1. Epigenetics
  2. PKC
  3. Bisindolylmaleimide I

Bisindolylmaleimide I (Synonyms: GF109203X; Go 6850)

Cat. No.: HY-13867 Purity: 98.14%
Handling Instructions

Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.

For research use only. We do not sell to patients.

Bisindolylmaleimide I Chemical Structure

Bisindolylmaleimide I Chemical Structure

CAS No. : 133052-90-1

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10 mM * 1  mL in DMSO USD 77 In-stock
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Based on 6 publication(s) in Google Scholar

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Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.

IC50 & Target[1]

Bovine brain PKC

10 nM (IC50)


16 nM (IC50)


17 nM (IC50)


20 nM (IC50)


20 nM (IC50)


65 μM (IC50)

In Vitro

Bisindolylmaleimide I is a competitive inhibitor with respect to ATP (Ki=14 nM) and displays high selectivity for PKC as compared to five different protein kinases. GF 109203X efficiently prevents PKC-mediated phosphorylations of an Mr=47,000 protein in platelets and of an Mr=80,000 protein in Swiss 3T3 cells. GF 109203X inhibits collagen- and a-thrombin-induced platelet aggregation as well as collagen-triggered ATP secretion. However, ADP-dependent reversible aggregation is not modified. In Swiss 3T3 fibroblasts, GF 109203X reverses the inhibition of epidermal growth factor binding induced by phorbol 12,13-dibutyrate and prevents [3H] thymidine incorporation into DNA, only when this is elicited by growth promoting agents which activate PKC[1].

In Vivo

Pial arteriole diameter changes are monitored using a closed cranial window in vivo microscopy technique. The pial arteriole dilatory response associated with SNS is decreased by 45%, when comparing DM vs either ND or TR rats. Also, pial arteriolar dilations to topical KCl and NS1619 are largely attenuated in DM rats, but not in ND or TR animals. These responses are completely restored by the acute application of Bisindolylmaleimide I to the brain surface. The PKC inhibitor has no effect on vascular responses in normoglycemic and TR animals. In conclusion, DM-associated chronic impairment of neurovascular coupling may be readily reversed by a PKC-α/β/γ inhibitor or prevented via pancreatic islet transplantation. Specific PCK isoforms (α/β/γ) are believed to be mechanistically linked to the neurovascular uncoupling seen with hyperglycemia[2].

Molecular Weight









Room temperature in continental US; may vary elsewhere.


4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (77.58 mM)

*"≥" means soluble, but saturation unknown.

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4244 mL 12.1218 mL 24.2436 mL
5 mM 0.4849 mL 2.4244 mL 4.8487 mL
10 mM 0.2424 mL 1.2122 mL 2.4244 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
Kinase Assay

Assay of PKC is arrayed by measuring 32Pi transferred from [γ-32Pi] ATP to lysine-rich histone type Ill-s. The reaction mixture (80 μL) contains 50 mM Tris-HCI, pH 7.4. 100 μM CaCl2, 10 mM MgCI2, 37.5 μg/mL histone type Ill-s, l0 μM [γ-32Pi] ATP (1250cpm/pmol), 31 μM bovine brain phosphatidylserine and 0.5 μM 1,2 sn-dioleylglycerol. 15 μL of purified PKC (final concentration in assay 0.38 μg/mL) is added to the incubation mixture. After 10 minutes, the reaction is stopped by addition of at 30 μL of casein 30 mg/mL and 0.9 mL of 12% trichlomacetic acid[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Three sets of Lewis rats is used for this study: 1) euglycemic 4–6 month old non-diabetic controls (ND group, n=11); 2) streptozotocin (STZ)-treated diabetic rats (6 month old, 4 months post-STZ) (DM group, n=6); and 3) STZ-treated diabetic animals, subjected to pancreatic islet transplantation soon after the establishment of the diabetic model, studied 100–110 days after the transplant (TR group, n=7)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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Bisindolylmaleimide IGF109203XGo 6850Go6850Go-6850PKCProtein kinase CInhibitorinhibitorinhibit

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