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erk

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  • Inhibitors & Agonists
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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).
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Tizaterkib
AZD-0364
T104292097416-76-5
Tizaterkib (AZD-0364) is a potent and selective ERK2 inhibitor.
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PAF (C16)
C16-PAF
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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6-8 weeks
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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.
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pd98059
PD 98059
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.
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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.
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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.
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Tauroursodeoxycholate
Ursodeoxycholyltaurine, UR 906, TUDCA, Tauroursodeoxycholic Acid, Taurolite
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.
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MK-8353
SCH900353
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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8-10 weeks
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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. It regulates the cell cycle and exhibits anti-melanin tumor activities.
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trans-Zeatin
(E)-Zeatin
TMS21811637-39-4
trans-Zeatin ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing.
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bongkrekic acid
Bongkrek 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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7-10 days
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FR 180204
FR180204
T1956865362-74-9
FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.
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Ravoxertinib
GDC-0994
T65111453848-26-4
Ravoxertinib (GDC-0994) is an efficacious, orally available ERK1 2 inhibitor with an IC50 of 1.1 0.3 nM.
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bix02189
BIX 02189
T212951265916-41-3
BIX02189 is a potent and selective inhibitor of MEK5 and ERK5 (IC50: 1.5 nM and 59 nM).
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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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7-10 days
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β,β-Dimethylacrylshikonin
β, β-Dimethylacrylshikonin, Dimethylacrylshikonin
T3S234424502-79-2
1. β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) is a promising agent for developing an improved strategy for radiotherapy against tumors. (a) Injection of Dimethylacrylshikonin combined with IR treatment significantly suppressed tumor growth of the HCT-116 xenograft. (b) Dimethylacrylshikonin significantly suppressed the growth of H(22) transplantable hepatoma, and induced the activation of caspase-3 . (c) Dimethylacrylshikonin inhibited growth of gastric cancer SGC-791 cells by inducing ERK signaling pathway. 2. Dimethylacrylshikonin inhibits the proliferation of MCF-7 cells in vitro by inducing apoptosis through the downregulation of Bcl-2, upregulation of Bax and partial inactivation of the NF-κB pathway.
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XMD8-92
T18431234480-50-2
XMD8-92 is an effective and specific BMK1 ERK5 inhibitor (Kd: 80 nM).
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Methylnissolin
3-Hydroxy-9,10-dimethoxyptercarpan
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.
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xmd17-109
XMD17 109, ERK5-IN-1
T18421435488-37-1
XMD17-109 (ERK5-IN-1) is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells).
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Deltonin
T384455659-75-1
Deltonin has an inhibition of ERK1 2 and AKT activation. Deltonin shows cytotoxicity against human HepG2 cells (IC50: 7.66 μM), mouse C26 cells (IC50: 1.22 μM), and human MDA-MB-231 cells (IC50: 1.58 μM).
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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).
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broussonin a
TN353973731-87-0
Broussonins A and B, new phytoalexins from diseased paper mulberry. Broussonin A shows estrogenic activity with ligand-binding activity of estrogen receptor, transcriptional activity of estrogen-responsive element-luciferase reporter genes. Broussonin A c
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VX-11e
VTX-11e, Vertex-11e, TCS ERK 11e
T3166896720-20-0
VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
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