Art. -Nr.: HY-13867A

Bisindolylmaleimide I hydrochloride

Name: Bisindolylmaleimide I hydrochloride
Brand: MedChemExpress
SKU: HY-13867A
Price: 35.00 USD
Availability: InStock
Rating: 5 (44 reviews)

(Synonyms: GF109203X hydrochloride; Go 6850 hydrochloride)

44 Cited Publications

Kundenbewertung

Based on 44 publication(s) in Google Scholar

Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC₅₀ of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor.

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Reinheit: 98.44%
CAS. Nr.: 176504-36-2
Formel: C₂₅H₂₅ClN₄O₂
Molecular Weight:448.94

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bisindolylmaleimide I hydrochloride Chemical Structure

CAS. Nr.: 176504-36-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (44)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Bovine brain PKC

10 nM (IC₅₀)

PKC-βII

16 nM (IC₅₀)

PKC-βI

17 nM (IC₅₀)

PKCα

20 nM (IC₅₀)

PKCγ

20 nM (IC₅₀)

FDGFG

65 μM (IC₅₀)

Alle PKC Isoform-spezifische Produkte anzeigen :

Alle GSK-3 Isoform-spezifische Produkte anzeigen :

In Vitro

Bisindolylmaleimide I hydrochloride (5 μM) inhibits α-thrombin-induced P47 phosphorylation^[1].
Bisindolylmaleimide I hydrochloride (0-1 μM) inhibits DNA synthesis in quiescent swiss 3T3 cells^[1].
Bisindolylmaleimide I hydrochloride (5 μM) reduces GSK-3 activity to 25.1±4.3% in adipocytes lysates^[3].
Bisindolylmaleimide I hydrochloride (10 μM, 24 h) inhibits exosome and microvesicle (EMV) release from PC3 cells^[4].
Bisindolylmaleimide I hydrochloride (10 μM, 24 h) enhances cytotoxicity of 5-fluorouracil (HY-90006)^[4].

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

In Vivo

Bisindolylmaleimide I hydrochloride (0.02 mg/kg, i.p.) reduced the inceased NLRP3, P-PKCɑ, and PKCɑ levels in mechanical ventilation (MV) group^[5].
Bisindolylmaleimide I hydrochloride (0-20 mg/kg, i.p.) reduces the mean frequency of Quinpirole-induced vomiting in shrews^[6].

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

Animal Model:

Quinpirole-treated shrews^[2]
Dosage:

0-20 mg/kg
Administration:

i.p.
Result:

Reduced the mean frequency of Quinpirole-induced vomiting.
Blocked Quinpirole-mediated ERK1/2 phosphorylation in shrew brainstems.

Chemical Information

CAS. Nr. 176504-36-2
Appearance Solid
Molecular Weight 448.94
Formel C₂₅H₂₅ClN₄O₂
Color Orange to red
SMILES

[H]Cl.O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O
Synonyms

GF109203X hydrochloride; Go 6850 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (44)

All WBFlow CytometryCell Proliferation/Viability AssayELISACell Imaging/Staining

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Journal Impact Factor

Bioact Mater

Food-derived β-lactoglobulin nanofibrils: An efficacy, safe, and scalable solution to overcome oral insulin delivery challenges. [Abstract]

2025 Nov 25:57:646-659. PMID: 41377894
J Adv Res

Paeonol protects against doxorubicin-induced cardiotoxicity by promoting Mfn2-mediated mitochondrial fusion through activating the PKCε-Stat3 pathway. [Abstract]

2023 May:47:151-162. PMID: 35842187
Redox Biol

BNP protects against diabetic cardiomyopathy by promoting Opa1-mediated mitochondrial fusion via activating the PKG-STAT3 pathway. [Abstract]

2023 Jun:62:102702. PMID: 37116257
Redox Biol

Paeonol promotes Opa1-mediated mitochondrial fusion via activating the CK2α-Stat3 pathway in diabetic cardiomyopathy. [Abstract]

2021 Oct;46:102098. PMID: 34418601
Theranostics

A novel small-molecule PROTAC selectively promotes tau clearance to improve cognitive functions in Alzheimer-like models. [Abstract]

2021 Mar 11;11(11):5279-5295. PMID: 33859747

Bisindolylmaleimide I hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 11;11(11):5279-5295. [Abstract]

SH-SY5Y cells were simultaneously treated with C004019 (1 or 10 µM) and wortmainnin (WO, 1 µM) and Bisindolylmaleimide I (GF-109203X) (GFX, 1 µM) for 24 h to induce tau hyperphosphorylation, and then tau was measured by Western blotting.
Neural Regen Res

NOX4 exacerbates Parkinson's disease pathology by promoting neuronal ferroptosis and neuroinflammation. [Abstract]

2025 Jul 1;20(7):2038-2052. PMID: 38993139

Bisindolylmaleimide I hydrochloride purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2025 Jul 1;20(7):2038-2052. [Abstract]

Cell viability was measured by cell counting kit-8 in MN9D cells with/without MPP⁺ 0.5 mM and Bisindolylmaleimide I (BIM) 5 µM treatment for 24 hours.

Bisindolylmaleimide I hydrochloride purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2025 Jul 1;20(7):2038-2052. [Abstract]

C11-BODIPY fluorescence analysis suggested that MPP⁺ increased intracellular lipid peroxidation in MN9D cells, and that this effect was reversed by Bisindolylmaleimide I (BIM) (5 μM) treatment.
Free Radic Biol Med

HIF-1α translation mediated by PKCδ facilitates RSV-induced production of innate inflammatory cytokines in vitro and in vivo. [Abstract]

2026 Mar 16:246:614-626. PMID: 41611036
Chin J Nat Med

A 75 kDa glycoprotein isolated from Cudrania tricuspidata Bureau induces colonic epithelial proliferation and ameliorates mouse colitis induced by dextran sulfate sodium. [Abstract]

2021 Jan;19(1):46-55. PMID: 33516451
Chin J Nat Med

Phytoglycoprotein isolated from Dioscorea batatas Decne promotes intestinal epithelial wound healing. [Abstract]

2020 Oct;18(10):738-748. PMID: 33039053
J Ethnopharmacol

Dendrobium nobile Lindl. alkaloid decreases Tau hyperphosphorylation via regulating PI3K/Akt/GSK-3β pathway in vitro and in vivo. [Abstract]

2024 Mar 25:322:117592. PMID: 38097026
CNS Neurosci Ther

Vitamin D3 Attenuates Neuropathic Pain via Suppression of Mitochondria-Associated Ferroptosis by Inhibiting PKCα/NOX4 Signaling Pathway. [Abstract]

2024 Sep;30(9):e70067. PMID: 39328008
Ecotoxicol Environ Saf

Perfluorooctanoic acid alters the developmental trajectory of female germ cells and embryos in rodents and its potential mechanism. [Abstract]

2022 May 1;236:113467. PMID: 35390687
Cell Mol Life Sci

Proximal tubular FHL2, a novel downstream target of hypoxia inducible factor 1, is a protector against ischemic acute kidney injury. [Abstract]

2024 May 30;81(1):244. PMID: 38814462
Cells

Nanospheres Loaded with Curcumin Improve the Bioactivity of Umbilical Cord Blood-Mesenchymal Stem Cells via c-Src Activation During the Skin Wound Healing Process. [Abstract]

2020 Jun 15;9(6):1467. PMID: 32549381
Cells

Nanosphere Loaded with Curcumin Inhibits the Gastrointestinal Cell Death Signaling Pathway Induced by the Foodborne Pathogen Vibrio vulnificus. [Abstract]

2020 Mar 5;9(3):631. PMID: 32151068
Front Endocrinol

A Type IIb, but Not Type IIa, GnRH Receptor Mediates GnRH-Induced Release of Growth Hormone in the Ricefield Eel. [Abstract]

2018 Nov 30:9:721. PMID: 30555419
Biomolecules

PAR2 Participates in the Development of Cough Hypersensitivity in Guinea Pigs by Regulating TRPA1 Through PKC. [Abstract]

2025 Feb 1;15(2):208. PMID: 40001511
Mucosal Immunol

Bilirubin represents a negative regulator of ILC2 in allergic airway inflammation. [Abstract]

2022 Feb;15(2):314-326. PMID: 34686839

Bisindolylmaleimide I hydrochloride purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2022 Feb;15(2):314-326. [Abstract]

Lung ILC2s were treated with vehicle or UCB (50 μM) and /or Honokiol (5 μM) and /or Bisindolylmaleimide I (BIM1) (5 μM) in the presence of IL-2, IL-7 and IL-33 for 48 h. Flow cytometric analysis of p-ERK1/2 levels was performed.

Bisindolylmaleimide I hydrochloride purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2022 Feb;15(2):314-326. [Abstract]

The amounts of IL-5 and IL-13 in the supernatants were measured by ELISA.
J Nutr Biochem

Nanospheres loaded with curcumin promote gut epithelial motility through F-actin-related migration signaling events. [Abstract]

2021 Feb:88:108555. PMID: 33249186
Biosci Rep

Parathyroid hormone-related protein induces fibronectin up-regulation in rat mesangial cells through reactive oxygen species/Src/EGFR signaling. [Abstract]

2019 Apr 26;39(4):BSR20182293. PMID: 30926678
Front Mol Neurosci

The chronification mechanism of orofacial inflammatory pain: Facilitation by GPER1 and microglia in the rostral ventral medulla. [Abstract]

2023 Jan 6:15:1078309. PMID: 36683848
Pain Rep

Monoclonal antibody inhibition of PAR2 reduces phenotype severity and pain in murine inflammatory bowel disease. [Abstract]

2026 Apr 20;11(3):e1446. PMID: 42021789
Am J Physiol Endocrinol Metab

Hyperglycemia impairs EAAT2 glutamate transporter trafficking and glutamate clearance in islets of Langerhans: implications for type 2 diabetes pathogenesis. [Abstract]

2024 Jul 1;327(1):E27-E41. PMID: 38690938
Neurobiol Stress

Glucocorticoids modulate neural activity via a rapid non-genomic effect on Kv2.2 channels in the central nervous system. [Abstract]

2023 Nov 25:28:100593. PMID: 38075025
Microbiol Spectr

Protein Kinase C Inhibitors Reduce SARS-CoV-2 Replication in Cultured Cells. [Abstract]

2022 Oct 26;10(5):e0105622. PMID: 36000889
Viruses

Inducible miR-150 Inhibits Porcine Reproductive and Respiratory Syndrome Virus Replication by Targeting Viral Genome and Suppressor of Cytokine Signaling 1. [Abstract]

2022 Jul 7;14(7):1485. PMID: 35891465
Pulm Pharmacol Ther

The promoting role of Cx43 on the proliferation and migration of arterial smooth muscle cells for angiotensin II-dependent hypertension. [Abstract]

2021 Oct:70:102072. PMID: 34428599
Peptides

Neuropeptide Y promotes hepatic apolipoprotein A1 synthesis and secretion through neuropeptide Y Y5 receptor. [Abstract]

2022 Aug:154:170824. PMID: 35660638
Cell Biol Int

Gö6983 attenuates breast cancer-induced osteolysis by the apoptotic pathway. [Abstract]

2020 Mar;44(3):838-847. PMID: 31814221
J Leukoc Biol

Transient receptor potential vanilloid 4 (TRPV4) in neutrophils enhances myocardial ischemia/reperfusion injury. [Abstract]

2023 Sep 1;114(3):266-279. PMID: 37232941
Int J Food Sci Tech

2024 Jul 18.
Psychopharmacology (Berl)

The effects of serotonergic psychedelics in synaptic and intrinsic properties of neurons in layer II/III of the orbitofrontal cortex. [Abstract]

2023 Jun;240(6):1275-1285. PMID: 37071130
Food Chem Toxicol

G-Rh4 improves pancreatic β-cells dysfunction in vivo and in vitro by increased expression of Nrf2 and its target genes. [Abstract]

2021 Feb:148:111925. PMID: 33359794
Food Chem Toxicol

Intestinal epithelial cell apoptosis due to a hemolytic toxin from Vibrio vulnificus and protection by a 36 kDa glycoprotein from Rhus verniciflua Stokes. [Abstract]

2019 Mar:125:46-54. PMID: 30592968
Mechanobiol Med

Piezo1 activates nitric oxide synthase in red blood cells via protein kinase C with increased activity in diabetes. [Abstract]

2025 Jul 28;3(3):100145. PMID: 40809083
PeerJ

Androgen promotes oocyte development by upregulating gap junction intercellular communication activity in granulosa cells in mice. [Abstract]

2026 Apr 30:14:e21194. PMID: 42083638
Vet Microbiol

Highly pathogenic porcine reproductive and respiratory syndrome virus (HP-PRRSV) induces IL-6 production through TAK-1/JNK/AP-1 and TAK-1/NF-κB signaling pathways. [Abstract]

2021 May:256:109061. PMID: 33836390
Med Sci Monit

Salicylate Induced GABAAR Internalization by Dopamine D1-Like Receptors Involving Protein Kinase C (PKC) in Spiral Ganglion Neurons. [Abstract]

2021 Oct 18;27:e933278. PMID: 34657931
Harvard University

2026.
Res Sq

2026 May 6.
bioRxiv

2026 Feb 10.
SSRN

2024 Jan 22.
Research Square Preprint

2021 Aug.
Elife

Dynamic Na+/H+ exchanger 1 (NHE1) - calmodulin complexes of varying stoichiometry and structure regulate Ca2+-dependent NHE1 activation. [Abstract]

2021 Mar 3:10:e60889. PMID: 33655882

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (139.22 mM; ultrasonic and warming and heat to 60°C; 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

2.2275 mL

11.1373 mL

22.2747 mL

5 mM

0.4455 mL

2.2275 mL

4.4549 mL

10 mM

0.2227 mL

1.1137 mL

2.2275 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.63 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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)

Verweise

[1]. Toullec D, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81. [Content Brief]

[2]. Vetri F, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54. [Content Brief]

[3]. Hers I, et al. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6. [Content Brief]

[4]. Kosgodage US, et al. Chloramidine/Bisindolylmaleimide-I-Mediated Inhibition of Exosome and Microvesicle Release and Enhanced Efficacy of Cancer Chemotherapy. Int J Mol Sci. 2017 May 9;18(5):1007. [Content Brief]

[5]. Liu M, et al. Aerobic exercise alleviates ventilator-induced lung injury by inhibiting NLRP3 inflammasome activation. BMC Anesthesiol. 2022 Dec 1;22(1):369. [Content Brief]

[6]. Belkacemi L, et al. Signal transduction pathways involved in dopamine D2 receptor-evoked emesis in the least shrew (Cryptotis parva). Auton Neurosci. 2021 Jul;233:102807. [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	2.2275 mL	11.1373 mL	22.2747 mL	55.6867 mL
	5 mM	0.4455 mL	2.2275 mL	4.4549 mL	11.1373 mL
	10 mM	0.2227 mL	1.1137 mL	2.2275 mL	5.5687 mL
	15 mM	0.1485 mL	0.7425 mL	1.4850 mL	3.7124 mL
	20 mM	0.1114 mL	0.5569 mL	1.1137 mL	2.7843 mL
	25 mM	0.0891 mL	0.4455 mL	0.8910 mL	2.2275 mL
	30 mM	0.0742 mL	0.3712 mL	0.7425 mL	1.8562 mL
	40 mM	0.0557 mL	0.2784 mL	0.5569 mL	1.3922 mL
	50 mM	0.0445 mL	0.2227 mL	0.4455 mL	1.1137 mL
	60 mM	0.0371 mL	0.1856 mL	0.3712 mL	0.9281 mL
	80 mM	0.0278 mL	0.1392 mL	0.2784 mL	0.6961 mL
	100 mM	0.0223 mL	0.1114 mL	0.2227 mL	0.5569 mL

Bioz

Keywords

Bisindolylmaleimide I hydrochloride

44 Cited Publications

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