GF109203X (133052-90-1) Description:
GF-109203X is a potent and highly selective PCK inhibitor, which inhibits PKC isozymes alpha, beta 1, beta 2, gamma, delta and epsilon in vitro . GF-109203X inhibited GSK-3 in vitro, when assayed either in cell lysates (IC(50) 360 nM or in GSK-3beta immunoprecipitates (IC(50) 170 nM derived from rat epididymal adipocytes. Pretreatment of adipocytes with GF-109203X (5 microM) reduced GSK-3 activity in total cell lysates, to 25.1+/-4.3% of control.
Bisindolylmaleimide I (GF 109203X) is a staurosporine (sc-3510) inspired molecule, which has been shown to display equally potent inhibition, but with vastly superior selectivity, for all of the known isoforms of PKC (IC50 = 8-20 nM). Inhibition is competitive with respect to ATP, which suggests that Bisindolylmaleimide I occupies the ATP binding domain of the PKC isoforms. Bisindolylmaleimide I (GF 109203X) has been used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. It inhibits PKC within intact platelets and T cells, Fas-mediated apoptosis, and T cell-mediated autoimmune diseases, as well as GSK-3. Bisindolylmaleimide I (GF 109203X) is an inhibitor of PHK/CaM, PKC α, PKC β, PKC δ, PKC ε, PKC γ and SR/HTR3.
GF109203X (133052-90-1) Specifications:
|Synonym||GF109203X; GF-109203X; GF 109203X; bisindolylmaleimide; GO 6850; GO-6850; GO6850. BIMI.|
|Monoisotopic Mass||412.18993 g/mol|
|Solubility||Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 1:10 DMSO:PBS (pH 7.2) (~0.1 mg/ml). Insoluble in water.|
|Shelf life||>5 years if stored properly|
|Handling||Protect from air and moisture|
|Application||A potent and highly selective PCK inhibitor|