| YK-4-279RNA Helicase A (RHA) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.72%
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Chemical structure
| Description | YK-4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1 | |||||
| Targets | RNA Helicase A | |||||
| IC50 | ||||||
| Cell experiment [1-3]: | |
Cell lines | VCaP cells, LNCaP cells |
Preparation method | The solubility of this compound in DMSO is >16.35 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 10 μM, 48 hr |
Applications | YK-4-279 inhibited ERG and ETV1 mediated transcriptional activity. YK-4-279 bound to ERG with an affinity (KD) of 11.7 μM and bound to ETV1 with an affinity of 17.4 μM. In LNCaP cells, YK-4-279 (1 μM) resulted in decreased gene expression of MMP13 without significant reduction in ETV1 levels. In VCaP cells, YK-4-279 (10 μM, 48 hours) decreased expression of PLAU, ADAM19 and PLAT mRNA. YK-4-279 inhibited VCaP (10 μM) and LNCaP (1 μM) cell invasion of HUVECs. YK-4-279 (10 μM) inhibited motility in a scratch assay in high-passage LNCaP cells. YK-4-279 showed anti-proliferative activity with the IC50 values of 1 and 8 μM in primary cell lines ES925 and GUES1. YK-4-279 induced caspase-3 activity in four ESFT cell lines (TC32, A4573, TC71, and ES925). Treatment of TC32, HEK293, HFK, and HEC with short-term (6 hours) high dose (50 μM) YK-4-279 resulted in significant apoptosis of the ESFT cells. In LNCaP-luc-M6 cells, YK-4-279 (1 μM) significantly reduced mRNA levels of several ETV1 target genes, including MMP7, MMP13, FKBP10 and GLYATL2, without affecting the expression of ETV1. YK-4-279 treatment of LNCaP-luc-M6 cells resulted in a significant decrease in cell migration. |
| Animal experiment [2,3]: | |
Animal models | SCID/bg mice bearing ESFT (orthotopic) or prostate cancer cell xenograft tumors, SCID/beige mice subcutaneously injected with LNCaP-luc-M6 |
Dosage form | Intraperitoneal injection, 1.5mg/dose, three times per week; 75 mg/kg YK-4-279 three times a week and 150 mg/kg YK-4-279 five times a week |
Application | YK-4-279 (1.5 mg/dose i.p.) inhibited the growth of ESFT xenograft tumors. In SCID/beige mice were subcutaneously injected with LNCaP-luc-M6 cells, YK-4-279 (75 mg/kg YK-4-279 three times a week and 150 mg/kg YK-4-279 five times a week) reduced tumor growth and inhibited lung metastasis. YK-4-279 treatment resulted in decreased gene expression of MMP7, GLYATL2 and FKBP10 in LNCaP-luc-M6 animals. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Rahim S, Beauchamp E M, Kong Y, et al. YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion[J]. PloS one, 2011, 6(4): e19343. [2]. Erkizan H V, Kong Y, Merchant M, et al. A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing"s sarcoma[J]. Nature medicine, 2009, 15(7): 750-756. [3]. Rahim S, Minas T, Hong S H, et al. A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model[J]. PloS one, 2014, 9(12): e114260. | |
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| Cas No. | 1037184-44-3 | SDF | Download SDF |
| Synonyms | YK 4-279 | ||
| Chemical Name | 4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one | ||
| Canonical SMILES | COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O | ||
| Formula | C17H13Cl2NO4 | M.Wt | 366.2 |
| Solubility | ≥16.35 mg/mL in DMSO, ≥24.25 mg/mL in EtOH with ultrasonic, <2.44 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| 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. | ||
YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.
EWS-FLI1 is a disordered protein that precludes standard structure-based small-molecule inhibitor design. EWS-FLI1 binding to RNA helicase A (RHA) is important for its oncogenic function.
In vitro: ESFT cells treated with YK-4-279 showed a dissociation of EWS-FLI1 from RHA by 10 mM, consistent with the KD value. The EWS-FLI1–transfected cells showed a dose-dependent decrease in promoter activity when treated for 18 h with 3 mM and 10 mM YK-4-279. YK-4-279 was relatively specific for ESFT cells as compared to the nontransformed HEK293 cells [1].
In vivo: The tumor growth rate of YK-4-279–treated mice bearing CHP-100 was lower than that in mice having PC3 prostate tumors. The cumulative data from five independent experiments with the ESFT xenografts (TC71 and CHP-100) show a marked overall tumor reduction in the YK-4-279–treated mice. Pathological analysis of mice treated with YK-4-279 did not show any signs of toxicity, except for sterile inflammatory lesions in the abdominal cavities of mice [1].
Clinical trial: No clinical data are available currently.
Reference:[1] Erkizan HV, Kong Y, Merchant M, Schlottmann S, Barber-Rotenberg JS, Yuan L, Abaan OD, Chou TH, Dakshanamurthy S, Brown ML, Uren A, Toretsky JA. A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing"s sarcoma. Nat Med. 2009;15(7):750-6.
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特点
零耐药性，零药物残留，调控瘤胃微生物，提高饲料吸收，提高产奶量、降低体细胞、防治隐性乳房炎。
主要成分
抗牛乳房炎特异性IgY、乳酸芽孢杆菌、嗜酸乳杆菌、螯合维生素、半胱胺肽、全卵蛋白肽、活性酵母菌、螯合铁、铜、锌，抗病因子、保健因子、有益菌、生物活性复合酶、生物活性小肽等多种高档原料。
产品性状
本品呈黄褐色粉末，有特别的发酵芳香味。
功能特点
采用“三步多相联合发酵”专利技术生产,经深层发酵，离心、真空低温干燥后，辅以免疫多糖和多种科学配制而成。
1、可彻底分解霉变饲料中的弱极性霉菌毒素，可完全替代预防用抗生素;
2、可明显提高奶牛生产的各个指标，试验证明提高产奶量8-20%。延长产奶高峰15-35天，提高乳脂率0.25-0.4%，同时提高乳蛋白含量0.02-0.05%;
3、对防治奶牛乳房炎有特效，可降低乳房炎发病率60-70%，同时防治奶牛酸奶症效果突出;
4、加快犊牛瘤胃发育，可有效降低腹泻率47%，提高饲料利用率2.5%;
5、生物学稳定性高，耐挤压、耐酸碱(PH3-9)、耐高温(90℃加热30分钟活菌损失不到1%);
6、减少粪便排泄量，可降低牛舍氨臭味，减少。
应用范围：
犊牛、青年牛、高产奶牛、干乳奶牛。
使用方法：
①犊牛本品1000g拌料1000-2000斤，如发生腹泻时本品1000g拌料500斤均匀混饲;
②青年牛和干乳奶牛本品1000g拌料1000-2000斤，均匀混饲;
③高产奶牛本品1000g拌料500-1000斤，均匀混饲，如遇天气突变、转群、噪音等各种应激情况本品1000g拌料500-1000斤添加使用。
望采纳！！
英 [kənˈtɪnju:]美 [kənˈtɪnju]
vi.
持续;逗留;维持原状
vt.
延期;使延伸;使持续;继续说
如题，求购做wb时适用于牛的抗纤连蛋白抗体，分装或者试用装皆可，不求多么高质量，做出来的东西能毕业就行，谢谢~~
有没有知道哪个公司可以买到几种牛病毒的荧光标记的抗体？
我要做细胞的免疫荧光实验。
1．Bluetongue蓝舌病毒
2．BovineAdenovirus牛腺病毒
3．BovineParvovirus牛细小病毒
4．BovineRespiratorySyncytialVirus牛呼吸道融合病毒
5．BovineVirusDiarrhoea牛腹泻病毒
6．Reovirus呼肠孤病毒－3
7．InfectiousBovineRhinotracheitis，IBR传染性牛鼻气管炎病毒
8．BovineParainfluenzaVirusType3，PI3牛副流行性感冒3型病毒
9．RABIes狂犬病毒
能提供一种的也可以，多谢啊～～～～～～～
