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HomeProduct name listBISINDOLYLMALEIMIDE I HYDROCHLORIDE

BISINDOLYLMALEIMIDE I HYDROCHLORIDE

Synonym(s):2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide, HCl;Bisindolylmaleimide I, Hydrochloride - CAS 176504-36-2 - Calbiochem

BISINDOLYLMALEIMIDE I HYDROCHLORIDE Structural

What is BISINDOLYLMALEIMIDE I HYDROCHLORIDE?

Description

Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine . It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM). It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.

The Uses of BISINDOLYLMALEIMIDE I HYDROCHLORIDE

GF 109203X hydrochloride has been used to inhibit protein kinase C in human neuroblastoma-derived kelly cells.

What are the applications of Application

Bisindolylmaleimide I, HCl is a water soluble inhibitor for all known isoforms of PKC

General Description

GF 109203X prevents collagen-triggered adenosine and three phosphate (ATP) secretion. It also inhibits collagen and α-thrombin-induced platelet aggregation. It functions as an inhibitor of glycogen synthase kinase-3 (GSK-3). GF 109203X also functions as an anti-inflammatory agent.

Biochem/physiol Actions

Inhibitor of protein kinase C; potent inhibitor of GSK-3.

Properties of BISINDOLYLMALEIMIDE I HYDROCHLORIDE

storage temp.  2-8°C
solubility  DMF: 10 mg/mL; DMSO: 16 mg/mL; DMSO:PBS(pH 7.2) (1:4): 0.2 mg/mL
form  Orange-red solid
color  Orange to red

Safety information for BISINDOLYLMALEIMIDE I HYDROCHLORIDE

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Computed Descriptors for BISINDOLYLMALEIMIDE I HYDROCHLORIDE

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