BMS 195614
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BMS 195614是RARα的选择性拮抗剂[1],可结合RARα亚基[5]。
BMS195614,4-[[[[5,6-二氢-5,5-二甲基-8-(3-喹啉基)]-2-萘基]羰基]氨基]苯甲酸[2],是维甲酸的拮抗剂,通过伴随地转染视黄酸受体(RAR),抑制全反式视黄酸诱导的(ATRA诱导的)视黄酸反应元件-氯霉素乙酰转移酶(RARE-CAT)报告子表达[3][4]。
视黄酸(RA)是维生素A(视黄醇)最主要的具有生物活性的衍生物(一并称作维甲酸)。视黄酸对细胞分化、脊椎动物发育和稳态有多种重要作用[6]。
BMS 195614可逆转RARα选择性激活剂AM580、AM80和BMS 194753对急性早幼粒细胞白血病细胞系NB4和HL60分化的诱导效应[1]。视黄酸(RA)(10-6 M)处理72小时可显著降低T47D乳腺癌细胞转移。但RA与BMS 195614结合不影响细胞运动[7]。在牛肌内脂肪来源的间质-血管细胞中,BMS 195614可显著减弱ATRA的抗脂肪形成作用[8]。
BMS 195614在小鼠口服给药时体内活性较差。BMS 195614口服给药1个月对精子生成无抑制作用[3]。口服BMS 195614不能抑制小鼠精子生成[9]。
参考文献:
[1]. F. Christopher Zusi, Matthew V. Lorenzi and Valerie Vivat-Hannah. Selective retinoids and rexinoids in cancer therapy and chemoprevention. Drug Discovery Today, 2002, 7(23):1165-1174.
[2]. John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, et al. Bristol-Myers Squibb Co. Retinoid-like Heterocycles. US patent 5,559,248. 1996 Sep. 24.
[3]. Sanny S. W. Chung, Rebecca A. D. Cuellar, Xiangyuan Wang, et al. Pharmacological Activity of Retinoic Acid Receptor Alpha-Selective Antagonists in Vitro and in Vivo. ACS Med. Chem. Lett., 2013, 4: 446-450.
[4]. Eun Young Park, Alice Dillard, Elizabeth A. Williams, et al. Retinol Inhibits the Growth of All-Trans-Retinoic Acid–Sensitive and All-Trans-Retinoic Acid–Resistant Colon Cancer Cells through a Retinoic Acid Receptor–Independent Mechanism. Cancer Res., 2005, 65(21):9923-9934.
[5]. Dongchun Liang, Aijun Zuo, Hui Shao, et al. Retinoic Acid Inhibits CD25 Dendritic Cell Expansion and cd T-Cell Activation in Experimental Autoimmune Uveitis. Invest Ophthalmol Vis Sci., 2013, 54:3493-3503.
[6]. Pierre Chamban. A decade of molecular biology of retinoic acid receptors. FASEBJ., 1996, 10:940-954.
[7]. Flamini Marina Ines, Gauna Gisel Valeria, Sottile Mayra Lis, et al. Retinoic acid reduces migration of human breast cancer cells: role of retinoic acid receptor β. J. Cell. Mol. Med., 2014, 18(6): 1113-1123.
[8]. Nikolas Gunkel, Thorsten Meyer and John Michael Graettinger; N/A. Method of Modulating the Degree of Adipose Tissue Deposited Intramuscularly. US patent 20140094512A1. 2014 Apr. 3.
[9]. Fern E. Murdoch and Erwin Goldberg. Male contraception: Another holy grail. Bioorg. Med. Chem. Lett., 2014, 24:419-424.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 448.5 |
Cas No. | 182135-66-6 |
Formula | C29H24N2O3 |
Synonyms | BMS 614 |
Solubility | <11.21mg/ml in DMSO |
Chemical Name | 4-[[[5,6-dihydro-5,5-dimethyl-8-(3-quinolinyl)-2-naphthalenyl]carbonyl]amino]-benzoic acid |
SDF | Download SDF |
Canonical SMILES | CC1(CC=C(C2=C1C=CC(C(NC3=CC=C(C(O)=O)C=C3)=O)=C2)C4=CC(C=CC=C5)=C5N=C4)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |