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CGP 53353

Cat. No. 2442 3 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Selective inhibitor of PKCβII
Chemical Name: 5,6-bis[(4-Fluorophenyl)amino]-1H-isoindole-1,3(2H)-dione
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for CGP 53353

CGP 53353 is a selective inhibitor of PKCβII (IC50 values are 0.41 and 3.8 μM for PKCβII and PKCβI respectively). Also inhibits prionogenic Sup35 fibrillization (IC50 ~ 3.4 μM) and inhibits de novo Aβ42 assembly in vitro.

Compound Libraries for CGP 53353

CGP 53353 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for CGP 53353

M. Wt 365.34
Formula C20H13F2N3O2
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 145915-60-2
PubChem ID 6711154
InChI Key RONQPWQYDRPRGG-UHFFFAOYSA-N
Smiles FC1=CC=C(NC2=CC3=C(C=C2NC2=CC=C(F)C=C2)C(=O)NC3=O)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CGP 53353

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.53 100
ethanol 7.31 20

Preparing Stock Solutions for CGP 53353

The following data is based on the product molecular weight 365.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.74 mL 13.69 mL 27.37 mL
5 mM 0.55 mL 2.74 mL 5.47 mL
10 mM 0.27 mL 1.37 mL 2.74 mL
50 mM 0.05 mL 0.27 mL 0.55 mL

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References for CGP 53353

References are publications that support the biological activity of the product.

Kouroedov et al (2004) Selective inhibition of protein kinase Cβ2 prevents acute effects of high glucose on vascular cell adhesion molecule-1 expression in human endothelial cells. Circulation 110 91 PMID: 15210597

Wang et al (2008) Direct and selective elimination of specific prions and amyloids by 4,5-dianilinophthalimide and analogs. Proc.Natl.Acad.Sci.USA 105 7159

If you know of a relevant reference for CGP 53353, please let us know.

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3 Citations for CGP 53353

Citations are publications that use Tocris products. Selected citations for CGP 53353 include:

Liu et al (2014) PKCβII acts downstream of chemoattractant receptors and mTORC2 to regulate cAMP production and myosin II activity in neutrophils. Mol Biol Cell 25 1446 PMID: 24600048

He et al (2011) Stanniocalcin-1 promotes tumor angiogenesis through up-regulation of VEGF in gastric cancer cells. J Neurosci 18 39 PMID: 21672207

Ramana et al (2007) Aldose reductase-regulated tumor necrosis factor-α production is essential for high glucose-induced vascular smooth muscle cell growth. Endocrinology 148 4371 PMID: 17584970

Do you know of a great paper that uses CGP 53353 from Tocris? Please let us know.

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