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
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.
Safety
- HS Code
- 2930909899
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.
N-Bromosuccinimide Price
- Product number
- 662005
- Product name
- U0126 - CAS 109511-58-2 - Calbiochem
- Packaging
- 5mg
- Price
- $303
- Updated
- 2024/03/01
- Product number
- 662005
- Product name
- U0126 - CAS 109511-58-2 - Calbiochem
- Packaging
- 10mg
- Price
- $475
- Updated
- 2024/03/01
- 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
- Product number
- J61246
- Product name
- U0126, 99+%
- Packaging
- 25mg
- Price
- $196
- Updated
- 2023/06/20
- Product number
- J61246
- Product name
- U0126, 99+%
- Packaging
- 100mg
- Price
- $349
- Updated
- 2023/06/20
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
U0126 Suppliers
- Tel
- 888-539-0666
- Fax
- 888-539-0666
- info@emmx.com
- Country
- United States
- ProdList
- 8449
- Advantage
- 60
- Tel
- +1-781-999-5354 +1-00000000000
- marketing@targetmol.com
- Country
- United States
- ProdList
- 19892
- Advantage
- 58
- Tel
- +1-708-310-1919 +1-13798911105
- Fax
- 708-557-7486
- sales@invivochem.cn
- Country
- United States
- ProdList
- 6393
- Advantage
- 58
- Tel
- +1 (732)236-3202
- sales@cckinase.com
- Country
- United States
- ProdList
- 2738
- Advantage
- 58
- Tel
- +1-833-552-7181
- sales@aladdinsci.com
- Country
- United States
- ProdList
- 57511
- Advantage
- 58
View Lastest Price from U0126 manufacturers
- 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