SMER3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SMER3  纯度: 98.02%

SMER3 一种 Rapamycin 增强剂, 是选择性的 Skp1-Cullin-F-box (SCF)Met30 泛素连接酶抑制剂。SMER3 通过抑制 SCFMet30 来增强 Rapamycin 的生长抑制作用。

SMER3

SMER3 Chemical Structure

CAS No. : 67200-34-4

规格 价格 是否有货 数量
5 mg ¥600 In-stock
10 mg ¥1000 In-stock
25 mg ¥2000 In-stock
50 mg ¥3000 In-stock
100 mg ¥4500 In-stock
200 mg   询价  
500 mg   询价  

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SMER3 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Oxygen Sensing Compound Library
  • Ubiquitination Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin’s growth inhibitory effect by inhibition of SCFMet30[1].

体外研究
(In Vitro)

In yeast cells, Met4 ubiquitination is blocked in cells exposed to SMER3 (0-60 μM). The met4Δ cells are less susceptible to growth inhibition by SMER3[1].
Addition of SMER3 to the ligase reactions inhibited ubiquitination of Met4 by SCFMet30 in a dose-dependent manner. SMER3 significantly inhibits the binding of Met30 to Skp1, and does not affect the Skp1 and Met30 protein levels[1].

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

224.18

Formula

C11H4N4O2

CAS 号

67200-34-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL (55.76 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.4607 mL 22.3035 mL 44.6070 mL
5 mM 0.8921 mL 4.4607 mL 8.9214 mL
10 mM 0.4461 mL 2.2304 mL 4.4607 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。-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: 1.25 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (5.58 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 12.5 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

*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]. Mariam Aghajan, et al. Chemical genetics screen for enhancers of rapamycin identifies a specific inhibitor of an SCF family E3 ubiquitin ligase. Nat Biotechnol. 2010 Jul;28(7):738-42.

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SMER28

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SMER28  纯度: 99.99%

SMER28 是一个调节自噬的、独立于 mTOR 信号通路机制的小分子阳性调节剂,能够阻止β淀粉样蛋白肽的累积。

SMER28

SMER28 Chemical Structure

CAS No. : 307538-42-7

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 ¥550 In-stock
5 mg ¥500 In-stock
10 mg ¥700 In-stock
25 mg ¥1400 In-stock
50 mg ¥2700 In-stock
100 mg ¥5200 In-stock
200 mg ¥8500 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

SMER28 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Autophagy Compound Library

生物活性

SMER28 is a positive regulator of autophagy acting via an mTOR-independent mechanism. SMER28 prevents the accumulation of amyloid beta peptide.

体外研究
(In Vitro)

SMER28 (5-200 μM; 24 hours) shows a dose dependent decline of cell viability[4].

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.

Cell Viability Assay[4]

Cell Line: MMS1 cells
Concentration: 5, 25, 50, 75, 100, 150, 200 μM
Incubation Time: 24 hours
Result: Showed a dose dependent decline of cell viability.

体内研究
(In Vivo)

SMER28 (15-65 mg/kg; i.h.; daily, two days before irradiation and during the three days of irradiation) significantly protects against post-irradiation weight loss and enhances survival of mice at 65 mg/kg[5].

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.

Animal Model: 14 to 16 weeks male mice (Balb/c)[5]
Dosage: 15, 65 mg/kg
Administration: Subcutaneous injection; two days before irradiation and during the three days of irradiation (total 5 days)
Result: Significantly protected against post-irradiation weight loss and enhanced survival of mice at 65 mg/kg.

分子量

264.12

Formula

C11H10BrN3

CAS 号

307538-42-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 32 mg/mL (121.16 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7862 mL 18.9308 mL 37.8616 mL
5 mM 0.7572 mL 3.7862 mL 7.5723 mL
10 mM 0.3786 mL 1.8931 mL 3.7862 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。-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: ≥ 2.5 mg/mL (9.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.47 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (9.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.47 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (9.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.47 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 25.0 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]. Renna M et al. Chemical inducers of autophagy that enhance the clearance of mutant proteins in neurodegenerative diseases. J Biol Chem. 2010 Apr 9;285(15):11061-7.

    [2]. Nekova TS, et al. Small molecule enhancers of rapamycin induce apoptosis in myeloma cells via GSK3A/Bpreferentially within a protective bone marrow microenvironment. Br J Haematol. 2014 Oct;167(2):272-4.

    [3]. Shen D et al. Novel cell- and tissue-based assays for detecting misfolded and aggregated protein accumulation within aggresomes and inclusion bodies. Cell Biochem Biophys. 2011 Jul;60(3):173-85.

    [4]. Koukourakis MI, et al. SMER28 is a mTOR-independent small molecule enhancer of autophagy that protects mouse bone marrow and liver against radiotherapy. Invest New Drugs. 2018 Oct;36(5):773-781.

    [5]. Tian Y et al. A small-molecule enhancer of autophagy decreases levels of Abeta and APP-CTF via Atg5-dependent autophagy pathway. FASEB J. 2011 Jun;25(6):1934-42.

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SMER18

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SMER18 

SMER18是Rapamycin的一种小分子增强剂, 充当mTOR非依赖性的的自噬诱导剂。

SMER18

SMER18 Chemical Structure

CAS No. : 944153-47-3

规格 价格 是否有货 数量
2 mg ¥2333 In-stock
5 mg ¥3500 In-stock
10 mg ¥5000 In-stock
50 mg ¥15000 询价
100 mg ¥21000 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SMER18 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Autophagy Compound Library

生物活性

SMER18 is a small molecule enhancer of rapamycin which act as a mTOR-independent autophagy inducer. Target: mTOR SMER18 induces autophagy independently of Rapamycin in mammalian cells, enhancing the clearance of autophagy substrates such as mutant huntingtin and A53T alpha-synuclein, which are associated with Huntington’s disease and familial Parkinson’s disease, respectively. SMER18 acts either independently or downstream of the target of Rapamycin, attenuates mutant huntingtin-fragment toxicity in Huntington’s disease cell and Drosophila melanogaster models, which suggests therapeutic potential.

分子量

287.74

Formula

C16H14ClNO2

CAS 号

944153-47-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Sarkar S, et al. Small molecules enhance autophagy and reduce toxicity in Huntington’s disease models. Nat Chem Biol. 2007 Jun;3(6):331-338.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务