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2097938-51-5
  • names:

    R-10015

  • CAS號:

    2097938-51-5

    MDL Number: No data available
  • MF(分子式): C20H19ClN6O2 MW(分子量): 410.86
  • EINECS:No data available Reaxys Number:No data available
  • Pubchem ID:129896912 Brand:BIOFOUNT
R-10015
R-10015(2097938-51-5)是一種用于 HIV 感染的廣譜抗病毒化合物,R-10015是高效選擇性的 LIMK 抑制劑,R-10015通過結(jié)合 ATP 結(jié)合口袋阻斷 LIMK,抑制人 LIMK1 的 IC50 值為 38 nM。
貨品編碼 規(guī)格 純度 價格 (¥) 現(xiàn)價(¥) 特價(¥) 庫存描述 數(shù)量 總計 (¥)
YZM000862-10mg 10mg 99% ¥ 5568.00 ¥ 5568.00 2-3天
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0.00
YZM000862-5mg 5mg 99% ¥ 3412.00 ¥ 3412.00 2-3天
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中文別名 R-10015(2097938-51-5)
英文別名 R-10015,2097938-51-5
CAS號 2097938-51-5
Inchi InChI=1S/C20H19ClN6O2/c1-29-20(28)12-2-3-14-15(8-12)26-17(25-14)11-4-6-27(7-5-11)19-16-13(21)9-22-18(16)23-10-24-19/h2-3,8-11H,4-7H2,1H3,(H,25,26)(H,22,23,24)
InchiKey MGRJCGXCUUCOQG-UHFFFAOYSA-N
分子式 Formula C20H19ClN6O2
分子量 Molecular Weight 410.86
溶解度Solubility 生物體外In Vitro:DMSO溶解度62.5 mg/mL(152.12 mM;Need ultrasonic)H2O< 0.1 mg/mL(insoluble)
性狀 灰白色至粉紅色固體粉末
儲藏條件 Storage conditions -20°C 3 years年 4°C 2 years年 / 溶液中:-80°C 6 months月 -20°C 1 month月

R-10015(2097938-51-5)實驗注意事項:
1.實驗前需戴好防護眼鏡,穿戴防護服和口罩,佩戴手套,避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生,必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲,并交于專業(yè)生物廢氣物處理公司處理,以免造成環(huán)境污染

R-10015(2097938-51-5) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tag:R-10015(2097938-51-5),R-10015試劑,R-10015抑制劑,R-10015的作用,R-10015的合成,R-10015的純度,R-10015的生產(chǎn),R-10015的使用,R-10015的外觀,R-10015的溶解度,R-10015的含量,R-10015的選擇,R-10015的MSDS
產(chǎn)品說明 R-10015(2097938-51-5)是一種用于 HIV 感染的廣譜抗病毒化合物,R-10015是高效選擇性的?LIMK?抑制劑
IntroductionR-10015 (2097938-51-5) is a broad-spectrum antiviral compound for HIV infection, R-10015 is a highly effective and selective LIMK inhibitor
Application1
Application2
Application3

Discovery of Novel Small-Molecule Inhibitors of LIM Domain Kinase for Inhibiting HIV-1
Abstract:
A dynamic actin cytoskeleton is necessary for viral entry, intracellular migration, and virion release. For HIV-1 infection, during entry, the virus triggers early actin activity by hijacking chemokine coreceptor signaling, which activates a host dependency factor, cofilin, and its kinase, the LIM domain kinase (LIMK). Although knockdown of human LIM domain kinase 1 (LIMK1) with short hairpin RNA (shRNA) inhibits HIV infection, no specific small-molecule inhibitor of LIMK has been available. Here, we describe the design and discovery of novel classes of small-molecule inhibitors of LIMK for inhibiting HIV infection. We identified R10015 as a lead compound that blocks LIMK activity by binding to the ATP-binding pocket. R10015 specifically blocks viral DNA synthesis, nuclear migration, and virion release. In addition, R10015 inhibits multiple viruses, including Zaire ebolavirus (EBOV), Rift Valley fever virus (RVFV), Venezuelan equine encephalitis virus (VEEV), and herpes simplex virus 1 (HSV-1), suggesting that LIMK inhibitors could be developed as a new class of broad-spectrum antiviral drugs.IMPORTANCE The actin cytoskeleton is a structure that gives the cell shape and the ability to migrate. Viruses frequently rely on actin dynamics for entry and intracellular migration. In cells, actin dynamics are regulated by kinases, such as the LIM domain kinase (LIMK), which regulates actin activity through phosphorylation of cofilin, an actin-depolymerizing factor. Recent studies have found that LIMK/cofilin are targeted by viruses such as HIV-1 for propelling viral intracellular migration. Although inhibiting LIMK1 expression blocks HIV-1 infection, no highly specific LIMK inhibitor is available. This study describes the design, medicinal synthesis, and discovery of small-molecule LIMK inhibitors for blocking HIV-1 and several other viruses and emphasizes the feasibility of developing LIMK inhibitors as broad-spectrum antiviral drugs.

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