| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C23H20N4O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Bisindolylmaleimide III is an inhibitor of protein kinase C (PKC), with IC50 values of 0.26 μM, 5.7 μM, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. It also inhibits several off-targets, with IC50 values of 0.17 μM, 1 μM, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively, and a Ki of 16.5 μM for NQO2. The compound selectively binds activated Rsk1 following EGF stimulation and can be used to detect the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK, in studies of signal transduction and colorectal cancer[1][2][3]. It is supplied as a brown to reddish brown solid (C23H20N4O2, MW 384.43) at 98.95% purity.
Physical & Chemical Properties
| CAS Number | 137592-43-9 |
|---|---|
| Molecular Formula | C23H20N4O2 |
| Molecular Weight | 384.43 g/mol |
| Purity | 98.95% |
| Appearance | Solid |
| Color | Brown to reddish brown |
| SMILES | O=C(C(C1=CN(CCCN)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O |
| Target | PKCα, PKCδ, PKCμ, cdk2/cyclin A, NQO2 |
| Signaling Pathway | Epigenetics; TGF-beta/Smad; Cytoskeleton; Metabolic Enzyme/Protease; Neuronal Signaling; Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 25 mg/mL (65.03 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
PKCα 0.26 μM (IC50) |
PKCδ 5.7 μM (IC50) |
PKCμ 6 μM (IC50) |
cdk2/cyclin A 1 μM (IC50) |
NQO2 16.5 μM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (65.03 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 1.25 mg/mL (3.25 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.25 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (12.5 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 1.25 mg/mL (3.25 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 1.25 mg/mL. For 1 mL of working solution: add 100 μL DMSO stock (12.5 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
In human IM-9 lymphocytes, Bisindolylmaleimide III (75 min) potently and selectively inhibits PKCα, reducing PDBu-induced hGH-BP release with an IC50 of 0.33 μM[2]. Phosphorylation of the PDBu-enhanced 42, 45, 53 and 83 kDa extracellular proteins in IM-9 human lymphocytes is inhibited by Bisindolylmaleimide III (0.1-2.5 μM; 45 min), with IC50 values ranging from 0.23 to 0.32 μM[2]. In human colon adenocarcinoma COLO 205 cells, Bisindolylmaleimide III hydrochloride (20 μM; 6-24 h) does not sensitize the cells to TNF-α-dependent apoptosis, as evidenced by procaspase-3 levels staying unchanged and just a mild drop in cell viability within 24 hours[3]. In human colon adenocarcinoma COLO 205 cells, the TNF-α-dependent apoptosis-sensitizing activity of Bisindolylmaleimide IX is not affected by Bisindolylmaleimide III hydrochloride (20 μM; 21 h)[3].
Cell Viability Assay[3]
| Cell Line | human colon adenocarcinoma COLO 205 cells |
|---|---|
| Concentration | 20 μM (co-treated with 10 ng/mL TNF-α) |
| Incubation Time | 6 h, 12 h, 24 h |
| Result | Moderately reduced cell viability over 24 hours, with significant decreases observed at 6, 12, and 24 h compared to controls. Showed no reduction in procaspase-3 protein levels after co-treatment at 6, 12, or 24 h. |
Apoptosis Analysis[3]
| Cell Line | human colon adenocarcinoma COLO 205 cells |
|---|---|
| Concentration | 20 μM (pre-incubation; followed by co-treatment with 5 μM Bisindolylmaleimide IX and 10 ng/mL TNF-α) |
| Incubation Time | 60 min (pre-incubation); 20 h (co-treatment) |
| Result | Did not affect the ability of Bisindolylmaleimide IX to sensitize COLO 205 cells to TNF-α-dependent apoptosis. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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