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2097938-51-5
  • names:

    R-10015

  • CAS号:

    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)是一种用于 HIV 感染的广谱抗病毒化合物,R-10015是高效选择性的 LIMK 抑制剂,R-10015通过结合 ATP 结合口袋阻断 LIMK,抑制人 LIMK1 的 IC50 值为 38 nM。
货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
YZM000862-10mg 10mg 99% ¥ 5568.00 ¥ 5568.00 2-3天
- +
¥ 0.00
YZM000862-5mg 5mg 99% ¥ 3412.00 ¥ 3412.00 2-3天
- +
¥ 0.00
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中文别名 R-10015(2097938-51-5)
英文别名 R-10015,2097938-51-5
CAS号 2097938-51-5
SMILES O=C(C1=CC=C2NC(C3CCN(C4=C5C(NC=C5Cl)=NC=N4)CC3)=NC2=C1)OC
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
闪点 FP No data available
熔点 Melting point No data available
沸点 Boiling point No data available
Polarizability极化度 No data available
密度 Density No data available
蒸汽压 Vapor Pressure No data available
溶解度Solubility 生物体外In Vitro:DMSO溶解度62.5 mg/mL(152.12 mM;Need ultrasonic)H2O< 0.1 mg/mL(insoluble)
性状 灰白色至粉红色固体粉末
储藏条件 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)实验注意事项:
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染

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试剂,R-10015抑制剂,R-10015的作用,R-10015的合成,R-10015的纯度,R-10015的生产,R-10015的使用,R-10015的外观,R-10015的溶解度,R-10015的含量,R-10015的选择,R-10015的MSDS
产品说明 R-10015(2097938-51-5)是一种用于 HIV 感染的广谱抗病毒化合物,R-10015是高效选择性的?LIMK?抑制剂
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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