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.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
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Apoptosis >
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Autophagy >
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Cytoskeleton >
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JAK/STAT Signaling >
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MAPK/ERK Pathway >
ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
ATP Synthase BCRP Calcium Channel CFTR Chloride Channel CRAC Channel CRM1 EAAT2 GABA Receptor GlyT HCN Channel iGluR Monoamine Transporter Monocarboxylate Transporter Na+/Ca2+ Exchanger Na+/HCO3- Cotransporter Na+/K+ ATPase nAChR NKCC P-glycoprotein P2X Receptor Potassium Channel Proton Pump SGLT Sodium Channel TRP Channel URAT1
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15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
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PI3K/Akt/mTOR >
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Protein Tyrosine Kinase/RTK >
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Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
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Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

FR-900359

FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research[1][2][3][4].

  • CAS Number: 107530-18-7
  • MF: C49H75N7O15
  • MW: 1002.16
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML192

ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation[1].

  • CAS Number: 460331-61-7
  • MF: C20H22N4O2S
  • MW: 382.479
  • Catalog: PKC
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Salicyloyltryptamine

N-Salicyloyltryptamine acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect[1]-[5].

  • CAS Number: 31384-98-2
  • MF: C17H16N2O2
  • MW: 280.32100
  • Catalog: Guanylate Cyclase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Gardenin A

Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects[1][2].

  • CAS Number: 21187-73-5
  • MF: C21H22O9
  • MW: 418.39400
  • Catalog: PAK
  • Density: 1.3g/cm3
  • Boiling Point: 624.2ºC at 760 mmHg
  • Melting Point: 162-163ºC
  • Flash Point: 218.5ºC

ERK2 IN-1

ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM[1].

  • CAS Number: 1093061-47-2
  • MF: C36H34FN7O2S
  • MW: 647.76
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ERK-IN-3

ERK-IN-3 is a potent and oral inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.[1].

  • CAS Number: 2055597-12-9
  • MF: C22H25ClFN7O2
  • MW: 473.93
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4′-Demethylnobiletin

4′-Demethylnobiletin is a bioactive metabolite that activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment associated with NMDA receptor antagonism by stimulating ERK signaling[1].

  • CAS Number: 34810-62-3
  • MF: C20H20O8
  • MW: 388.36800
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tauroursodeoxycholate-d4-1

Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

  • CAS Number: 2573035-17-1
  • MF: C26H41D4NO6S
  • MW: 503.73
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BIX02188

BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.

  • CAS Number: 334949-59-6
  • MF: C25H24N4O2
  • MW: 412.484
  • Catalog: ERK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 615.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 326.2±31.5 °C

Sodium tauroursodeoxycholate

Tauroursodeoxycholate Sodium is an ambiphilic bile acid that helps with liver and gallbladder issues.

  • CAS Number: 35807-85-3
  • MF: C26H44NNaO6S
  • MW: 521.685
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ulixertinib hydrochloride

Ulixertinib hydrochloride 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 hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line[1][2].

  • CAS Number: 1956366-10-1
  • MF: C21H23Cl3N4O2
  • MW: 469.79
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MK2-IN-5

MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation[1][2][3].

  • CAS Number: 474713-20-7
  • MF: C61H113N21O16
  • MW: 1396.68
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TIC10

TIC10 is a potent, orally active, and stable TRAIL inducer, also inhibits Akt and ERK activity.

  • CAS Number: 1616632-77-9
  • MF: C24H26N4O
  • MW: 386.489
  • Catalog: TNF Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 559.7±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 292.3±32.9 °C

Ravoxertinib

Ravoxertinib (GDC-0994) is an orally bioavailable ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

  • CAS Number: 1453848-26-4
  • MF: C21H18ClFN6O2
  • MW: 440.858
  • Catalog: ERK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 734.6±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 398.0±35.7 °C

ROCK-IN-5

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of ROCK, ERK, GSK, and AGC protein kinases. ROCK-IN-5 has the potential for proliferative, cardiac and neurodegenerative diseases research[1].

  • CAS Number: 692870-25-0
  • MF: C16H11ClFN3OS
  • MW: 347.79
  • Catalog: ROCK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lidocaine HCl

Lidocaine hydrochloride hydrate (Lignocaine hydrochloride hydrate) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia[1][2].

  • CAS Number: 6108-05-0
  • MF: C14H25ClN2O2
  • MW: 288.814
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: 350.8ºC at 760 mmHg
  • Melting Point: 68.5ºC
  • Flash Point: 166ºC

ERK1/2 inhibitor 7

ERK1/2 inhibitor 7 is a potent ERK inhibitor with an IC50 of 0.94 nM for ERK2 (WO2021110168A1, WX006)[1].

  • CAS Number: 2648455-13-2
  • MF: C23H22FN7OS
  • MW: 463.53
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DEL 22379

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.

  • CAS Number: 181223-80-3
  • MF: C26H28N4O3
  • MW: 444.526
  • Catalog: ERK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 763.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 415.8±32.9 °C

Hydrangenol

Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level[1].

  • CAS Number: 480-47-7
  • MF: C15H12O4
  • MW: 256.253
  • Catalog: COX
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 528.3±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 206.4±23.6 °C

AX 15836

AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.

  • CAS Number: 2035509-96-5
  • MF: C32H40N8O5S
  • MW: 648.78
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Zeatin

(E/Z)-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; (E/Z)-Zeatin also inhibits UV-induced MEK/ERK activation.

  • CAS Number: 13114-27-7
  • MF: C10H13N5O
  • MW: 219.24
  • Catalog: ERK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 395.0±52.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 192.7±30.7 °C

Lidocaine

Lidocaine, an amide local anesthetic, has anti-inflammatory properties in vitro and in vivo, possibly due to an attenuation of pro-inflammatory cytokines, intracellular adhesion molecule-1 (ICAM-1), and reduction of neutrophils influx.Target: Lidocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery. Lidocaine, the first amino amide–type local anesthetic, was first synthesized under the name xylocaine by Swedish chemist Nils Lofgren in 1943. His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself.Lidocaine is approximately 95% metabolized (dealkylated) in the liver by CYP3A4 to the pharmacologically-active metabolites monoethylglycinexylidide (MEGX) and then subsequently to the inactive glycine xylidide. MEGX has a longer half life than lidocaine but also is a less potent sodium channel blocker. The elimination half-life of lidocaine is approximately 90–120 minutes in most patients. This may be prolonged in patients with hepatic impairment (average 343 minutes) or congestive heart failure (average 136 minutes).

  • CAS Number: 137-58-6
  • MF: C14H22N2O
  • MW: 234.337
  • Catalog: Apoptosis
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 372.7±52.0 °C at 760 mmHg
  • Melting Point: 66-69°C
  • Flash Point: 179.2±30.7 °C

ERK5-IN-5

ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC50 value of 6.23 µg/mL for A549 cells[1].

  • CAS Number: 2318792-30-0
  • MF: C19H16ClN3O
  • MW: 337.80
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HIOC

HIOC is a potent and selective activator of TrkB (tropomyosin related kinase B) receptor. HIOC can pass the blood-brain and blood-retinal barriers.HIOC activates TrkB/ERK pathway and decreases neuronal cell apoptosis. HIOC attenuates early brain injury after SAH (subarachnoid hemorrhage). HIOC shows protective activity in an animal model for light-induced retinal degeneration[1][2][3].

  • CAS Number: 314054-36-9
  • MF: C16H19N3O3
  • MW: 301.34
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 746.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 405.0±32.9 °C

Insulin Detemir

Insulin Detemir is an artificial insulin, shows effect on controlling blood sugar levels. Insulin Detemir stimulates GLP-1 secretion as a consequence of enhanced Gcg expression by a mechanism involving activation of Akt- and/or extracellular signal-regulated kinase (ERK)-dependent-cat and CREB signaling pathways. Insulin Detemir can be used for type 2 diabetes research[1][2].

  • CAS Number: 169148-63-4
  • MF: C267H402N64O76S6
  • MW: 5916.82198
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MY-673

MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro[1].

  • CAS Number: 2944459-96-3
  • MF: C18H14N2O4
  • MW: 322.31
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tenuifoliside A

Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells[1].

  • CAS Number: 139726-35-5
  • MF: C31H38O17
  • MW: 682.623
  • Catalog: ERK
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 917.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 291.4±27.8 °C

Rutin hydrate

Rutin hydrate is a flavonol glycoside, able to cross the blood-brain barrier, and acts by inhibiting JNK and ERK1/2 activation and activating mTOR signalling.

  • CAS Number: 207671-50-9
  • MF: C27H3O16.xH2O
  • MW: 664.56300
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 195°C dec. (Lit.)
  • Flash Point: N/A

MEK1 Derived Peptide Inhibitor 1

MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable[1].

  • CAS Number: 355367-87-2
  • MF: C68H118N18O17S
  • MW: 1491.84
  • Catalog: ERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methylnissolin

Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade[1].

  • CAS Number: 73340-41-7
  • MF: C17H16O5
  • MW: 300.306
  • Catalog: ERK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 428.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 213.2±28.7 °C