(2Z,3Z)-U0126 is a selective non-competitive inhibitor of MEK1 and MEK2, exhibiting potent anti-inflammatory properties with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. This compound effectively inhibits anchorage-independent growth in Ki-ras-transformed rat fibroblasts by interfering with the extracellular signal-regulated kinase and mammalian target of rapamycin signaling pathways. It also has the potential to undergo isomerization and cyclization, leading to various derivatives with lower affinity for MEK and reduced inhibition of AP-1 activity compared to the original compound.
(2Z,3Z)-U0126 is a selective non-competitive inhibitor of MEK1 and MEK2, exhibiting potent anti-inflammatory properties with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. This compound effectively inhibits anchorage-independent growth in Ki-ras-transformed rat fibroblasts by interfering with the extracellular signal-regulated kinase and mammalian target of rapamycin signaling pathways. It also has the potential to undergo isomerization and cyclization, leading to various derivatives with lower affinity for MEK and reduced inhibition of AP-1 activity compared to the original compound.
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