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SR 11302

现货
Catalog No.
A8185
AP-1转录因子抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 960.00
现货
10mg
¥ 1,750.00
现货
25mg
¥ 3,940.00
Ship with 10-15 days

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Background

SR 11302 is an inhibitor of activator protein-1 (AP-1) [1].AP-1 is a transcription factor that displays antitumor effects in vivo.
SR 11302 is an inhibitor of AP-1 but don’t activate RARs and RXR. SR11302 failed to inhibit the proliferation of F9 cells, the embryonal carcinoma cell line. While, it can inhibit the growth of breast cancer cell line T-47D, the lung cancer line Calu-6 and HeLa cells[1]. SR 11302 had very little effect on either the proliferation or the differentiation of HL-60, fresh APL and NB4 cells, which indicate that AP-1 may not be involved in the signaling pathway of proliferation and differentiation of HL-60, fresh APL and NB4 cells [2].
In an AP-1-luciferase transgenic mouse carcinogenesis model, SR11302 significantly inhibit both AP-1 activation in 7,12-dimethyl benz(a)anthracene-initiated mouse skin and 12-O-tetradecanoylphorbol-13-acetate-induced papilloma formation. While, SR11235, a retinoid with RARE transactivating activity, but lack of AP-1 inhibiting effect, didn’t inhibit papilloma formation and AP-1 activation. These results show that the antitumor effect of retinoids is mediated by blocking AP-1 activity in vivo [3].
References:
[1]. Fanjul A, Dawson MI, Hobbs PD, et al. A new class of retinoids with selective inhibition of AP-1 inhibits proliferation. Nature, 1994, 372(6501): 107-111.
[2]. Shiohara M, Dawson MI, Hobbs PD, et al. Effects of novel RAR- and RXR-selective retinoids on myeloid leukemic proliferation and differentiation in vitro. Blood, 1999, 93(6): 2057-2066.
[3]. Huang C, Ma WY, Dawson MI, et al. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc Natl Acad Sci U S A, 1997, 94(11): 5826-5830.

文献引用

1. Ding RR, Yuan JL, et al. "Epstein-Barr virus-encoded LMP1 regulated Pim1 kinase expression promotes nasopharyngeal carcinoma cells proliferation." Onco Targets Ther. 2019 Feb 11;12:1137-1146. PMID:30809095
2. Wang T, Jin X, et al."Association of NF-κB and AP-1 with MMP-9 Overexpression in 2-Chloroethanol Exposed Rat Astrocytes." Cells. 2018 Aug 7;7(8). pii: E96. PMID:30087244
3. Michael John Vanden Oever. "Regulation of Type VII Collagen in Patients with Recessive Dystrophic Epidermolysis Bullosa." UNIVERSITY OF MINNESOTA.2017.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt376.54
Cas No.160162-42-5
FormulaC26H32O2
SolubilitySoluble in DMSO
Chemical Name3-methyl-7-(4-methylphenyl)-9-(2,6,6-trimethylcyclohexen-1-yl)nona-2,4,6,8-tetraenoic acid
SDFDownload SDF
Canonical SMILESCC1=C(C(CCC1)(C)C)C=CC(=CC=CC(=CC(=O)O)C)C2=CC=C(C=C2)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

T-47D,Calu-6和HeLa细胞系

溶解方法

在DMSO中的溶解度> 10 mM。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

10-6 M

应用

SR 11302可有效抑制T-47D,Calu-6和HeLa细胞的增殖,可作为新的低副作用的类视黄醇治疗剂的候选者。

动物实验[2]:

动物模型

AP-1-荧光素酶转基因小鼠

剂量

34nmol溶解于300μl丙酮中,连续7天,每天4次

应用

SR 11302可以通过阻断小鼠体内AP-1的活性,从而介导抗肿瘤效果,是化疗和化学预防癌症最有希望的候选药物之一。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Fanjul A, Dawson MI, Hobbs PD, et al. A new class of retinoids with selective inhibition of AP-1 inhibits proliferation. Nature, 1994, 372(6501): 107-111.

[2] Huang C, Ma WY, Dawson MI, et al. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc Natl Acad Sci U S A, 1997, 94(11): 5826-5830.

质量控制

质量控制和MSDS

批次:

化学结构

SR 11302

相关生物数据

SR 11302

相关生物数据

SR 11302

相关生物数据

SR 11302