IWR-1-endo (Synonyms: endo-IWR 1; IWR-1-endo)
目录号: PC78843 纯度: ≥98%

IWR-1是端锚聚合酶抑制剂,抑制Wnt/β-catenin信号传导途径。

CAS No. :1127442-82-3
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中文名称
IWR-1-endo
中文别名
H-89二盐酸盐;H-89二盐酸盐水合物;H-89二盐酸盐;N-[2-(p-溴肉桂酰基氨基)乙基]-5-异喹啉磺酰胺双盐酸盐
英文名称
IWR-1-endo
英文别名
5-Isoquinolinesulfonamide,N-[2-[[3-(4-bromophenyl)-2-propen-1-yl]amino]ethyl]-, hydrochloride (1:2);N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinoline Sulfonamide Dihydrochloride;H-89 dihydrochloride hydrate;H 89 2HCl;5-Isoquinolinesulfonamide,N-[2-[[3-(4-bromophenyl)-2-propen-1-yl]amino]ethyl]-, hydrochloride ...;H 89 dihydrochloride;H-89, Dihydrochloride;Protein kinase inhibitor H-89 dihydrochloride;H-89 hydrate dihydrochloride;(E)-N-(2-(4-bromocinnamylamino)ethyl)isoquinoline-5-sulfonamide dihydrochloride;(E)-N-(2-((3-(4-bromophenyl)allyl)amino)ethyl)isoquinoline-5-sulfonamide dihydrochloride;N-[2-[[3-(4-BroMophenyl)-2-propen-1-yl]aMino]ethyl]-5-isoquinolinesulfonaMide Hydrochloride;5-IsoquinolinesulfonaMide, N-[2-[[3-(4-broMophenyl)-2-propenyl]aMino]ethyl]-, dihydrochloride;N-[2-[[3-(4-Bromophenyl)-2-Propen-1-Yl]Amino]Ethyl]-5-Isoquinolinesulfonamide Hydrochloride (1:2);H-89 Dihydrochloride Hydrate,N-[2-(P-Bromocinnamylamino)Et;H-89 dihydrochloride
Cas No.
1127442-82-3
分子式
C25H19N3O3
分子量
409.44
包装储存
Powder -20°C 3 years|4°C 2 years
In solvent -80°C 2 years|-20°C 1 year
产品详情
IWR-1是端锚聚合酶抑制剂,抑制Wnt/β-catenin信号传导途径。
生物活性
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
性状
固体
IC50 & Target[1][2]
IC50: 180 nM (Wnt)
体外研究(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].
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years|4°C 2 years
In solvent -80°C 2 years|-20°C 1 year
参考文献

[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. 

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