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KHS 101

KHS 101

产品编号 T4968   CAS 1262770-73-9

KHS 101 是一种新型转化酸性卷曲螺旋蛋白 3 (TACC3) 的抑制剂。它是神经元分化的选择性诱导剂。

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KHS 101 Chemical Structure
KHS 101, CAS 1262770-73-9
规格 价格/CNY 货期 数量
1 mg ¥ 382 现货
5 mg ¥ 900 现货
10 mg ¥ 1,380 现货
25 mg ¥ 2,200 现货
50 mg ¥ 3,400 现货
100 mg ¥ 4,930 现货
产品目录号及名称: KHS 101 (T4968)
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纯度: 98.00%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 KHS101 is a novel inhibitor of transforming acidic coiled-coil protein 3 (TACC3). It is a selective inducer of neuronal differentiation.
体外活性 KHS101 increased neuronal differentiation of adherently cultured rat NPCs in a dose-dependent fashion (EC50 ~ 1 μM). KHS101-induced neuron formation (40–60% TuJ1+ cells at 1.5–5 μM KHS101) was also observed under neurosphere-forming conditions in secondary neurospheres derived from both the hippocampus and the subventricular zone (SVZ) of adult rats [2]. SMMC-7721 and SK-Hep-1 cells were cultured with different KHS101 concentrations (40 μM and 20 μM, respectively) to determine the IC50 values. The number and size of spheres were significantly decreased after treatment with KHS101 compared with the control (DMSO) treatment. Sphere formation was dependent on the KHS101 concentration. Bmi1, c-Myc, and Nanog were all decreased in the presence of KHS101. Compared with the control (DMSO), KHS101 decreases the expression of p-AKT, p-GSK3β and β-catenin, as well as the expression of the downstream markers c-Myc and cyclin D1 [2].
体内活性 The doses of 6 mg/kg KHS101 (i.v. and s.c.) resulted in reasonable plasma concentrations (>1.5 μM) with a plasma half-life of 1.1–1.4 h, and relative bioavailability of 69% following s.c. dosing. Most importantly, the distribution of KHS101 to the brain was extensive as demonstrated by a brain-to-plasma AUC(0–3h) ratio of ~8 (dosing: 3 mg/kg KHS101, i.v.) [1].
激酶实验 NPC lysate was prepared by sonication in PBS and protein samples were prepared at a concentration of 2 mg/mL. The benzophenone-KHS101 compound (KHS101-BP, 5 μM) was added to 50 μL of the proteome reaction with and without unlabeled compound (250 μM). Irradiation was for 1 h using a hand-held UV lamp at long wavelength (365 nm), and subsequently, a copper-catalyzed azide-alkyne cycloaddition reaction was performed. After incubation for 1 h at RT, proteins were precipitated using trichloroacetic acid and resuspended in isoelectric focusing sample buffer. 2D SDS/PAGE was performed using ReadyStripe IPG stripes following the manufacturer's protocol [1].
细胞实验 Rat NPCs were derived and cultured as described previously by others. After hippocampal cell isolation, the number of dissociated cells was determined and ~5 × 10^5 cells were plated in 60-mm uncoated plates. After overnight incubation (37 °C, 5% CO2, and 95% humidity), the medium was changed and the cells were expanded and maintained in an undifferentiated state on polyornithine- (10 μg/mL in water) and laminin-coated (5 μg/mL in PBS;) dishes in DMEM/F12 supplemented with N2 and basic fibroblast growth factor (bFGF, 20 ng/mL;). For KHS101 and shRNA-induction experiments, early passage cells (passaged no more than six times after hippocampal isolation) were trypsinized and plated at a density of ~1,000 cells/cm2 into N2 medium (DMEM/F12 supplemented with N2) containing KHS analogs (e.g., KHS101, KHS92, and NP; SI Text) at different concentrations (0.5–5 μM) or DMSO (0.1%), RA (1–2 μM), BDNF (100 ng/mL), and/or BMP4 (50–100 ng/mL) for 4 d [1].
动物实验 To investigate the pharmacokinetic properties of KHS101, male Sprague–Dawley rats were administered 3 mg/kg KHS101 i.v. or s.c. One rat was killed per time point at 5 min, 40 min, 1 h, and 3 h after dosing, and samples of blood (100 μL) and whole brains were collected. In a separate study, rats were administered 6 mg/kg KHS101 i.v. or s.c. Five blood samples of 100 μL each were collected serially via a jugular vein catheter at 2 min (i.v. only), 0.5 h (s.c. only), and 1, 3, 7 and 24 h after dosing. Plasma and homogenized whole brain samples were analyzed by liquid chromatography-tandem mass spectrometry (LC-MS/MS). To study neuronal differentiation upon KHS101 administration in vivo, adult Fisher 344 rats (~10 wk old) received s.c. injections of 6 mg/kg KHS101 or vehicle control (5% ethanol in 15% Captisol). All rats received one daily i.p. injection of 200 mg/kg BrdU for 6 consecutive days after the first day. After 14 d, the animals were killed and perfusion fixed, and the brains were removed and subjected to immunohistochemical analysis [1].
分子量 339.46
分子式 C18H21N5S
CAS No. 1262770-73-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 15 mg/mL

DMSO: 15 mg/mL

计算器

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参考文献

1. Wurdak H, et al. A small molecule accelerates neuronal differentiation in the adult rat. Proc Natl Acad Sci U S A. 2010 Sep 21;107(38):16542-7. 2. Zhou DS, et al. TACC3 promotes stemness and is a potential therapeutic target in hepatocellular carcinoma. Oncotarget. 2015 Sep 15;6(27):24163-77.

文献引用

1. Shi S, Guo D, Ye L, et al.Knockdown of TACC3 inhibits tumor cell proliferation and increases chemosensitivity in pancreatic cancer.Cell Death & Disease.2023, 14(11): 778.
Mebendazole N-[2-(5-Chloro-1H-indol-3-yl)ethyl]-4'-cyanobiphenyl-2-carboxaMide Verubulin Epothilone A Albendazole Tau-aggregation and neuroinflammation-IN-1 Colchicine Thiocolchicine

相关化合物库

该产品包含在如下化合物库中:
微管靶向化合物库 NO PAINS 化合物库 抑制剂库 经典已知活性库 神经元分化化合物库 干细胞分化化合物库 已知活性化合物库 细胞骨架化合物库

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

KHS 101 1262770-73-9 Cytoskeletal Signaling Microtubule Associated KHS-101 KHS101 Inhibitor inhibitor inhibit

 

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