| AM580Selective RARα agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.60%
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| Cas No. | 102121-60-8 | SDF | Download SDF |
| Canonical SMILES | O=C(C1=CC=C2C(C)(C)CCC(C)(C)C2=C1)NC3=CC=C(C(O)=O)C=C3 | ||
| Formula | C22H25NO3 | M.Wt | 351.44 |
| Solubility | ≥14.3mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AM580 is a selective agonist of retinoic acid receptor α (RARα) with IC50 and EC50 values of 8 nM and 0.36 nM, respectively [1].
RARα is ubiquitously expressed. It is important for retinoid response during growth and differentiation of epithelial cells. RARα have functions in the inhibition of cell and mammary tumour growth, increase in tumour latency, induction of cell cycle arrest, stimulation of cell death, and up-regulation of RARα and RARγ mRNA [1, 2]. In addition, RARα is involved in the production of human T cell activation and type 2 cytokine [3].
In SK-BR-3 and T47D breast cancer cell lines, treatment with AM580 at concentrations of 1 nM and 10 nM for 7 days resulted in the decrease in the number of cells [1]. AM580 at a concentration of 200 nM, enhanced the anti-proliferative effect shown by the knockdown of RAR-γ in MCF-10A breast epithelial and MCF-7 cell lines [2].
When 200 nM AM580 was applied to MMTV-Myc female mice for 96 hours, this led to impaired cell proliferation capacity. Furthermore, combination of AM580 with 100 nM CD437 and SR11253 resulted in strong growth inhibition, clearly demonstrating the ability of AM580 to reduce the tumour growth in MMTV-Myc tumour model [2].
References: [1]. Schneider S, Offterdinger M, Huber H, et al. Activation of Retinoic Acid Receptor a Is Sufficient for Full Induction of Retinoid Responses in SK-BR-3 and T47D Human Breast Cancer Cells. Cancer Res, 2000, 60(19):5479-87.[2]. Bosch A, Bertran S, Lu Y, et al. Reversal by RARa agonist Am580 of c-Myc induced imbalance in RARa/RARγ expression during MMTV-Myctumorigenesis. Breast Cancer Res, 2012, 14(4):R121.[3]. Dawson H, Collins G, Pyle R, et al. The Retinoic Acid Receptor-α mediates human T-cell activation and Th2 cytokine and chemokine production. BMC Immunol, 2008, 9:16.
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之前是担心所需组织量不够（要求是200-300mg，我的组织只有20mg左右）才跑不出来，后来换用大鼠心脏测试，组织量绝对够。。。而且在跑western之前进行了说明书上的蛋白浓缩步骤，可是在加loADIngbuffer之后，蛋白沉淀怎么都溶解不掉~说明书也注明了如果有沉淀可以取上清继续上样，可是每次上样感觉样品往上浮，只有部分样品往孔里沉，而且跑出来什么都没有，连内参都没有。用的是β-actin的内参。。
western之前浓缩步骤如下:
1、取所得提取物，每100ul膜蛋白加入约300ul的溶解buffer和约100ul三氯乙酸（TCA）试剂，混匀后置冰上20-30min后，13000rpm，离心15min，尽可能去除上清。
2、沉淀加入1ml丙酮，室温静置10min后，13000rpm离心15min。
3、弃上清，沉淀真空旋干或置冰上干燥10min（敞开离心管盖），按适当体积比加入loadingbuffer（使用前没100ulloadingbuffer加入2-5ulβ-巯基乙醇）溶解，彻底分散（枪头反复吹吸或剧烈涡旋），煮沸5min。【注：加入loadingbuffer后如有部分难容物，可取上清继续上样。】
