
产品名称:U0126
化学名:1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)-butadiene
CAS No:109511-58-2
分子式:C18H16N6S2
分子量:380.49
纯度:≥99%
溶解度:Soluble in DMSO at 200 mg/mL, solubility in ethanol or water is low
保存:-20 ºC
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货号:abs810003
规格: 大包装询价
货号 产品名称 规格
abs810003a U0126 5mg
abs810003b U0126 10mg
abs810003c U0126 25mg
abs810003d U0126 50mg
abs810003e U0126 100mg
库存:现货
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生物活性:
U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 was
found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual
specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited
anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both
extracellular signal-regulated 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 shown that U0126
selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with
constitutively activated ERK. Loss of contact with substratum triggers apoptosis in many normal cell types,
a phenomenon termed anoikis. U0126 sensitized MDA-MB231 and HBC4 to anoikis, i.e., upon treatment
with U0126, cells deprived of anchorage entered apoptosis.
U0126 is also a weak inhibitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 and
Cdk4