1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. 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. Purity: ≥98% by HPLC. Ref.: DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175. Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett. 8, 2839. Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623. |
