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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C27H30F3N3O3
CAS Number:
497259-23-1
Molecular Weight:
501.54
MDL number:
MFCD09037558
UNSPSC Code:
12352202
NACRES:
NA.77

Key Documents

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Product Name

α-Amyloid Precursor Protein Modulator, A cell-permeable benzolactam derived PKC activator (Ki = 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.

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

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

Quality Level

100

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PKC
Product does not compete with ATP.
Reversible: no
Target Ki: 11.9 nM for activating PKCα

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable PKC activator (Ki = 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 (Ki = 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.

Other Notes

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

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Yan Fung Wong et al.
Nature cell biology (2023-01-24)
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The HNF1αp291fsinsC truncation is the most common mutation associated with maturity-onset diabetes of the young 3 (MODY3). Although shown to impair HNF1α signaling, the mechanism by which HNF1αp291fsinsC causes MODY3 is not fully understood. Here we use MODY3 patient and
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Cell reports, 33(10), 108455-108455 (2020-12-10)
The ever-increasing therapeutic and pharmaceutical demand for liver cells calls for systems that enable mass production of hepatic cells. Here we describe a large-scale suspension system that uses human endoderm stem cells (hEnSCs) as precursors to generate functional and transplantable

Global Trade Item Number

SKUGTIN
565740-1MGCN04055977267648

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