Key features and details
- Potent, selective PKC inhibitor. Potent GSK-3 inhibitor. Potent 5-HT3 antagonist.
- CAS Number: 133052-90-1
- Purity: > 98%
- Soluble in DMSO to 25 mM
- Form / State: Solid
- Source: Synthetic
Product nameGF 109203X (Bisindolylmaleimide i), PKC inhibitor
DescriptionPotent, selective PKC inhibitor. Potent GSK-3 inhibitor. Potent 5-HT3 antagonist.
- Bisindolylmaleimide I
Biological descriptionPotent, selective PKC inhibitor (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Potent GSK-3 inhibitor (IC50 = 360 nM). Potent 5-HT3 antagonist (Ki = 29.5 nM). Shows anti-inflammatory effects in vivo.
Storage instructionsStore at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 25 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
- Pathways and Processes
- Metabolic signaling pathways
- Energy transfer pathways
- Integration of energy
1.5 x 10e7 THP-1 cells were incubated with 100 nM GF 109203X (ab144264) or Ro 31-8220 mesylate (ab120374) for 30 minutes prior to activation with 10 µg x mL-1 PMA (Sigma) for 4 hours. Control cells were left without inhibitors or PMA. Cells were lysed in 1 mL of lysis buffer, and 30 µL were tested for PKC activity (duplicates; +/- SD).
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
ab144264 has been referenced in 1 publication.
- Sutherland-Deveen ME et al. Differential Regulation of Human Ether-à-Go-Go-Related Gene (hERG) Current and Expression by Activation of Protein Kinase C. Mol Pharmacol 96:1-12 (2019). PubMed: 31015282