BISINDOLYLMALEIMIDE I HYDROCHLORIDE
BISINDOLYLMALEIMIDE I HYDROCHLORIDE Basic information
- Product Name:
- BISINDOLYLMALEIMIDE I HYDROCHLORIDE
- Synonyms:
-
- BIM 1 hydrochloride
- 3-[1-(dimethylaminopropyl)indol-3-yl]-4-(indol-3-yl)maleimide hydrochloride
- BisindolylMaleiMide I( Hydrochloride Salt)
- BisindolylMaleiMide I . hydrochloride [GF-109203K
- 3-[1-[3-(Dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione monohydrochloride
- 3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
- Bisindolylmaleimide I, Hydrochloride - CAS 176504-36-2 - Calbiochem
- GF 109203X hydrochloride >=95%
- CAS:
- 176504-36-2
- MF:
- C25H25ClN4O2
- MW:
- 448.95
- Mol File:
- 176504-36-2.mol
BISINDOLYLMALEIMIDE I HYDROCHLORIDE Chemical Properties
- 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
BISINDOLYLMALEIMIDE I HYDROCHLORIDE Usage And Synthesis
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.
Uses
GF 109203X hydrochloride has been used to inhibit protein kinase C in human neuroblastoma-derived kelly cells.
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.
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