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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.

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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SCH772984
T6066942183-80-4
SCH772984 is an ERK inhibitor that inhibits ERK1 and ERK2 (IC50=4 1 nM) and is highly selective and ATP-competitive. SCH772984 exhibits antitumor activity against BRAF or RAS mutant cells.
  • $48
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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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ERK-IN-3
T91412055597-12-9
ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations.
  • $56
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Beta-Tocopherol
TN1441148-03-8
Beta-Tocopherol has effects on human erythroleukemia cell (HEL) adhesion induced by phorbol 12-myristate 13-acetate (PMA).
  • $54
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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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Ravoxertinib
T65111453848-26-4
Ravoxertinib (GDC-0994) is an efficacious, orally available ERK1 2 inhibitor with an IC50 of 1.1 0.3 nM.
  • $34
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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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Licochalcone D
T4518144506-15-0
Licochalcone D may be a potential drug for human melanoma treatment by inhibiting proliferation, inducing apoptosis via the mitochondrial pathway and blocking cell migration and invasion. Licochalcone D has cardioprotective potential against myocardial is
  • $97
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Methylnissolin
TN235473340-41-7
Methylnissolin is a natural product isolated from Astragalus membranaceus that inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. It inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibiting the ERK1 2 MAP kinase cascade. It also inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1 2 (ERIC1 2) mitogen-activated protein (MAP) kinases and has antibacterial and anticancer effects.
  • $81
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Chrysoeriol
TN1490491-71-4
Chrysoeriol has antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities, it also shows selective bronchodilator effect.
  • $40
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Vincristine
T3S020957-22-7
Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and
  • $148
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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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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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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].
  • $40
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Selumetinib
T6218606143-52-6
Selumetinib (AZD6244) is a MEK1 2 inhibitor that inhibits MEK1 (IC50=14 nM) with potent selectivity and is non-ATP-competitive. Selumetinib has antitumor activity and is used for the treatment of neurofibromatosis type 1 (NF1).
  • $47
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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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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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ERK5-IN-2
T55351888305-96-1
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 values of 0.82 μM for ERK5 and 3 μM for ERK5 (MEF2D).
  • $41
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Sulforaphene
TL0016592-95-0
Sulforaphene is a natural product 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 signa
  • $31
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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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Jolkinolide B
T2S104037905-08-1
Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.
  • $60
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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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Epiberberine
T5S23616873-09-2
1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf MEK1 ERK1 2 and AMPKα Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.
  • $31
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Sophocarpine
T66776483-15-4
Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.
  • $45
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DMU-212
T36674134029-62-2
DMU-212 is a methylated derivative of resveratrol with antimitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities. It induces mitotic arrest, apoptosis, and activation of ERK1 2 protein and has oral activity[1][2]. DMU-212 (0.3125-40 μM) inhibits the growth of human melanoma cells (A375, MeWo, Bro, M5)[1]. At concentrations of 30-50 μM over 24 hours, it upregulates cell cycle inhibitors, induces apoptosis, and activates ERK in A375 cells[1]. DMU-212 also induces G2 M arrest and apoptosis in cancer cells[1]. In a xenograft model of human ovarian cancer with six-week-old SCID female mice (20-24 g), DMU-212 (50 mg kg, administered orally three times a week for 14 days) inhibits tumor growth[2]. [1]. Vasilis Pericles Androutsopoulos, et al. Activation of ERK1 2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4. [2]. Hanna Piotrowska, et al. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400.
  • $30
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Prunetin
T4S0878552-59-0
1. Prunetin (Prunusetin) significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity adipogenesis effects by suppressing obesity-related transcription through a feedback mechanism that regulates the expression of adiponectin, adipoR1, adipoR2, and AMPK. 3. Prunetin and biochanin A are potent reducers of NF-κB and ERK activation, zonula occludens 1 tyrosine phosphorylation, and metalloproteinase-mediated shedding activity, which may account for the barrier-improving ability of these isoflavones. 4. Prunetin significantly suppresses ATP-induced mucin secretion from cultured RTSE cells; Prunetin inhibits the production of MUC5AC mucin protein induced by EGF or PMA from NCI-H292 cells; Prunetin also inhibits the expression of MUC5AC mucin gene induced by EGF or PMA from NCI-H292 cells.
  • $39
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Cornuside
T4S2326131189-57-6
1. Cornuside (Comuside) has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3. Cornuside can treat myocardial I R and protect the liver from CCl4-induced acute hepatotoxicity, by reducing oxidative stress and suppressing inflammatory responses. 4. Cornuside has anti-inflammatory activity by downregulations of iNOS and COX-2 due to NF-κB inhibition as well as the negative regulation of ERK1 2, p38, and JNK1 2 phosphorylations in RAW 264.7 cells. 5. Cornuside has protective potential against cerebral ischemic injury, may be due to the suppression of intracellular Ca(2+) elevation and caspase-3 activity, and improvements in mitochondrial energy metabolism and antioxidant properties.
  • $97
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MK-8353
T120691184173-73-6In house
MK-8353 (SCH900353) is a potent, selective, and orally available inhibitor of ERK1 2 with IC50 values of 23.0 nM and 8.8 nM, respectively.
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Pluripotin
T6948839707-37-8
Pluripotin (SC1) (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.
  • $30
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ERK1/2 inhibitor 2
T84722095719-92-7
ERK1 2 inhibitor 2 (ASTX029) is a selective and orally bioavailable extracellular signal-regulated kinases 1 and 2 (ERK 1 2) inhibitor, with potential antineoplastic activity.
  • $41
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Tenuifoliside A
T3856139726-35-5
Tenuifoliside A has anti-apoptotic , neuroprotective activity. And tenuifoliside A has anti-inflammatory effect, which is mediated by the inhibition of the NF-κB and MAPK pathways.
  • $56
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TBHQ
T53641948-33-0
TBHQ (tert-Butylhydroquinone) is an antioxidant that induces an antioxidant response through the redox-sensitive transcription factor Nrf2.
  • $41
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ERα degrader-2
T397272235396-63-9
ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation. It can be used for the prevention and treatment of HER-positive breast cancer.
  • $263
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12(S)-HETE
T3704754397-83-0
12(S)-HETE, a 12-lipoxygenase metabolite of arachidonic acid, is mitogenic for cancer cell proliferation and enhances angiotensin II-induced contraction of BLT2 (type 2 receptor in arteries of leukotriene B4 mice) and TP (thromboxane receptor)-mediated mechanisms. 12(S)-HETE promotes superoxide and isothromboxane-like metabolites in arterial endothelial cells. production.
  • $443
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A-443654
T14072552325-16-3
A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).
  • $84
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Gypenoside L
TN172194987-09-4
Gypenoside L inhibits autophagic flux and induces cell death in human esophageal cancer cells through endoplasm reticulum stress-mediated Ca2+ release. It also inhibit non-small cell lung carcinoma A549 cell inhibitory activity.
  • $128
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Piperlongumine
T694720069-09-4
Piperlongumine (Piplartine) is a natural alkaloid from Piper longum L. It selectively kills cancer cells and strengthens the level of reactive oxygen species (ROS).
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Hederacolchiside A1
T2P2806106577-39-3
Hederacolchiside A1 (Raddeanoside R13) shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and potential. Hederacolchiside A1 shows antiproliferation activities in three cancer cell lines with the IC50 value of 2.4 uM, it exhibits a preferential cytotoxicity on a pigmented melanoma cell line. It suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K Akt mTOR signaling pathway.
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DEL-22379
T6818181223-80-3
DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ~0.5 μM.
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CHPG hydrochloride
T10809L In house
CHPG hydrochloride is a selective agonist of mGluR5.
  • $85
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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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FR 180204
T1956865362-74-9
FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.
  • $36
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ERK5-IN-1
T51841234479-76-5
ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM) and also inhibits LRRK2[G2019S] (IC50: 26 nM).
  • $48
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Pachymic acid
T6S061929070-92-6
Pachymic acid (3-O-Acetyltumulosic acid) is a natural product, and inhibits Akt and ERK signaling pathways.
  • $72
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VX-11e
T3166896720-20-0
VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
  • $50
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Catalposide
TN36096736-85-2
Catalposide is a potent inducer of (HO)-1 isolated from Catalpa ovate G. Don (Bignoniaceae). Catalposide possesses antioxidant, anti-apoptotic, anti-microbial, anti-tumoral, and anti-inflammatory properties.
  • $228
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Corynoxeine
T6S0655630-94-4
1. Corynoxeine is a potent ERK1 2 inhibitor of key PDGF-BB-induced VSMC proliferation and may be useful in the prevention and treatment of vascular diseases and restenosis after angioplasty.
  • $40
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