您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > AC 55649
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:
 
AC 55649
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。
AC 55649图片
CAS NO:59662-49-6
规格:98%
分子量:310.44
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
RARβ2 agonist, potent and selective
CAS:59662-49-6
分子式:C21H26O2
分子量:310.44
纯度:98%
存储:Store at -20°C

Background:

AC 55649 is a potent and selective agonist of retinoic acid receptor β2 (RARβ2) isotype with a pEC50 value of 6.9 ± 0.4 [1].


RARβ2 is a tumor suppressor gene. In several human neoplasms, it is frequently hypermethylated [2].


In MCF7 cells, AC 55649 significantly inhibited cellular growth, appeared to inhibit DNA synthesis as seen in experiments of [3H] thymidine incorporation. The extent of the inhibition was comparable to the one resulted from the presence of all-trans-retinoic acid [1]. In vitro, RARβ2 induced the neurite outgrowth in adult mouse spinal cord [3]. Before neurite outgrowth, cells were stimulated with either AC 55649 or retinoic acid for 1 week. Treatment with retinoic acid largely increased the neurite outgrowth of cells, compared with the control. This result was revealed by immunocytochemistry. AC 55649 also induced the neurite outgrowth of NTERA-2 cells. This indicated that AC 55649 mediated neuronal differentiation in a manner similar to that found with retinoic acid. Using another differentiation marker, Neurofilament L, similar results were also evident [1].


Retinoids influence both differentiation and morphogenetic events during development of the vertebrate limb. These effects are mediated by nuclear retinoid receptors. In the posterior limb bud, transcripts of RARβ2 but not RARβ1 are enriched to three-fold. Transcripts of RARβ1 are initially present throughout the limb bud ectoderm and mesenchyme, then become restricted within the loose connective tissue and perichondrial regions of the limb [4]. In Xenopus, treated with AC 55649 at 100 nM, approximately 65% of larvae survived and practically all started to form a pair of bilaterally symmetric limb buds. Treatments with AC 55649 provoked the death of larvae at the metamorphosis onset at around stage 62. Stage 62 is a stage showing peak levels of T3 and T4 thyroid hormones. Meanwhile all larvae without treatment were metamorphosed [5].


参考文献:
[1].  Piu F, Gauthier NK, Olsson R, et al. Identification of novel subtype selective RAR agonists. Biochemical pharmacology, 2005, 71(1): 156-162.
[2].  Jerónimo C, Henrique R, Hoque MO, et al. Quantitative RARβ2 Hypermethylation A Promising Prostate Cancer Marker. Clinical Cancer Research, 2004, 10(12): 4010-4014.
[3].  Maden M, Hind M. Retinoic acid, a regeneration-inducing molecule. Developmental dynamics, 2003, 226(2): 237-244.
[4].  Cuervo R, Chimal-Monroy J. Chemical activation of RARβ induces post-embryonically bilateral limb duplication during Xenopus limb regeneration. Scientific reports, 2013, 3.
[5].  Smith SM, Kirstein IJ, Wang ZS, et al. Differential expression of retinoic acid receptor-β isoforms during chick limb ontogeny. Developmental Dynamics, 1995, 202(1): 54-66.