Bisindolylmaleimide I

SKU: orb1300703

Description

Bisindolylmaleimide I (GF109203X) is a highly selective and potent protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM. This cell-permeable compound is widely used in both in vitro and in vivo research to investigate PKC signaling pathways in cancer, neuroscience, and cardiovascular studies.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 133052-90-1
• MW: 412.48
• Purity: 98.19%
• Formula: C₂₅H₂₄N₄O₂
• SMILES: CN(C)CCCn1cc(C2=C(C(=O)NC2=O)c2c[nH]c3ccccc23)c2ccccc12
• Target: PKC,PDGFR,GSK-3
• Solubility: DMSO:26.67 mg/mL (64.66 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.42 mM)

Bioactivity

• Target IC50:
  FDGFR:65 μM|PKC (bovine brain):10 nM|PKCγ:20 nM|PKCβII:16 nM|PKC:14 nM|PKCα:20 nM|PKCβI:17 nM
• In Vivo:
  GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats.
• In Vitro:
  Bisindolylmaleimide I, as an ATP-competitive PKC inhibitor, prevents platelet aggregation induced by stimuli that activate PKC, and has the potential as a tool for studying the involvement of PKC in signal transduction pathways. GF 109203X produces reversal activity on P-glycoprotein and MRP -mediated multidrug resistance. PKC inhibition by Bisindolylmaleimide I significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells.
• Cell Research:
  Cell proliferation is monitored by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Cells are seeded in 96-well plates and allowed to grow overnight. The cells are serum-starved for 18–24 hours and then treated with 1 mM carbachol for 48 hours in 100 μL serum-free RPMI 1640. Inhibitors are added 30 min prior to carbachol treatment. Following the treatment, 10 μL of MTT solution (5 mg/ml) is applied to each well, and the plates were incubated for 3 h at 37 °C. After the medium is removed, the formazan crystals formed are solubilized in 100 μL DMSO. The absorbance at 570 nm is measured using a microplate reader and the background absorbance at 690 nm is subtracted. Each assay is performed in triplicate. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bisindolylmaleimide I, PDGFR, inhibit, Go 6850, Go6850, Go-6850, GF109203X, Inhibitor, PKC, PKCβ2, PKCγ, PKCβ1, PKCα, Protein kinase C

Compound Identifiers

PubChem CID

2396