Bisindolylmaleimide I

Bisindolylmaleimide I (GF109203X) 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 is also a GSK-3 inhibitor[1][2][3].

Product Specifications

CAS Number

[133052-90-1]

Product Name Alternative

GF109203X; Go 6850

UNSPSC

12352005

Hazard Statement

H351

Target

GSK-3; PKC

Type

Reference compound

Related Pathways

Epigenetics; PI3K/Akt/mTOR; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Metabolic Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/Bisindolylmaleimide-I.html

Purity

98.15

Solubility

DMSO : 10 mg/mL (ultrasonic)

Smiles

O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O

Molecular Formula

C25H24N4O2

Molecular Weight

412.48

Precautions

H351

References & Citations

[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.|[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.|[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. |[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. |[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. |[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.