U0126

5 mg

Cat. No.: 84-P22

$99.00

U0126 is a highly selective inhibitor of both MEK1 (IC50 of 72nM) and MEK2 (IC50 of 58 nM). U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-related kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways. The effects of U0126 on the growth of eight human breast cancer cell lines have shown that U0126 selectively represses anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. Upon treatment with U0126, cells deprived of anchorage entered apoptosis.

 

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TECHNICAL INFORMATION

Other Names: 1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio] butadiene

Chemical Formula: C18H16N6S2

CAS Number: 109511-58-2

Molecular Weight: 380.49

Purity:  99% pure

Appearance: White solid

Melting Point: 156°- 159°C

Solubility: DMSO

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C.

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO at 200mg/ml. U0126 is very poorly soluble in ethanol and water. The maximum solubility in water is estimated to be 10-50µl.

 

References

Favata MF et al. (1998). Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem. 273 (29):18623-32.

DeSilva D et al. (1998). Inhibition of mintogen-activated protein kinase kinase blocks T cell proliferation but does not induce or prevent anergy. J Immunol. 160(9): 4175-81.

Steinberg R et al. (2007). A protein kinase Cepsilion-anti-apoptotic kinase signaling complex protects human vascular endothelial cells against apoptosis through induction of Bcl-2. J Biol Chem. 282 (44):32288-97.

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