CGP 53353

Names

[ Name ]:
CGP 53353

[Synonym ]:
CGP 53 353
DAPH 2
5,6-Bis[(4-fluorophenyl)amino]-2H-isoindole-1,3-dione DAPH 2
PKCbetaII/EGFR Inhibitor
1H-Isoindole-1,3(2H)-dione, 5,6-bis[(4-fluorophenyl)amino]-
4,5-bis(4-fluoroanilino)phthalimide
5,6-BIS[(4-FLUOROPHENYL)AMINO]-1H-ISOINDOLE-1,3(2H)-DIONE
Pam2CSK4 Biotin

Biological Activity

[Description]:

CGP-53353 (DAPH-7) is an potent PKC inhibitor with IC50s of 0.41 mM and 3.8 mM for PKCβII and PKCβI, respectively. CGP-53353 can inhibit glucose-induced cell proliferation and DNA synthesis in AoSMC and A10 cells. CGP-53353 can be used for researching atherosclerosis of diabetic patients[1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

Research Areas >> Metabolic Disease

Signaling Pathways >> TGF-beta/Smad >> PKC

[Target]

PKCβII:0.41 mM (IC50)

PKCβI:3.8 mM (IC50)

[In Vitro]

CGP-53353 (DAPH-7) (1 μM; 48-96 hours) inhibits glucose-induced cell proliferation in A10 cells[1]. CGP-53353 (1 μM ; 0-48 hours) inhibits the glucose-induced increase and acceleration of DNA synthesis in A10, also blocks the glucose-induced increase of S-phase cell percentage[1]. Cell Proliferation Assay Cell Line: A10 (cell proliferation induced by glucose)[1] Concentration: 1 μM Incubation Time: 48-96 hours Result: Inhibited glucose-induced cell proliferation, although A10 cell proliferation was stimulated by increasing glucose concentrations.

[References]

[1]. Yamamoto M, et al. Acute glucose-induced downregulation of PKC-betaII accelerates cultured VSMC proliferation. Am J Physiol Cell Physiol. 2000;279(3):C587-C595.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₂₀H₁₃F₂N₃O₂

[ Molecular Weight ]:
365.33

[ Exact Mass ]:
365.097595

[ PSA ]:
70.23000

[ LogP ]:
3.89

[ Index of Refraction ]:
1.703

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport