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MW 438.5 Da, Purity >97%. Potent, selective ATP-competitive PKC inhibitor (IC50 values are 0.01, 0.75 and 2 μM for PKC, phosphorylase kinase and PKA respectively). Potent noncompetitive nAChR antagonist (IC50 = 0.03 μM, catecholamine secretion in nicotine-stimulated PC-12 cells). Shows more potent antinicotinic effects than Bisindolylmaleimide IV (ab144208) and V (ab144205). Induces apoptosis and shows antiproliferative effects.

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Images

Chemical Structure - Bisindolylmaleimide II, PKC inhibitor (AB144206), expandable thumbnail

Key facts

CAS number
137592-45-1
Purity
> 97%
Molecular weight
438.5 Da
Molecular formula
C27H26N4O2
PubChem identifier
2397
Nature
Synthetic

Alternative names

Recommended products

MW 438.5 Da, Purity >97%. Potent, selective ATP-competitive PKC inhibitor (IC50 values are 0.01, 0.75 and 2 μM for PKC, phosphorylase kinase and PKA respectively). Potent noncompetitive nAChR antagonist (IC50 = 0.03 μM, catecholamine secretion in nicotine-stimulated PC-12 cells). Shows more potent antinicotinic effects than Bisindolylmaleimide IV (ab144208) and V (ab144205). Induces apoptosis and shows antiproliferative effects.

Key facts

Purity
> 97%
PubChem identifier
2397
Solubility

Soluble in DMSO to 100 mM.

Biochemical name
Bisindolylmaleimide II
Biological description

Potent, selective ATP-competitive PKC inhibitor (IC50 values are 0.01, 0.75 and 2 μM for PKC, phosphorylase kinase and PKA respectively). Potent noncompetitive nAChR antagonist (IC50 = 0.03 μM, catecholamine secretion in nicotine-stimulated PC-12 cells). Shows more potent antinicotinic effects than Bisindolylmaleimide IV (ab144208) and V (ab144205). Induces apoptosis and shows antiproliferative effects.

Canonical SMILES
CN1CCCC1CCN2C=C(C3=CC=CC=C32)C4=C(C(=O)NC4=O)C5=CNC6=CC=CC=C65
InChI
InChI=1S/C27H26N4O2/c1-30-13-6-7-17(30)12-14-31-16-21(19-9-3-5-11-23(19)31)25-24(26(32)29-27(25)33)20-15-28-22-10-4-2-8-18(20)22/h2-5,8-11,15-17,28H,6-7,12-14H2,1H3,(H,29,32,33)
InChIKey
LBFDERUQORUFIN-UHFFFAOYSA-N
IUPAC name
3-(1H-indol-3-yl)-4-[1-[2-(1-methylpyrrolidin-2-yl)ethyl]indol-3-yl]pyrrole-2,5-dione

Storage

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 info

This supplementary information is collated from multiple sources and compiled automatically.
Activity summary

CaMKII delta also known as CaMKIIδ or CaMK2D is a member of the CaMKII family of proteins recognized for its role as a serine/threonine protein kinase. This protein has a molecular mass of approximately 55 kDa. It is highly expressed in the brain and the heart where it plays essential roles in cellular functions. The domain structure of CaMKII delta allows for calcium/calmodulin activation which is important for its activity in phosphorylating substrates. This protein can bind to other intracellular molecules and is sensitive to regulation by its surrounding environment.

Biological function summary

CaMKII delta participates in several critical processes such as calcium signaling and regulation of gene expression. This protein influences synaptic plasticity muscle contraction and cell cycle control. It forms part of larger complexes interacting with other proteins and playing a role in adjusting cellular responses to various stimuli. It is also subject to inhibition with the compound Bisindolylmaleimide II known to influence its activity. Understanding the biological roles of CaMKII delta allows for insights into its effects on cellular mechanisms especially in neuronal and muscular tissues.

Pathways

CaMKII delta is significant in pathways like the calcium signaling pathway and the PI3K/Akt pathway. It serves as a modulator allowing the integration of various signals which is necessary for maintaining cellular homeostasis. CaMKII delta interacts with proteins such as protein kinase C (PKC) inhibitors affecting cellular signaling outputs. Its role in these pathways highlights the importance of CaMKII delta in regulating processes critical to cell survival growth and adaptation.

Associated diseases and disorders

CaMKII delta is associated with conditions such as cardiac hypertrophy and Alzheimer's disease. These diseases often involve dysregulation of calcium signaling where CaMKII delta plays a part. CaMKII delta's association with proteins like PKC and their dysregulation contributes to the pathogenesis observed in these conditions. Understanding these interactions can aid in developing therapeutic strategies focused on modulating CaMKII delta activity to mitigate disease progression.

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1 product image

  • Chemical Structure - Bisindolylmaleimide II, PKC inhibitor (ab144206), expandable thumbnail

    Chemical Structure - Bisindolylmaleimide II, PKC inhibitor (ab144206)

    2D chemical structure image of ab144206, Bisindolylmaleimide II, PKC inhibitor

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Product protocols

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