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
- Molecular Weight:
- 380.49
- MDL Number:
- MFCD09971039
- MOL File:
- 109511-58-2.mol
- MSDS File:
- SDS
| 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). |
| form | White solid |
| pka | 2.11±0.10(Predicted) |
| 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. |
| FDA UNII | 8027P94HLL |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P280a-P304+P340-P305+P351+P338-P405-P501a |
| HS Code | 2930909899 |
U0126 price More Price(39)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 662005 | U0126 - CAS 109511-58-2 - Calbiochem | 109511-58-2 | 5mg | $303 | 2024-03-01 | Buy |
| Sigma-Aldrich | 662005 | U0126 - CAS 109511-58-2 - Calbiochem | 109511-58-2 | 10mg | $475 | 2024-03-01 | Buy |
| Sigma-Aldrich | 19-147 | U0126 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. | 109511-58-2 | 1MG | $181 | 2024-03-01 | Buy |
| Alfa Aesar | J61246 | U0126, 99+% | 109511-58-2 | 25mg | $196 | 2023-06-20 | Buy |
| Alfa Aesar | J61246 | U0126, 99+% | 109511-58-2 | 100mg | $349 | 2023-06-20 | Buy |
U0126 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29797 | 60 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| Zhengzhou Alfa Chemical Co.,Ltd | +8618530059196 | sale04@alfachem.cn | China | 12468 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| Shanghai UCHEM Inc. | +862156762820 +86-13564624040 | sales@myuchem.com | China | 6710 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Henan Aochuang Chemical Co.,Ltd. | +86-0371-63689365 +8618638391208 | sales@aochuangchem.com | China | 9425 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
View Lastest Price from U0126 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2022-09-23 | 2,3-bis(amino((2-aminophenyl)thio)methylene)butanedinitrile
109511-58-2
|
US $0.00-0.00 / kg | 1kg | 98% | 1Ton | Henan Aochuang Chemical Co.,Ltd. |
-
- 2,3-bis(amino((2-aminophenyl)thio)methylene)butanedinitrile
109511-58-2
- US $0.00-0.00 / kg
- 98%
- Henan Aochuang Chemical Co.,Ltd.