IWP-3 Struktur

IWP-3

Bezeichnung:IWP-3

CAS-Nr687561-60-0

Englisch Name:IWP-3

CBNumberCB82714671

SummenformelC22H17FN4O2S3

Molgewicht484.59

MOL-Datei687561-60-0.mol

IWP-3 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>248°C (dec.)
storage temp.	2-8°C
Löslichkeit	DMSO: soluble2mg/mL (clear solution, warmed)
Aggregatzustand	powder
Farbe	white to beige

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
WGK Germany	3

Gefahreninformationscode (GHS)

IWP-3 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
IWP-3 is a potent inhibitor for porcupine which is known to catalyze the palmitoylation of Wnt proteins which are crucial in tumorigenesis.
Biologische Aktivität
iwp-3 is an inhibitor of wnt production.wnt signaling proteins, a group of small secreted proteins, are active in tissue homeostasis, embryonic development, as well as tumorigenesis. wnt proteins can bind to the cell surface receptors, initiating a signaling cascade that results in the β-catenin activation of gene transcription.
Biochem/physiol Actions
IWP-3 is a Wnt inhibitor that prevents palmitylation of Wnt proteins by Porcupine (Porcn). IWP-3 is an inactivator of Porcn function that acts as inhibitors of Wnt production. Studies revealed that IWP-3 induces differentiation of human mesoderm cells to form cardiomyocytes.
in vitro
in previous study, iwp-3 was identified as an inhibitor of wnt production that could regulate in vitro wnt pathway activity with an ic50 value of 40 nm. in addition, iwp-3 was found to be able to inactivate porcupine, a o-acyltransferase for palmitoylating wnt proteins that was critical for the signaling ability and secretion. moreover, iwp-3 at 5 μm was found to block wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 and the scaffold protein dishevelled, resulting in preventing the accumulation of β-catenin [1]. in another study, iwp-3 was applied to promote cardiomyocyte generation from human embryonic stem cells by inhibiting wnt signaling [2].
IC 50
40 nm
Einzelnachweise
[1] b. chen, m. e. dodge, w. tang, et al. small molecule-mediated disruption of wnt-dependent signaling in tissue regeneration and cancer. nature chemical biology 5(2), 100-107 (2009).
[2] e. willems, s. spiering, h. davidovics, et al. small molecule inhibitors of the wnt pathway potently promote cardiomyocytes from human embryonic stem cell derived mesoderm. circulation research 109(4), 360-364 (2011).

IWP-3 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Send Inquriy