General description
A potent and specific inhibitor of MEK1 (IC50 = 72 nM) and MEK2 (IC50 = 58 nM). The inhibition is noncompetitive with respect to both 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. 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. Reported to undergo rapid isomerization in DMSO and exist as an equilibrium mixture of (Z,Z), E,E) and (Z,E) isomers with minimal loss of activity over a period of 1 month.
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Physical form
A 100 mM (5 mg/124 µl) solution of U0126 (Cat. No. 662005) in DMSO.
Reconstitution
Following initial thaw, aliquot into precooled vials, freeze immediately at (-70°C).
Other Notes
Duncia, J.V., et al. 1998. Bioorg. Med. Chem. Lett.8, 2839.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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- UPC:
- 51112015
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 662009-5MG
- CAS:
- 109511-58-2
- Temperature Control Device:
- Yes