24
    T27242342808-40-6In house
    EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK. EF24 shows potent anti-tumor activity in oral squamous cell carcinoma (OSCC) via deactivation of the MAPK/ERK signaling pathway.
    • $33
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  • PAF (C16)
    T2154774389-68-7In house
    PAF (C16) is a potent MAPK and MEK/ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.
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  • ROCK-IN-5
    T67748692870-25-0In house
    ROCK-IN-5 (compound I-B-37) is a potent inhibitor of protein kinases, including ROCK, ERK, GSK, and AGC. ROCK-IN-5 exhibits the potential for cardiac, proliferative and neurodegenerative diseases research.
    • $38
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  • Olomoucine
    T21588101622-51-9In house
    Olomoucine is an ATP competitive inhibitor of Cdk2/cyclin A, Cdc2/CyclinB, CDK2/CyclinE, CDK5/p35, and ERK1/p44 MAP kinase with IC50s of 7, 7, 7, 3 and 25 µM, respectively. Olomoucine regulates cell cycle and exhibits anti-melanin tumor activities.
    • $67
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  • ERK1/2 inhibitor 1
    T112262095719-90-5In house
    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.
    • $213
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  • Galangin
    T3668548-83-4
    Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.
    • $30
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  • Temuterkib
    T40911951483-29-6
    Temuterkib (LY3214996) is a potent and selective, orally available inhibitor of the extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity.
    • $64
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  • Lidocaine hydrochloride
    T114473-78-9
    Lidocaine hydrochloride (Lignocaine hydrochloride) is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.
    • $45
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  • Tauroursodeoxycholate sodium
    T699335807-85-3
    Tauroursodeoxycholate sodium (TUDC) is an endoplasmic reticulum (ER) stress inhibitor, used for the treatment of gallstones and liver cirrhosis.
    • $30
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  • Honokiol
    T300135354-74-6
    Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.
    • $50
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  • Ulixertinib
    T7005869886-67-9
    Ulixertinib (VRT752271) (BVD-523, VRT752271) is an effective and reversible ERK1/ERK2 inhibitor. The IC50 of Ulixertinib is less than 0.3 nM for ERK2.
    • $34
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  • 5α-Hydroxycostic acid
    TN3139132185-83-2
    5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.
    • $162
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  • Bongkrekic acid
    T3606711076-19-0
    Bongkrekic acid (Bongkrekic Acid (ammonium salt)) is a mitochondrial toxin secreted by Burkholderia gladioli that inhibits adenine nucleotide translocase (ANT).Bongkrekic acid Bongkrekic acid Bongkrekic acid induces extracellular traps in neutrophils through signaling mediated by p38, ERK, PAD4, and P2X1.
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  • Ravoxertinib
    T65111453848-26-4
    Ravoxertinib (GDC-0994) is an effective and orally available ERK1/2 inhibitor (IC50: 1.1/0.3 nM).
    • $34
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  • Selumetinib
    T6218606143-52-6
    Selumetinib (AZD6244) (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).
    • $47
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  • FR 180204
    T1956865362-74-9
    FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.
    • $36
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  • PD98059
    T2623167869-21-8
    PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.
    • $34
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  • Bohemine
    T2029189232-42-6
    Bohemine is a cyclin-dependent kinase inhibitor.
    • $47
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  • ERK-IN-2
    T112252743576-56-7
    ERK-IN-2, an ERK2 inhibitor, exhibits an IC50 value of 1.8 nM. At doses greater than 10 μM, it may induce off-target toxicity and/or activity [1].
    • $1,520
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  • Ro-3306
    T2356872573-93-8
    RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.
    • $32
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  • Tauroursodeoxycholate
    T253214605-22-2
    Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
    • $50
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  • Bakkenolide IIIa
    TN3486915289-60-0
    Bakkenolide IIIa has antioxidant, and neuroprotective effects, it protects against cerebral damage by inhibiting AKT and ERK1/2 activation and inactivated NF-κB signaling.
    • $740
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  • Pseudoginsenoside Rh2
    TN21141370264-16-6
    Pseudoginsenoside Rh2 has cytotoxicity, it induces mitochondrial apoptosis in A549 cells and is responsible for excessive activation of the Ras/Raf/ERK/p53 pathway. (20Z) -Pseudoginsenoside Rh2 and (20E)-Pseudoginsenoside Rh2 have antioxidative activity.
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  • 7,8-Didehydrocimigenol
    TN3219150972-72-8
    7,8-Didehydrocimigenol can be used for the treatment of cardiovascular disorders such as atherosclerosis. It upregulates PPAR-γ in EC inhibits NF-kB activity of TNF-α-activated EC which leads to selective inhibition of VCAM-1 expression.
    • $550
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  • Nyasol
    TN468396895-25-9
    Nyasol may have potential to be developed as medicines for the treatment of allergies by inhibiting the activation of mast cells. Nyasol shows anti-inflammatory properties by inhibiting iNOS expression; it also has antifungal activity, it is significantly
    • $1,790
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  • Haginin A
    TN417974174-29-1
    Haginin A is an effective inhibitor of hyperpigmentation caused by UV irradiation or by pigmented skin disorders through downregulation via ERK and Akt/PKB activation, MITF, and also by the subsequent downregulation of tyrosinase and TRP-1 production. Hag
    • $750
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  • Peonidin chloride
    TN1062134-01-0
    Peonidin chloride has antioxidant activity. Peonidin has show potent inhibitory and apoptotic effects on cancer cells in vitro, notably metastatic human breast cancer cells.
    • $155
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  • Cimiside E
    TN3655154822-57-8
    Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/2, PI3K, and PKC are involved in this effect.Cimiside E may be an effective chemopreventive agen
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  • Pinusolide
    TL001431685-80-0
    Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to treat neurodegenerative diseases. Pinusolide attenuates blockade of insulin signaling by enhancing IRS-1 tyrosine phosphorylation by the activating the AMPK pathway, indicates the targeting of AMPK represents a new therapeutic strategy for hyperglycemia-induced insulin resistance and type 2 diabetes.
    • $310
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  • mSIRK
    T80548593267-11-9
    mSIRK (G-Protein βγ Binding Peptide) is a cell-permeable activator of ERK 1/2 with an EC50 of 2.5-5 μM. It disrupts the interaction between the α and βγ subunits, facilitating α subunit dissociation without inducing nucleotide exchange [1].
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  • Dehydroglyasperin C
    TN3806199331-35-6
    Dehydroglyasperin C is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C possesses potent antioxidant, cancer chemopreventive, and neuroprotective activities, it has protective effects against chronic diseases
    • $871
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