Cat. No.: HY-108254

Bisindolylmaleimide IV

(Synonyms: Arcyriarubin A)

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Based on 1 Customer Validation

Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC₅₀s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC₅₀=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC₅₀ of 0.2 μM.

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

Purity: 99.71%
CAS No.: 119139-23-0
Formula: C₂₀H₁₃N₃O₂
Molecular Weight:327.34

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bisindolylmaleimide IV Chemical Structure

CAS No.: 119139-23-0

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC₅₀s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC₅₀=3.1-11.8μM)^[1]. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC₅₀ of 0.2 μM^[2].

IC₅₀ & Target^[1]^[2]

PKC

0.1-0.55 μM (IC₅₀)

HCMV

0.2 μM (IC₅₀)

All PKC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	4.14 μM Compound: Bisindolyl-maleimide	Cytotoxicity activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 30119011]
A549	IC₅₀	56.61 μM Compound: Ro-316233	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 19447039]
ECa-109 cell line	IC₅₀	15.9 μM Compound: Bisindolyl-maleimide	Cytotoxicity activity against human Eca-109 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity activity against human Eca-109 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 30119011]
ECa-109 cell line	IC₅₀	83.55 μM Compound: Ro-316233	Antiproliferative activity against human ECA109 cells after 48 hrs by MTT assay Antiproliferative activity against human ECA109 cells after 48 hrs by MTT assay	[PMID: 19447039]
HL-60	CC₅₀	>8 μM Compound: 82	Cytotoxicity against human HL-60 cells Cytotoxicity against human HL-60 cells	[PMID: 33539089]
Jurkat	IC₅₀	6.3 μg/mL Compound: 4	Cytotoxicity against Jurkat cells Cytotoxicity against Jurkat cells	[PMID: 15911254]
K562	IC₅₀	17.46 μM Compound: Ro-316233	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 19447039]
KB	IC₅₀	53.78 μM Compound: Ro-316233	Antiproliferative activity against human KB cells after 48 hrs by MTT assay Antiproliferative activity against human KB cells after 48 hrs by MTT assay	[PMID: 19447039]
KB 3-1	IC₅₀	>25 μg/mL Compound: 4	Cytotoxicity against KB/VJ300 cells Cytotoxicity against KB/VJ300 cells	[PMID: 15911254]
MCF7	CC₅₀	>8 μM Compound: 82	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 33539089]
PC-3	IC₅₀	10.3 μM Compound: Bisindolyl-maleimide	Cytotoxicity activity against human PC-3 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity activity against human PC-3 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 30119011]
SMMC-7721	IC₅₀	>100 μM Compound: Ro-316233	Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 19447039]
SMMC-7721	IC₅₀	13.2 μM Compound: Bisindolyl-maleimide	Cytotoxicity activity against human SMMC-7721 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity activity against human SMMC-7721 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 30119011]

In Vitro

Bisindolylmaleimide IV (Arcyriarubin A) inhibits PKC with an IC₅₀ of 0.1 μM in 1 % DMSO, while the IC₅₀ of 0.55 μM in 10 % DMSO^[1].

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

Chemical Information

CAS No. 119139-23-0
Appearance Solid
Molecular Weight 327.34
Formula C₂₀H₁₃N₃O₂
Color Orange to red
SMILES

O=C(C(C1=CNC2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O
Synonyms

Arcyriarubin A
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (381.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0549 mL

15.2746 mL

30.5493 mL

5 mM

0.6110 mL

3.0549 mL

6.1099 mL

10 mM

0.3055 mL

1.5275 mL

3.0549 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.08 mg/mL (6.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Davis PD, et al. Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84. [Content Brief]

[2]. Slater MJ, et al. Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication. Bioorg Med Chem. 1999 Jun;7(6):1067-74. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0549 mL	15.2746 mL	30.5493 mL	76.3732 mL
	5 mM	0.6110 mL	3.0549 mL	6.1099 mL	15.2746 mL
	10 mM	0.3055 mL	1.5275 mL	3.0549 mL	7.6373 mL
	15 mM	0.2037 mL	1.0183 mL	2.0366 mL	5.0915 mL
	20 mM	0.1527 mL	0.7637 mL	1.5275 mL	3.8187 mL
	25 mM	0.1222 mL	0.6110 mL	1.2220 mL	3.0549 mL
	30 mM	0.1018 mL	0.5092 mL	1.0183 mL	2.5458 mL
	40 mM	0.0764 mL	0.3819 mL	0.7637 mL	1.9093 mL
	50 mM	0.0611 mL	0.3055 mL	0.6110 mL	1.5275 mL
	60 mM	0.0509 mL	0.2546 mL	0.5092 mL	1.2729 mL
	80 mM	0.0382 mL	0.1909 mL	0.3819 mL	0.9547 mL
	100 mM	0.0305 mL	0.1527 mL	0.3055 mL	0.7637 mL

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Bisindolylmaleimide IV

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Antiviral Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

All PKC Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bisindolylmaleimide IV

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Antiviral Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

All PKC Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bisindolylmaleimide IV Related Classifications

HY-108254 Related Classifications