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IWR-1

Names

[ CAS No. ]:
1127442-82-3

[ Name ]:
IWR-1

[Synonym ]:
4-[(1R,2S,6R,7S)-3,5-Dioxo-4-azatricyclo[5.2.1.0]dec-8-en-4-yl]-N-(8-quinolinyl)benzamide
4-[(1R,2S,6R,7S)-3,5-Dioxo-4-azatricyclo[5.2.1.0]dec-8-en-4-yl]-N-(quinolin-8-yl)benzamide
Benzamide, 4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinyl-
IWR-1

Biological Activity

[Description]:

IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> Wnt
Research Areas >> Cancer

[Target]

IC50: 180 nM (Wnt)


[In Vitro]

Both IWR-1 and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects in vitro. IWR-1 exerts its effect via interaction with Axin, while XAV939 binds TNKS directly[1]. IWR-1 (10 μM) induces stabilization of β-catenin disruption complex. IWR-1 (10 μM) is added to the medium together with MIF, the size of cell colonies is extremely decreased, and that indicates the promoting effect of MIF on NSPC proliferation is inhibited by IWR-1 in any MIF concentration group. 2, 5 and 10 μM of IWR-1 significantly inhibits the proliferation of NSPC dose-dependently. IWR-1 inhibites the promoting effect of MIF on NSPC differentiation to neuron lineage[2]. IWR-1 treatment in the presence of maximal stimulatory dose of FSH (0.5 ng/mL) results in a dose dependent inhibition of the stimulatory effect of FSH with > 75% inhibition observed at the maximal inhibitory dose of IWR-1 (1 µM). IWR-1 treatment partially reverses the FSH-induced inhibition of granulosa cell CARTPT mRNA expression[3].

[References]

[1]. Lu J, et al. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7.

[2]. Zhang X, et al. Macrophage migration inhibitory factor promotes proliferation and neuronal differentiation of neural stem/precursor cells through Wnt/β-catenin signal pathway. Int J Biol Sci. 2013 Nov 28;9(10):1108-20.

[3]. Gupta PS, et al. Regulation and Regulatory Role of WNT Signaling in Potentiating FSH Action during Bovine Dominant Follicle Selection. PLoS One. 2014 Jun 17;9(6):e100201.


[Related Small Molecules]

ICG-001 | Salinomycin | Wnt-C59 | Berberine chloride hydrate | Pyrvinium pamoate | ETC-159 | BML 284 | IWP-2 | Heparan Sulfate | KYA 1797K | FH535 | SKL2001 | CCT251545 | iCRT-14 | NCB-0846

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
643.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H19N3O3

[ Molecular Weight ]:
409.437

[ Flash Point ]:
343.2±31.5 °C

[ Exact Mass ]:
409.142639

[ PSA ]:
79.37000

[ LogP ]:
2.65

[ Appearance of Characters ]:
white to beige

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.741

[ Storage condition ]:
Store at RT

[ Water Solubility ]:
DMSO: soluble5mg/mL, clear

Related Compounds