LIN28 inhibitor LI71

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。

LIN28 inhibitor LI71  纯度: 98.10%

LIN28 inhibitor LI71 是一种高效、细胞渗透性的 LIN28 抑制剂,能消除 LIN28 介导的寡核苷酸化,其 IC50 值为 7 uM。LIN28 inhibitor LI71 能直接绑定 CSD,抑制 LIN28 对 let-7 的作用活性。

LIN28 inhibitor LI71

LIN28 inhibitor LI71 Chemical Structure

CAS No. : 1357248-83-9

规格 价格 是否有货 数量
5 mg ¥4200 In-stock
10 mg ¥7000 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

LIN28 inhibitor LI71 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells[1].

IC50 & Target

IC50: 7 uM (LIN28)[1]

分子量

335.40

Formula

C21H21NO3

CAS 号

1357248-83-9

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 : 23 mg/mL (68.57 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9815 mL 14.9076 mL 29.8151 mL
5 mM 0.5963 mL 2.9815 mL 5.9630 mL
10 mM 0.2982 mL 1.4908 mL 2.9815 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。

参考文献
  • [1]. Wang L, et al. Small-Molecule Inhibitors Disrupt let-7 Oligouridylation and Release the Selective Blockade of let-7 Processing by LIN28. Cell Rep. 2018 Jun 5;23(10):3091-3101.

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

BC-LI-0186

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。

BC-LI-0186  纯度: 98.85%

BC-LI-0186 是一种有效的选择性亮氨酸 tRNA 合成酶 (Leucyl-tRNA synthetase (LRS)) 与 Ras 相关的 GTP 结合蛋白 D (RagD) 相互作用的抑制剂 (IC50=46.11 nM)。BC-LI-0186 与 LRS 的 RagD 相互作用位点 (Kd=42.1 nM) 竞争,并对 LRS- vps34、LRS- eprs、RagB-RagD 缔合、mTORC1 复合物的形成没有产生影响。BC-LI-0186 能有效抑制肿瘤相关 MTOR 突变体的活性和雷帕霉素耐药癌细胞的生长。BC-LI-0186 可用于肺癌的相关研究。

BC-LI-0186

BC-LI-0186 Chemical Structure

CAS No. : 695207-56-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ¥900 In-stock
10 mg ¥1500 In-stock
25 mg ¥3300 In-stock
50 mg ¥5200 In-stock
100 mg ¥8000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

BC-LI-0186 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Lung Cancer Compound Library

生物活性

BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research[1][2].

IC50 & Target

IC50: 46.11 nM (LeuRS and RagD interaction)[1]
Kd: 42.1 nM (LeuRS and RagD interaction)[1]

体外研究
(In Vitro)

BC-LI-0186 (0-20 μM; starved for 90 min in the leucine-free medium and then in the serum-free media for 15 min) inhibits phosphorylation of S6K in a dose- and time-dependent manner, but it has no effects on hosphorylation of AKT (S473)[1].
BC-LI-0186 (0-20 μM; 6 hours) induces cleaved poly (ADP-ribose) polymerase (PARP) and caspase-3 and an increase of p62 in A549 and H460 cells[1].
BC-LI-0186 exhibits cytotoxic effect at nanomolar concentration in NSCLC cells, it exhibits IC50 values of 98 nM, 206 nM, 55 nM, 78 nM, 83 nM, 86 nM, 102  nM, 109 nM, 128 nM, and 206 nM in A549, H460, H2228, H1703, SNU1330, H1650, H2009, H358, H2279, H460, and H596 cells, respectively[1].
BC-LI-0186 overcome acquired rapamycin resistance and inhibits the mTORC1 pathway in isogenic HCT116 cell lines that harbored either M TOR WT (HCT116 MW) or S2035I mutations (HCT116 MM), it exhibits little changed efficacy between the wild-type and mutant cells (GI50: 39.49  nM and 42.03 nM, EC50: 105.03 nM and 100.45  nM)[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.

Cell Viability Assay[1]

Cell Line: NSCLC cells
Concentration: 0 μM, 0.1 μM, 0.2 μM,1 μM, 2 μM, 5 μM, 10 μM, 20 μM
Incubation Time: Starved for 90 min in the leucine-free medium and then in the serum-free media for 15 min
Result: Suppressed leucine-mediated mTORC1 activation in NSCLC cells.

体内研究
(In Vivo)

BC-LI-0186 (intraperitoneal injection; 50 mg/kg; alone or combines with cisplatin alone; 2 weeks; bid for 5 days per week) exhibits antitumor effects and significantly reduces tumor size compared with treatment with vehicle in an LSL K-ras G12D lung cancer animal model[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.

Animal Model: K-ras mouse lung cancer modelan LSL K-ras G12D lung cancer animal model[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 50 mg/kg; alone or combines with cisplatin alone; 2 weeks; bid for 5 days per week
Result: Showed activated caspase-3-positive cells higher in the BC-LI-0186-treated group than in the vehicle or cisplatin-treated group.
Reduced p-S6 and p-AKT level whereas cisplatin alone has minimal effect on both p-S6 and p-AKT expression.
Showed a slight (not statistically significant) increase in body weight during the treatment period.
Exhibited a specific inhibition of mTORC1 and not mTORC2.

分子量

429.53

Formula

C22H27N3O4S

CAS 号

695207-56-8

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 : 125 mg/mL (291.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3281 mL 11.6406 mL 23.2813 mL
5 mM 0.4656 mL 2.3281 mL 4.6563 mL
10 mM 0.2328 mL 1.1641 mL 2.3281 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: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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% corn oil

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.84 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 20.8 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]. Jong Hyun Kim, et al. Control of leucine-dependent mTORC1 pathway through chemical intervention of leucyl-tRNA synthetase and RagD interaction. Nat Commun. 2017 Sep 29;8(1):732.

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

LIN28 inhibitor LI71 enantiomer

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。

LIN28 inhibitor LI71 enantiomer  纯度: 99.83%

LIN28 inhibitor LI71 enantiomer 是 LIN28 inhibitor LI71 的 less active 对映异构体。LIN28 inhibitor LI71 是一种有效且可渗透细胞的 LIN28 抑制剂,其消除 LIN28 介导的低聚脲化的 IC50 为 7 uM。

LIN28 inhibitor LI71 enantiomer

LIN28 inhibitor LI71 enantiomer Chemical Structure

CAS No. : 956189-58-5

规格 价格 是否有货 数量
5 mg ¥4200 In-stock
10 mg ¥7000 In-stock
50 mg ¥20000 In-stock
100 mg ¥30000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

LIN28 inhibitor LI71 enantiomer 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

LIN28 inhibitor LI71 enantiomer is the enantiomer of LIN28 inhibitor LI71 with less active. LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM[1].

IC50 & Target

LIN280[1]

分子量

335.40

Formula

C21H21NO3

CAS 号

956189-58-5

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 : 2.7 mg/mL (8.05 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 2.9815 mL 14.9076 mL 29.8151 mL
5 mM 0.5963 mL 2.9815 mL 5.9630 mL
10 mM

*

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。

参考文献
  • [1]. Wang L, et al. Small-Molecule Inhibitors Disrupt let-7 Oligouridylation and Release the Selective Blockade of let-7 Processing by LIN28. Cell Rep. 2018;23(10):3091-3101.

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

LIN28 inhibitor LI71 enantiomer

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。

LIN28 inhibitor LI71 enantiomer  纯度: 99.83%

LIN28 inhibitor LI71 enantiomer 是 LIN28 inhibitor LI71 的 less active 对映异构体。LIN28 inhibitor LI71 是一种有效且可渗透细胞的 LIN28 抑制剂,其消除 LIN28 介导的低聚脲化的 IC50 为 7 uM。

LIN28 inhibitor LI71 enantiomer

LIN28 inhibitor LI71 enantiomer Chemical Structure

CAS No. : 956189-58-5

规格 价格 是否有货 数量
5 mg ¥4200 In-stock
10 mg ¥7000 In-stock
50 mg ¥20000 In-stock
100 mg ¥30000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

LIN28 inhibitor LI71 enantiomer 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

LIN28 inhibitor LI71 enantiomer is the enantiomer of LIN28 inhibitor LI71 with less active. LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM[1].

IC50 & Target

LIN280[1]

分子量

335.40

Formula

C21H21NO3

CAS 号

956189-58-5

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 : 2.7 mg/mL (8.05 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 2.9815 mL 14.9076 mL 29.8151 mL
5 mM 0.5963 mL 2.9815 mL 5.9630 mL
10 mM

*

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。

参考文献
  • [1]. Wang L, et al. Small-Molecule Inhibitors Disrupt let-7 Oligouridylation and Release the Selective Blockade of let-7 Processing by LIN28. Cell Rep. 2018;23(10):3091-3101.

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

LIN28 inhibitor LI71 enantiomer

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。

LIN28 inhibitor LI71 enantiomer  纯度: 99.83%

LIN28 inhibitor LI71 enantiomer 是 LIN28 inhibitor LI71 的 less active 对映异构体。LIN28 inhibitor LI71 是一种有效且可渗透细胞的 LIN28 抑制剂,其消除 LIN28 介导的低聚脲化的 IC50 为 7 uM。

LIN28 inhibitor LI71 enantiomer

LIN28 inhibitor LI71 enantiomer Chemical Structure

CAS No. : 956189-58-5

规格 价格 是否有货 数量
5 mg ¥4200 In-stock
10 mg ¥7000 In-stock
50 mg ¥20000 In-stock
100 mg ¥30000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

LIN28 inhibitor LI71 enantiomer 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

LIN28 inhibitor LI71 enantiomer is the enantiomer of LIN28 inhibitor LI71 with less active. LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM[1].

IC50 & Target

LIN280[1]

分子量

335.40

Formula

C21H21NO3

CAS 号

956189-58-5

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 : 2.7 mg/mL (8.05 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 2.9815 mL 14.9076 mL 29.8151 mL
5 mM 0.5963 mL 2.9815 mL 5.9630 mL
10 mM

*

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。

参考文献
  • [1]. Wang L, et al. Small-Molecule Inhibitors Disrupt let-7 Oligouridylation and Release the Selective Blockade of let-7 Processing by LIN28. Cell Rep. 2018;23(10):3091-3101.

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

Gypenoside LI

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。

Gypenoside LI  纯度: 98.29%

Gypenoside LI 是一种绞股蓝赶单体,具有抗肿瘤活性。Gypenoside LI 诱导癌细胞凋亡、细胞周期阻滞和迁移。

Gypenoside LI

Gypenoside LI Chemical Structure

CAS No. : 94987-10-7

规格 价格 是否有货 数量
5 mg ¥4500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Gypenoside LI 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

Gypenoside LI, a gypenoside monomer, possesses anti-tumor activity. Gypenoside LI induces cell apoptosis, cell cycle and migration[1][2].

体外研究
(In Vitro)

Gypenoside LI (0-80 μM) inhibits A549 cells in a dose-dependent manner. Gypenoside LI induces G2/M and arrest apoptosis in A549 cells[1].
Gypenoside LI increases intracellular ROS level. Gypenoside LI suppressed migration of A549 cells[1].
Gypenoside LI could obviously suppress the expression of CDK1 protein rather than CDK2 and CDK4 proteins[1].
Gypenoside LI inhibits cell proliferation and upregulates expression of miR-128-3p in melanoma cells[2].
Gypenoside LI (75 and 29.71 μg/mL) can induce intrinsic apoptosis along with S phase arrest. Gypenoside LI inhibited the colony formation ability of melanoma through inhibition of the Wnt/β-catenin signaling pathway[2].
Gypenoside LI induces PARP cleavage, increased the expression of cleaved caspase-9 and BID death agonist, and downregulates the expression of FLIP (long form) and BCl-2 in the A375 and SK-MEL-28 melanoma cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A549 cells.
Concentration: 0-80 μM.
Incubation Time: 24 h.
Result: Displayed the strongest activity with the IC50 values of 21.36 ± 0.78 μM.

分子量

801.01

Formula

C42H72O14

CAS 号

94987-10-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

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

参考文献
  • [1]. Shao-Fang Xing, et al. The inhibitory effect of gypenoside stereoisomers, gypenoside L and gypenoside LI, isolated from Gynostemma pentaphyllum on the growth of human lung cancer A549 cells. J Ethnopharmacol. 2018 Jun 12;219:161-172.

    [2]. Ma-Li Zu, et al. Monomer gypenoside LI from Gynostemma pentaphyllum inhibits cell proliferation and upregulates expression of miR-128-3p in melanoma cells. J Biochem Mol Toxicol. 2020 May;34(5):e22460.

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