IWR-1-endo

Bezeichnung:IWR-1-endo

CAS-Nr1127442-82-3

Englisch Name:IWR-1-endo

CBNumberCB82518787

SummenformelC25H19N3O3

Molgewicht409.44

MOL-Datei1127442-82-3.mol

IWR-1-endo physikalisch-chemischer Eigenschaften

alpha	-3.0～+3.0°(20℃/D)(c=0.1,CH3CN)
Siedepunkt	643.9±55.0 °C(Predicted)
Dichte	1.425±0.06 g/cm3(Predicted)
storage temp.	room temp
Löslichkeit	DMSO: soluble5mg/mL, clear
pka	11.88±0.43(Predicted)
Aggregatzustand	Liquid
Farbe	white to beige
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

WGK Germany

Gefahreninformationscode (GHS)

IWR-1-endo Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
IWR-1 endo (1127442-82-3) is a potent inhibitor of Wnt signaling (IC50=180 nM).1?Inhibits zebrafish tailfin regeneration (0.5 mM).2?Acts via inhibition of tankyrase and attenuates Wnt/β-catenin signaling in cancer stem-like cells.3?Promotes self-renewal and maintains pluripotency of human embryonic stem cells.4?Promotes differentiation of pluripotent stem cells into cardiomyocytes.5
Verwenden
IWR-3 act as inhibitors of Wnt response. It appear that IWR compounds induce stabilization of Axin proteins via a direct interaction, which is a part of the b-catenin destruction complex (consists of Apc, Axin, Ck1 and Gsk3b).Such compounds may be used in the treatment of Wnt protein signaling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.
Verwenden
IWR-1-endo act as inhibitors of Wnt response. It appear that IWR compounds induce stabilization of Axin proteins via a direct interaction, which is a part of the b-catenin destruction complex (consists of Apc, Axin, Ck1 and Gsk3b). Such compounds may be used in the treatment of Wnt protein signaling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosi s.
Definition
ChEBI: IWR-1-endo is a dicarboximide having an endo bridged phthalimide structure, substituted at nitrogen by a 4-(quinolin-8-ylcarbamoyl)benzoyl group. It has a role as an axin stabilizer and a Wnt signalling inhibitor. It is a dicarboximide, a bridged compound, a member of quinolines and a member of benzamides.
Allgemeine Beschreibung
A cell-permeable p-imidobenzamidoquinoline, endo-diastereomer that is shown to inhibit the activity of TNKS1/PARP5a and TNKS2/PARP5b in in vitro auto-PARsylation assays (IC₅₀ = 131 and 56 nM, respectively) and effectively suppress Wnt-stimulated transcription activity in L-Wnt-STF-based reporter assays (IC₅₀ = 180 nM), while exhibiting little activity against PARP1 or PARP2 (IC₅₀ >18.75 μM). Although both IWR-1-endo and XAV939 (Tankyrase1/2 Inhibitor; >Cat. No. 575545) act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects both in vitro and in vivo, IWR-1-endo exerts its effect via interaction with Axin, while XAV939 binds TNKS directly.
Biochem/physiol Actions
Cell permeable: yes
Lager
Store at RT
Einzelnachweise
1) Chen?et al. (2009),?Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer; Nature Chem. Biol.,?5?100 2) Lu?et al.?(2009),?Structure-activity Relationship Studies of Small-Molecule Inhibitors of Wnt Response; Bioorg. Med. Chem. Lett.,?19?3825 3) Martins-Neves?et al.?(2018),?IWR-1, a tankyrase inhibitor, attenuates Wnt/?-catenin signaling in cancer stem-like cells and inhibits in vivo the growth of subcutaneous human osteosarcoma xenograft; Cancer Lett.,?414?1 4) Kim?et al.?(2013),?Modulations of ?-catenin function maintains mouse epiblast stem cell and human embryonic stem cell self-renewal; Nat. Commun., 4?4403 5) Ren?et al.?(2011),?Small Molecule Wnt Inhibitors Enhance the Efficiency of BMP-4-directed Cardiac Differentiation of Human Pluripotent Stem Cells; J. Mol. Cell. Cardiol.,?51?280

IWR-1-endo Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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