您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > CUR 61414
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
CUR 61414
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CUR 61414图片
CAS NO:334998-36-6
包装与价格：
包装价格(元)
5mg电议
10mg电议

产品介绍
CUR 61414 是一种新型、有效且可渗透细胞的 Hedgehog 信号通路抑制剂 (IC50 \u003d100-200 nM)。
Cas No.334998-36-6
别名G-856
化学名N-[(3S,5S)-1-(1,3-benzodioxol-5-ylmethyl)-5-(1-piperazinylcarbonyl)-3-pyrrolidinyl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethyl-butanamide
Canonical SMILESO=C(CC(C)(C)C)N([C@H]1C[C@@H](C(N2CCN([H])CC2)=O)N(CC3=CC=C(OCO4)C4=C3)C1)CC5=CC(OC)=CC=C5
分子式C31H42N4O5
分子量550.7
溶解度≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 100-200 nM for hedgehog-induced cellular activity

CUR 61414 is a potent inhibitor of hedgehog-induced cellular activity.

The link between basal cell carcinoma (BCC) and aberrant activation of the Hedgehog (Hh) signaling pathway has been well established in humans and in mouse models.

In vitro: Previous study found that CUR61414 was able to arrest proliferation of basal cells within the BCC-like lesions and induce cells to undergo apoptosis resulting in complete regression of the lesions, without affecting neighboring skin cells [1].

In vivo: The efficacy of CUR61414 against basaloid lesions induced when mice were exposed to UV light. These mice were UV irradiated for 6-9 months, producing many microscopic BCC-like basaloid lesions throughout their skin. Results showed that the treatment with CUR61414 could cause regression of these lesions, as demonstrated by both X-gal staining and histological analyses. Moreover, the regression in the CUR61414-treated mice seemed to be the result of massive cell death, becuase a significant increase in apoptotic nuclei was seen in basaloid nests after treatment. In addition, no overt toxicity was observed in the skin surrounding the lesions [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Williams, J. A.,Guicherit, O.M.,Zaharian, B.I., et al. Identification of a small molecule inhibitor of the hedgehog signaling pathway: Effects on basal cell carcinoma-like lesions. Proceedings of the National Academy of Sciences of the United States of America 100(8), 4616-4621 (2003).