Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine.1 It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα-, β1-, β2-, γ-, δ-, and ε-isozymes.1 BIM I directly inhibits GSK3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).2 This compound also competitively antagonizes the 5-HT3 receptor with a Ki value of 61 nM.3
1Toullec, D., Pianetti, P., Coste, H., et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem266(24)15771-15781(1991).
2Hers, I., Tavaré, J.M., and Denton, R.M.The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett460433-436(1999).
3Coultrap, S.J., Sun, H., Tenner, T.E., et al. Competitive antagonism of the mouse 5-hydroxytryptamine receptor by bisindolylmaleimide I, a “selective” protein kinase C inhibitor. J Pharmacol Exp Ther290(1)76-82(1999).
Cayman Chemical Company regularly evaluates our shipping methods to ensure product stability is maintained and our corporate environmental impact is minimized. Products selected for review are evaluated and shipping methods are certified by our Scientists. While occasionally our method of shipping a product may change, rest assured the shipping conditions on all Cayman Chemical products have been reviewed and validated.
Upon receipt, it is important to check the storage requirements of your products and place them at the appropriate temperature. Products shipped without ice may require frozen storage for long term stability.
Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.
Manufacturer, supplier, and vendor of biochemical reagents, assay kits, forensic chemistry standards, antibodies, and proteins for scientific research
Analytical testing services and custom synthesis also available