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AB144206

Bisindolylmaleimide II, PKC inhibitor

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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.
1 Images
Chemical Structure - Bisindolylmaleimide II, PKC inhibitor (AB144206)
  • Chemical Structure

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Chemical Structure - Bisindolylmaleimide II, PKC inhibitor (AB144206)

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

Key facts

CAS number

137592-45-1

Purity

>97%

Molecular weight

438.5 Da

Molecular formula

C<sub>2</sub><sub>7</sub>H<sub>2</sub><sub>6</sub>N<sub>4</sub>O<sub>2</sub>

PubChem

2397

Nature

Synthetic

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

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.

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.

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.

Product protocols

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