U0126 monoethanolate

• Catalog No.: U120
• M. F.: C20H22N6OS2
• M. W.: 426.55828
• Purity: ≥98% (HPLC)
• Storage: protect from light

SYNONYMS

• IUPAC name: bis({amino[(2-aminophenyl)sulfanyl]methylidene})butanedinitrile; ethanol
• IUPAC Traditional name: bis({amino[(2-aminophenyl)sulfanyl]methylidene})butanedinitrile; ethyl alcohol
• Synonyms: 1,4-Diamino-2,3-dicyano-1,4-bis(o-aminophenylmercapto)butadiene monoethanolate

DATABASE IDS

• PubChem SID: 24278770

PROPERTIES

• Empirical Formula (Hill Notation): C18H16N6S2 · C2H5OH
• Purity: ≥98% (HPLC)
• Gene Information: human ... MAP2K1(5604), MAP2K2(5605)
• Apperance: white to off-white powder
• Solubility: DMSO: >10 mg/mL (Stock solutions in DMSO should be used within a month. Acidic solutions exhibit weaker inhibition)
• Personal Protective Equipment: Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter
• Storage Condition: protect from light
• Storage Temperature: 2-8°C
• German water hazard class: 3

DETAILS

Description (English)

Caution
photosensitive
Biochem/physiol Actions
U0126, 1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio] butadiene, is a highly selective inhibitor of both MEK1 and MEK2. 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.

Description (简体中文)

Caution
photosensitive
Biochem/physiol Actions
U0126, 1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio] butadiene, is a highly selective inhibitor of both MEK1 and MEK2. 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.