ChemicalBook > CAS DataBase List > U0126

U0126

Product Name
U0126
CAS No.
109511-58-2
Chemical Name
U0126
Synonyms
U0126;UO 126;CS-1122;U0126 >99%;U0126, >=98%;U0126;U 0126;U0126 (Uo126);U 0126 - U 126;1,4-DIAMINO-2,3-DICYANO-1;U0126, Selective MKK inhibitor
CBNumber
CB4758734
Molecular Formula
C18H16N6S2
Formula Weight
380.49
MOL File
109511-58-2.mol
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U0126 Property

Melting point:
approximate 154℃(dec.)
Boiling point:
565.1±50.0 °C(Predicted)
Density 
1.44
RTECS 
EJ9710000
storage temp. 
Desiccate at +4°C
solubility 
Soluble in DMSO (up to 200 mg/ml).
pka
2.11±0.10(Predicted)
form 
White solid
color 
White
Water Solubility 
Soluble in DMSO. Poorly soluble in ethanol and water
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
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Safety

HS Code 
2930909899
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
662005
Product name
U0126 - CAS 109511-58-2 - Calbiochem
Packaging
5mg
Price
$303
Updated
2024/03/01
Sigma-Aldrich
Product number
662005
Product name
U0126 - CAS 109511-58-2 - Calbiochem
Packaging
10mg
Price
$475
Updated
2024/03/01
Sigma-Aldrich
Product number
19-147
Product name
U0126
Purity
U0126 is a elective inhibitor of MEK-1 and MEK-2; weak inhibitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Abl, Cdk2 and Cdk4.
Packaging
1MG
Price
$181
Updated
2024/03/01
Alfa Aesar
Product number
J61246
Product name
U0126, 99+%
Packaging
25mg
Price
$196
Updated
2023/06/20
Alfa Aesar
Product number
J61246
Product name
U0126, 99+%
Packaging
100mg
Price
$349
Updated
2023/06/20
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U0126 Chemical Properties,Usage,Production

Description

U-0126 is a MEK inhibitor with IC50 values of 72 nM and 58 nM for MEK1 and MEK2, respectively. It is noncompetitive with respect adenosine triphosphate (ATP) and its phosphorylation target ERK and it shows little to no inhibition against a number of other kinases including PKC, Ab1, Raf, MEKK, ERK, JNK, MKK-3, MKK-4, MKK-6, Cdk2, and Cdk4. However, U-0126 does phosphorylate and activate AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC50 = 15 μM in HEK293 cells). It increases the ratios of ADP to ATP and AMP to ATP and increases phosphorylation of the AMPK target acetyl-CoA carboxylase (ACC).

Uses

A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2 with IC50s of 70 nM and 60 nM, respectively.

Uses

U0126 is a MEK inhibitor.

Definition

ChEBI: A dinitrile that is succinonitrile in which the methylene hydrogens at positions 2 and 3 are substituted by (2-aminophenyl)sulfanyl]methylidene groups. A potent and selective non-competitive inhibitor of MAP kinase kinase.

General Description

A potent and specific inhibitor of MEK1 (IC50 = 72 nM) and MEK2 (IC50 = 58 nM). The inhibition is noncompetitive with respect to MEK substrates, ATP and ERK. Has very little effect on other kinases, such as Abl, Cdk2, Cdk4, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, PKC, and Raf. Shown to block doxazosin-induced osteoblastic differentiation. U0126 also acts as an immunosuppressant by effectively blocking IL-2 synthesis and T cell proliferation without affecting the long-term outcomes of either T cell activation or tolerance. Noncompetitive with respect to ATP. Also available in InSolution format (Cat. No. 662009.

Biological Activity

Potent and selective non-competitive inhibitor of MAP kinase kinase. Inhibits MEK-1 and MEK-2 (IC 50 values of 0.07 and 0.06 μ M respectively) with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. Centrally active following systemic administration in vivo . Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™ .

Biochem/physiol Actions

Primary TargetMEK1 and MEK2

storage

+4°C (desiccate)

References

1) Favata et al. (1998), Identification of a novel inhibitor of mitogen activated protein kinase kinase; J. Biol. Chem., 273 8623 2) Miyoshi et al. (2012), Antitumor activity of MEK and PI3K inhibitors against malignant pleural mesothelioma cells in vitro and in vivo; Int. J. Oncol., 41 449 3) Pricola et al. (2009), Interleukin-6 Maintains Bone Marrow-Derived Mesenchymal Stem Cell Stemness by an ERK1/2-Dependent Mechanism; J. Cell Biochem., 108 577

U0126 Preparation Products And Raw materials

Raw materials

Preparation Products

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U0126 Suppliers

China 79 France 1 Germany 3 Japan 2 Switzerland 2 United Kingdom 8 United States 24 Global 119
EMMX Biotechnology LLC
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View Lastest Price from U0126 manufacturers

Henan Aochuang Chemical Co.,Ltd.
Product
2,3-bis(amino((2-aminophenyl)thio)methylene)butanedinitrile 109511-58-2
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1Ton
Release date
2022-09-22

109511-58-2, U0126Related Search:

RARECHEM BG FB 0126 IFLAB-BB F2108-0126 2-Quinoxalinecarbaldehyde RARECHEM AH CK 0126 Succinonitrile IFLAB-BB F1084-0126 RARECHEM BK PT 0126 RARECHEM AL BI 0126 RARECHEM AH PB 0126 RARECHEM AL BO 0126 AKOS PAO-0126 U0126 AKOS MSC-0126 AKOS BB/0126 AKOS BAR-0126 AKOS TOT-0126 IFLAB-BB F2593-0126 RARECHEM AK HW 0126

  • U0126
  • 1,4-DIAMINO-2,3-DICYANO-1,4-BIS(2-AMINOPHENYLTHIO)BUTADIENE
  • 1,4-DIAMINO-2,3-DICYANO-1,4-BIS(2-AMINOPHYNYLTIO)BUTADIENE
  • 1,4-DIAMINO-2,3-DICYANO-1,4-BIS(O-AMINOPHENYLMERCAPTO)BUTADIENE
  • 1,4-DIAMINO-2,3-DICYANO-1
  • UO 126
  • U0126 >99%
  • 2,3-Bis[amino[(2-aminophenyl)thio]methylene]butanedinitrile
  • Bis[amino(o-aminophenylthio)methylene]succinonitrile
  • U0126, >=98%
  • (2Z,3Z)-2,3-bis(amino((2-aminophenyl)thio)methylene)succinonitrile
  • (2Z,3Z)-bis{amino[(2-aminophenyl)sulfanyl]methylidene}butanedinitrile
  • Butanedinitrile,2,3-bis[aMino[(2-aMinophenyl)thio]Methylene]-
  • U0126 (Uo126)
  • U 0126 - U 126
  • CS-1122
  • U0126;U 0126
  • (2Z,3Z)-2,3-bis(amino((2-aminophenyl)thio)methylene)succinonitrile/U0126
  • 2,3-Bis(amino((2-aminophenyl)thio)methylene)succinonitrile
  • U0126, Selective MKK inhibitor
  • 109511-58-2
  • 109522-58-2
  • C18H16N6S2
  • Signalling
  • Protein Kinase
  • Inhibitor