Abcam, ab144264, GF 109203X (Bisindolylmaleimide i), PKC inhibitor

Size: 1mg / 5mg
MW 412.5 Da, Purity >98%. Potent, selective PKC inhibitor (IC 50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Potent GSK-3 inhibitor (IC 50 = 360 nM). Potent 5-HT3 antagonist (K i = 29.5 nM). Shows anti-inflammatory effects in vivo. .
Key facts
CAS number:133052-90-1,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:412.5 Da,
Molecular formula:C25H24N4O2,
PubChem:2396,
Nature:Synthetic,
Solubility:Soluble in DMSO to 25 mM,
Biochemical name:Bisindolylmaleimide i,
Biological description:Potent, selective PKC inhibitor (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Potent GSK-3 inhibitor (IC50 = 360 nM). Potent 5-HT3 antagonist (Ki = 29.5 nM). Shows anti-inflammatory effects in vivo.,
Canonical smiles:CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54,
InChi:InChI=1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31),
InChiKey:QMGUOJYZJKLOLH-UHFFFAOYSA-N,
IUPAC Name:3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(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.
Protein Kinase C (PKC) is a family of protein kinases including isoforms such as PKC delta PKC epsilon PKC beta 2 PKC gamma PKC eta and PKC theta (also known as PRKCQ). Cyclin D1 ERK2 (Extracellular Signal-Regulated Kinase 2) GSK3 beta (Glycogen Synthase Kinase 3 beta) Cdk4 (Cyclin-Dependent Kinase 4) and PIM1 are part of this elaborate network. The mass of each protein varies for example PKC epsilon has a mass of approximately 83 kDa. These proteins express widely in different tissues but notably PRKCQ shows significant expression in T-cells while H-ERG (human Ether-à-go-go-Related Gene) primarily functions in cardiac tissues.
Biological function summary
Many of these proteins regulate important cellular processes like cell cycle progression and signal transduction. Cyclin D1 acts as a regulator in the cell cycle forming a complex with Cdk4 or Cdk6 that drives transition from G1 phase to S phase. GSK3 beta is important in insulin and Wnt signaling pathways often affecting glycogen synthesis and gene transcription. PKC epsilon and PIM1 signal in cardiac and immune cells modulating cellular responses to external stimuli. H-ERG a potassium ion channel plays a substantial role in cardiac repolarization.
Pathways
PKC family members such as PKC delta and epsilon engage significantly in the NF-kB signaling pathway impacting transcriptional regulation of inflammatory cytokines. ERK2 participates in the MAPK/ERK pathway which influences cellular processes like growth differentiation and survival. Cyclin D1 and Cdk4 are essential for the transition from G1 to the S phase in the cell cycle pathway. GSK3 beta intersects with the Wnt signaling pathway altering gene expression and cellular fate. These proteins often interact with one another such as PKC isoforms which frequently modulate MAPK pathway signaling dynamics.
PKC delta and theta relate closely to autoimmune disorders where they modulate T-cell receptor signaling contributing to immune cell activation and response. Cyclin D1 and Cdk4 have links to several cancers notably breast cancer where their dysregulation causes unchecked cellular proliferation. H-ERG is critical in disorders like long QT syndrome which affects cardiac ion channels leading to arrhythmias. GSK3 beta dysregulation is implicated in neurodegenerative diseases such as Alzheimer's disease interacting with proteins like tau exacerbating pathological conditions.