U0126-EtOH
Catalog No.: GC12807Purity:>98.00%
U0126-EtOH is a non-ATP competitive and selective inhibitor of MEK1 and MEK2 with IC50 values of 72nM and 58nM, respectively.
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Cas No.: 1173097-76-1
10mM (in 1mL DMSO)In Stock
$60.00
1
5mgIn Stock
$33.00
1
10mgIn Stock
$53.00
1
50mgIn Stock
$147.00
1
100mgIn Stock
$243.00
1
200mgIn Stock
$353.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $60.00 | In Stock | 1 | |
| 5mg | $33.00 | In Stock | 1 | |
| 10mg | $53.00 | In Stock | 1 | |
| 50mg | $147.00 | In Stock | 1 | |
| 100mg | $243.00 | In Stock | 1 | |
| 200mg | $353.00 | In Stock | 1 |
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Citations
3 publicationsPublications from researchers using this productDescription
U0126-EtOH is a non-ATP competitive and selective inhibitor of MEK1 and MEK2 with IC50 values of 72nM and 58nM, respectively[1]. U0126-EtOH inhibits the activity of the ERK signaling pathway, thereby decreasing progesterone production and the expression of steroidogenic enzymes and steroidogenic factor 1 (SF1)[2]. U0126-EtOH has been widely used in parasitological research to inhibit the growth of Echinococcus granulosus in mice[3].
In vitro, U0126-EtOH treatment (0.5μM) for 24 hours led to a decrease in the phosphorylation level of ERK1/2 and the expression of cyclin D1 in H520 cells[4]. Treatment with 10μM U0126-EtOH in combination with 1μM Purmorphamine for 48 hours inhibited the activity of Rheumatoid arthritis (RA)-fibroblast-like synoviocytes (FLS) cells and altered the distribution of the cell cycle[5]. Treatment with 10μM U0126-EtOH for 8 hours significantly suppressed the invasion of A375 cells and reduced the secretion of uPA and MMP-9[6].
In vivo, U0126-EtOH treatment via a single tail vein injection of 10mg/kg alleviated acute renal failure induced by cisplatin in mice and reduced renal cell apoptosis[7]. Intraperitoneal injection of U0126-EtOH (30mg/kg) at 0 hour and 24 hours after reperfusion improved long-term neurological function in female rats following experimental stroke[8].
References:
[1] Favata M F, Horiuchi K Y, Manos E J, et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase[J]. Journal of Biological Chemistry, 1998, 273(29): 18623-18632.
[2] Xu P, Bao R, Zhang Y, et al. Prolyl oligopeptidase regulates progesterone secretion via the ERK signaling pathway in murine luteal cells[J]. Molecular reproduction and development, 2019, 86(6): 714-726.
[3] Zhang C, Li J, Aji T, et al. Identification of functional MKK3/6 and MEK1/2 homologs from Echinococcus granulosus and investigation of protoscolecidal activity of mitogen-activated protein kinase signaling pathway inhibitors in vitro and in vivo[J]. Antimicrobial Agents and Chemotherapy, 2019, 63(1): 10.1128/aac. 01043-18.
[4] Fu H, Gao H, Qi X, et al. Aldolase A promotes proliferation and G1/S transition via the EGFR/MAPK pathway in non-small cell lung cancer[J]. Cancer Communications, 2018, 38(1): 18.
[5] Liu F, Feng X X, Zhu S L, et al. Sonic hedgehog signaling pathway mediates proliferation and migration of fibroblast-like synoviocytes in rheumatoid arthritis via MAPK/ERK signaling pathway[J]. Frontiers in immunology, 2018, 9: 2847.
[6] Ge X, Fu Y M, Meadows G G. U0126, a mitogen-activated protein kinase kinase inhibitor, inhibits the invasion of human A375 melanoma cells[J]. Cancer letters, 2002, 179(2): 133-140.
[7] Jo S K, Cho W Y, Sung S A, et al. MEK inhibitor, U0126, attenuates cisplatin-induced renal injury by decreasing inflammation and apoptosis[J]. Kidney international, 2005, 67(2): 458-466.
[8] Ahnstedt H, Mostajeran M, Blixt F W, et al. U0126 attenuates cerebral vasoconstriction and improves long-term neurologic outcome after stroke in female rats[J]. Journal of Cerebral Blood Flow & Metabolism, 2015, 35(3): 454-460.
Protocol
| Cell experiment [1]: | |
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Cell lines |
A375 cells |
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Preparation Method |
A375 cells were cultured in minimal essential medium supplemented with 10% fetal bovine serum, sodium pyruvate, non-essential amino acids, 2mM l-glutamine, 60IU/ml penicillin, and 100IU/ml streptomycin at 37°C with 5% ambient CO2. The in vitro invasion assay was performed in a 24-well trans-well plate with 8μm pore size filter inserts coated with growth factor reduced Matrigel. Cells (5×104) in 500μl minimal essential medium in the absence or presence of different concentrations of U0126-EtOH (0, 1, 5, and 10μM) were plated into Matrigel-coated filter insert. A volume of 800μl of minimal essential medium in the absence or presence of different concentrations of U0126-EtOH (0, 1, 5, and 10μM) was added to the lower compartment of the invasion chamber. The chamber was incubated at 37°C for 8 h in 5% CO2. After incubation, the cells on the upper side of the insert filter were removed using cotton swabs. Invasion of A375 cells was measured. |
|
Reaction Conditions |
0, 1, 5, and 10μM; 8h |
|
Applications |
U0126-EtOH treatment reduced invasion of A375 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Male balb/c mice |
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Preparation Method |
Male balb/c mice (6-week-old) were housed on a 12h light/dark cycle and had free access to food and water at 22°C. Cisplatin was dissolved in normal saline at a concentration of 2mg/ml and mice were given a single intraperitoneal injection of 20mg/kg cisplatin and control animals received same volume of normal saline. One hour before cisplatin administration, either vehicle (0.1% DMSO in normal saline) or U0126-EtOH (10mg/kg) was injected intravenously via tail vein. Mice were sacrificed at 24, 48, and 72 hours after cisplatin administration. Kidneys were collected and processed for histology. |
|
Dosage form |
10mg/kg; once; tail vein injection |
|
Applications |
U0126-EtOH treatment markedly alleviated acute renal failure induced by cisplatin in mice and reduced renal cell apoptosis. |
References: [1] Ge X, Fu Y M, Meadows G G. U0126, a mitogen-activated protein kinase kinase inhibitor, inhibits the invasion of human A375 melanoma cells[J]. Cancer letters, 2002, 179(2): 133-140. [2] Jo S K, Cho W Y, Sung S A, et al. MEK inhibitor, U0126, attenuates cisplatin-induced renal injury by decreasing inflammation and apoptosis[J]. Kidney international, 2005, 67(2): 458-466. | |
Product Documents
Purity:>98.00%Appearance:A solid
Biological Data
1 / 2
Chemical Properties
CAS No.
1173097-76-1
Chemical Name
(2Z,3Z)-2,3-bis[amino-(2-aminophenyl)sulfanylmethylidene]butanedinitrile;ethanol
SMILES
CCO.C1=CC=C(C(=C1)N)SC(=C(C#N)C(=C(N)SC2=CC=CC=C2N)C#N)N
Molecular Formula
C18H16N6S2.C2H6O
Molecular Weight
426.56
Solubility
50 mg/ml in DMSO (Need ultrasonic)
Storage
Store at -20°C
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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