U0126-CAS109511-58-2-Calbiochem , 109511-58-2
Synonym(s):
InSolution U0126 - CAS 109511-58-2 - Calbiochem;Kinase inhibitor;MEK inhibitor
| Pack Size | Price | Stock | Quantity |
| 1MG | RMB881.78 | In Stock |
|
| 5MG | RMB2736.62 | In Stock |
|
| 10MG | RMB4250.78 | In Stock |
|
| 20MG | RMB6975.16 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| 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. |
| InChI | 1S/C18H16N6S2/c19-9-11(17(23)25-15-7-3-1-5-13(15)21)12(10-20)18(24)26-16-8-4-2-6-14(16)22/h1-8H,21-24H2/b17-11+,18-12+ |
| InChIKey | DVEXZJFMOKTQEZ-JYFOCSDGSA-N |
| SMILES | S(c2c(cccc2)N)\C(=C(\C(=C(\Sc1c(cccc1)N)/N)\C#N)/C#N)\N |
Description and Uses
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).
A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2 with IC50s of 70 nM and 60 nM, respectively.
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P280a-P304+P340-P305+P351+P338-P405-P501a |
| WGK Germany | WGK 1 |
| HS Code | 2930909899 |
| Storage Class | 10 - Combustible liquids |
