Description
Key facts
CAS number:119139-23-0,
Purity:>98%,
Molecular weight:327.3 Da,
Molecular formula:C20H13N3O2,
PubChem:2399,
Nature:Synthetic,
Solubility:Soluble in ethanol to 50 mMSoluble in DMSO to 50 mM,
Biochemical name:Bisindolylmaleimide IV,
Biological description:Potent cell-permeable PKC inhibitor (IC50 values are 0.1 - 0.55 μM). Inhibits PKA (IC50 values are 2 - 11.8 μM). Noncompetitive nAChR antagonist. Shows less potent antinicotinic effects than Bisindolylmaleimide II (ab144206). Induces apoptosis and shows antiproliferative effects.,
Canonical smiles:C1=CC=C2C(=C1)C(=CN2)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54,
InChi:InChI=1S/C20H13N3O2/c24-19-17(13-9-21-15-7-3-1-5-11(13)15)18(20(25)23-19)14-10-22-16-8-4-2-6-12(14)16/h1-10,21-22H,(H,23,24,25),
InChiKey:DQYBRTASHMYDJG-UHFFFAOYSA-N,
IUPAC Name:3,4-bis(1H-indol-3-yl)pyrrole-2,5-dione
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
The protein kinase C (PKC) family includes isoforms such as PKC delta PKC mu/PKD PKC epsilon PKC beta 2 PKC gamma PKC zeta PKC eta PKC theta/PRKCQ PKC iota PKC nu/PRKD3 and CaMKII delta. These isoforms play roles in signal transduction and involve phosphorylation. Each isoform has a distinct mass; for example PKC delta weighs around 77 kDa. PKC isoforms express in various tissues like the brain immune cells and muscle. Some PKCs have specific tissues where they are mostly active which helps in their functional specificity.
Biological function summary
PKCs function as enzymes that regulate cell activities including proliferation differentiation and apoptosis. These activities occur through their second messenger-dependent activation. PKC isoforms often exist as part of larger protein complexes that determine substrate specificity and cellular localization. For instance PKC iota associates within a complex that facilitates its activity in the cytoplasm. The bisindolylmaleimide compounds act as inhibitors to PKC functions by blocking their phosphorylation activity.
Pathways
Multiple signaling cascades incorporate PKC isoforms. Among them the MAPK/ERK and PI3K/AKT pathways engage PKCs extensively. In the MAPK/ERK pathway PKCs phosphorylate components that activate ERK impacting cell cycle regulation. Additionally PKCs relate to proteins such as RAF and MEK within these pathways emphasizing their roles in transmitting extracellular signals to intracellular responses. In the PI3K/AKT pathway PKCs help in mediating cell survival signals contributing to their significance in cellular homeostasis.
PKC isoforms have associations with cancer and type II diabetes. For instance aberrant PKC epsilon activity links to cancer progression due to its role in controlling cell proliferation. Moreover altered PKC beta 2 activity impacts insulin signaling pathways contributing to insulin resistance observed in diabetes. These proteins when dysregulated serve as therapeutic targets and inhibitors like bisindolylmaleimide facilitate the exploration of therapeutic interventions for such conditions.
