U-0126 |
Catalog No.GC45099
One-Click Copy Product Info
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A MEK inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 109511-58-2
Sample solution is provided at 25 µL, 10mM.
U-0126 is a MEK inhibitor with IC50 values of 72 nM and 58 nM for MEK1 and MEK2, respectively. [1] 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).[2] It increases the ratios of ADP to ATP and AMP to ATP and increases phosphorylation of the AMPK target acetyl-CoA carboxylase (ACC).
Reference:
[1]. Favata, M.F., Horiuchi, K.Y., Manos, E.J., et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J. Biol. Chem. 273(29), 18623-18632 (1998).
[2]. Dokladda, K., Green, K.A., Pan, D.A., et al. PD98059 and U0126 activate AMP-activated protein kinase by increasing the cellular AMP:ATP ratio and not via inhibition of the MAP kinase pathway. FEBS Lett. 579(1), 236-240 (2005).
| Cas No. | 109511-58-2 | SDF | |
| Chemical Name | 2,3-bis[amino[(2-aminophenyl)thio]methylene]-butanedinitrile | ||
| Canonical SMILES | N/C(SC1=CC=CC=C1N)=C(C#N)\C(C#N)=C(N)\SC2=C(N)C=CC=C2 | ||
| Formula | C18H16N6S2 | M.Wt | 380.5 |
| Solubility | 0.5mg/mL in ethanol, 25mg/mL in DMSO, 30mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6281 mL | 13.1406 mL | 26.2812 mL |
| 5 mM | 525.6 μL | 2.6281 mL | 5.2562 mL |
| 10 mM | 262.8 μL | 1.3141 mL | 2.6281 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
LGG-s lost the improvement of barrier function after MEK inhibition.B–D IF staining and quantification of ZO-1, Occludin, and Claudin-1. Scale bar = 50 μm.
In the LPS +LGG-s + U0126 (MEKinhibitor,used at 10 μM, GlpBio, Montclair, CA, USA) group, the cells were pretreated with LGG-s at three concentration gradients (1:100, 1:50, and1:25) for 3 h, then treated with LPS and U0126 for 24 h.
Cell Death & Disease 14.1 (2023): 68. PMID: 36709322 IF: 9.6963 -
Related Biological Data
HCV core protein regulated the expression of PEA3 and SRF/c-Fos via the MAPK/ERK signaling pathway in liver cells. B. L02-Neo, L02-Core and Huh7-Core cells were treated with U0126 (0, 100 and 200 mmol) for 24 h.
In some experiments, cells were treated with 0, 100, and 200 mmol U0126 (ERK1/2 inhibitor; #GC45099, Glpbio, Montclair, CA, USA) for 24 h.
Archives of Medical Research (2022). PMID: 35817647 IF: 8.3235 -
Related Biological Data
Inhibition of the ERK signaling pathway attenuated IAA-mediated alleviation of colitis.A Western blot was conducted to confirm that the ERK inhibitor U0126 successfully inhibited the ERK pathway (E).
To demonstrate the influence of IAA on the ERK pathway,U0126 (GLPBIO) was intraperitoneally injected daily to inhibit ERK at a dose of 20 mg/kg.
Archives of Pharmacal Research (2024): 1-12. PMID: 38489148 IF: 6.7
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)