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;Bis[amino(o-aminophenylthio)methylene]succinonitrile
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 77 France 1 Germany 3 Japan 2 Switzerland 2 United Kingdom 8 United States 23 Global 116
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
94657
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15839
Advantage
69
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Ascent Scientific
Tel
4401179829988
Fax
4402030 700 369
Email
customerservice@ascentscientific.co.uk
Country
United Kingdom
ProdList
279
Advantage
60
Chemsky (shanghai) International Co.,Ltd
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
15402
Advantage
60
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com (International market)
Country
China
ProdList
1856
Advantage
62
Tianjin YongSheng Biotechnology Co., Ltd.
Tel
022-60987737 13512258274
Fax
86-022-23500597
Email
sales@immortalbio.com
Country
China
ProdList
154
Advantage
55
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Nanjing Norris-Pharm Technology Co., Ltd
Tel
13901585132
Fax
+86-25-52131256
Email
799750417@qq.com
Country
China
ProdList
8878
Advantage
55
China Kouting Group Limited
Tel
+86 (21) 5811-6473 5811-6475
Fax
+86 (21) 6129-4103
Email
sales@koutingchina.com
Country
China
ProdList
496
Advantage
60
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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:

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  • 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
  • 109511-58-2
  • 109522-58-2
  • C18H16N6S2
  • Signalling
  • Protein Kinase
  • Inhibitor