KHS101 hydrochloride

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KHS101 hydrochloride  纯度: 99.87%

KHS101 hydrochloride 可选择性的诱导神经元分化表型,并能和转化酸性含螺旋蛋白 (TACC3) 发生相互作用。

KHS101 hydrochloride

KHS101 hydrochloride Chemical Structure

CAS No. : 1784282-12-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥935 In-stock
5 mg ¥850 In-stock
10 mg ¥1250 In-stock
25 mg ¥2500 In-stock
50 mg ¥4300 In-stock
100 mg ¥7310 In-stock
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500 mg   询价  

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生物活性

KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).

IC50 & Target

TACC3[1]

体外研究
(In Vitro)

KHS101 increases 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) is also observed under neurosphere-forming conditions in secondary neurospheres derived from both the hippocampus and the subventricular zone (SVZ) of adult rats. Moreover, hippocampal NPCs treated with KHS101 and cultured adherently on microelectrode arrays for 12 d exhibit neuronal morphologies as well as spontaneous spiking activity, hence indicating the presence of functional, maturing neurons[1]. KHS101 markedly attenuates tumor cell growth as compared to the cells treated with the vehicle [dimethyl sulfoxide (DMSO)]. TACC3 is a known target of KHS101 in rodent neural progenitor cells. KHS101 has been shown to cause cellular destabilization of TACC3, hence reducing endogenous TACC3 protein levels over time [2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Tumor cell proliferation is markedly reduced in KHS101-treated tumors (about twofold). KHS101-treated tumors show signs of elevated cell death (reduced cellularity/increased pyknosis) compared with tumors treated with vehicle control. KHS101 treatment markedly reduces both frontal-to-caudal tumor expansion and corpus callosum invasion of vimentin-positive GBM1 cells. It is also found that the survival of animals carrying GBMX1 tumors (established 2 or 6 weeks before treatment) is markedly increased by the KHS101 treatment regimen for 10 weeks. None of the mice have to be removed from the study because of adverse side effects of the treatment. An additional experiment using a continuous KHS101 treatment regimen until the experimental endpoints also shows a marked increase in the survival of GBMX1-bearing animals. Histological endpoint analysis of KHS101- and vehicle-treated animals confirms a significantly decreased tumor size in KHS101-treated mice[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

375.92

Formula

C18H22ClN5S

CAS 号

1784282-12-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 160 mg/mL (425.62 mM; Need ultrasonic)

H2O : 10 mg/mL (26.60 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6601 mL 13.3007 mL 26.6014 mL
5 mM 0.5320 mL 2.6601 mL 5.3203 mL
10 mM 0.2660 mL 1.3301 mL 2.6601 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.67 mg/mL (7.10 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (7.10 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 26.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.67 mg/mL (7.10 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (7.10 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 26.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.67 mg/mL (7.10 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (7.10 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 26.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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]. Polson ES, et al. KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. Sci Transl Med. 2018 Aug 15;10(454). pii: eaar2718.

Animal Administration
[2]

Rats[2]
Xenograft tumors in rats are allowed to establish for 6 weeks after injection of GBM1 cells (1×105 cells) into the forebrain striatum and treated with vehicle or KHS101 for 10 days [6 mg/kg, subcutaneously (sc), twice daily]. To examine whether the observed mitochondrial/redox anomaly is associated with reduced tumor progression, the KHS101 dosing regimen from previous neurogenesis work in rats is adapted using a 10-week tumor treatment strategy (6 mg/kg, sc, twice a day, and biweekly treatment alternating five and three treatment days per week)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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]. Polson ES, et al. KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. Sci Transl Med. 2018 Aug 15;10(454). pii: eaar2718.

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