565740

α-Amyloid Precursor Protein Modulator

≥95% (HPLC), solid, PKC activator, Calbiochem^®

• Synonym(s): α-Amyloid Precursor Protein Modulator, (2S,5S)-(E,E)-8-(5-(4-(Trifluoromethyl)phenyl)-2,4-pentadienoylamino)benzolactam, PKC Activator V
• Empirical Formula (Hill Notation): C₂₇H₃₀F₃N₃O₃
• CAS Number: 497259-23-1
• Molecular Weight: 501.54
• MDL number: MFCD09037558
• UNSPSC Code: 12352202
• NACRES: NA.77

Properties

• Product Name: α-Amyloid Precursor Protein Modulator, A cell-permeable benzolactam derived PKC activator (K_i = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblast AG06848.
• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange
• solubility: methanol: 1 mg/mL; DMSO: 50 mg/mL
• shipped in: wet ice
• storage temp.: −20°C
• SMILES string: FC(F)(F)c1ccc(cc1)\C=C\C=C\C(=O)Nc2cc3c(cc2)N([C@H](C(=O)N[C@@H](C3)CO)C(C)C)C
• InChI: 1S/C27H30F3N3O3/c1-17(2)25-26(36)32-22(16-34)15-19-14-21(12-13-23(19)33(25)3)31-24(35)7-5-4-6-18-8-10-20(11-9-18)27(28,29)30/h4-14,17,22,25,34H,15-16H2,1-3H3,(H,31,35)(H,32,36)/b6-4+,7-5+/t22-,25-/m0/s1
• InChI key: WOLVEMPZUIFSII-IHHOKICGSA-N

Description

General description

A cell-permeable PKC activator (K_i = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) but lacks any tumor promoting activity.

A cell-permeable benzolactam derived PKC activator (K_i = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblast AG06848. Displays a marked loss of tumor promoting activity.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PKC

Product does not compete with ATP.

Reversible: no

Target K_i: 11.9 nM for activating PKCα

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Kozikowski, A.P., et al. 2003. J. Med. Chem.46, 364.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable