标签归档：cmld

CMLD012612

发表于由

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。

CMLD012612 

CMLD012612 是一类含有异羟肟酸酯基团的 amidino-rocaglate，并且是有效的真核生物起始因子 4A (eIF4A) 抑制剂。CMLD012612 抑制细胞翻译，对 NIH/3T3 细胞具有细胞毒性，IC50 值为 2 nM。CMLD012612 通过修饰RNA解旋酶 eIF4A 来抑制真核细胞翻译起始，并具有有效的抗肿瘤活性。

CMLD012612

CMLD012612 Chemical Structure

CAS No. : 2368900-35-8

规格 价格 是否有货
1 mg ￥16500 询问价格 & 货期
5 mg ￥36000 询问价格 & 货期

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生物活性

CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity[1].

IC50 & Target

eIF4A[1]
体外研究
(In Vitro)

The IC50 of CMLD012612 toward NIH/3T3 cells is 2 nM. The primary mechanism of action of CMLD012612 is dependent on eIF4A1, since eIF4A1em1jp cells are at least 10-fold more resistant than parental NIH/3T3 cells. The sensitivity of eIF4A1em1jp cells to CMLD012612 observed at higher concentrations may be due to the presence of wild-type eIF4A2 in the cells[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.
体内研究
(In Vivo)

CMLD012612 (0.5 mg/kg; intraperitoneal injection; for 3 hours; female C57BL/6 mice) treatment effectively suppresses liver polysomes 3 hours after injection, indicating inhibitory activity toward protein synthesis[1].
When administered to mice bearing myr-Akt/Em-Myc lymphomas, CMLD012612 (0.2 mg/kg; intraperitoneal injection; daily; for 5 days; female C57BL/6 mice) treatment effectively synergizes with Doxorubicin, leading to complete tumor loss[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: Female C57BL/6 mice[1]
Dosage: 0.5 mg/kg
Administration: Intraperitoneal injection; for 3 hours
Result: Effectively suppressed liver polysomes 3 hours after injection.

分子量

559.61

Formula

C31H33N3O7
CAS 号

2368900-35-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chu J, et al. Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors. Cell Chem Biol. 2019 Nov 21;26(11):1586-1593.

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CMLD-2

发表于由

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。

CMLD-2  纯度: 98.22%

CMLD-2 是一种 HuR-ARE 相互作用 的抑制剂。CMLD-2 竞争性结合 HuR 蛋白，破坏其与富含腺嘌呤-尿苷元素 (ARE) 的 mRNA 靶标的相互作用 (Ki=350 nM)。CMLD-2 可诱导凋亡并在结肠癌，胰腺癌，甲状腺癌和肺癌细胞系中表现出抗肿瘤活性。Hu 抗原 R (HuR) 是一种 RNA 结合蛋白，可以调节靶标 mRNA 的稳定性和翻译。

CMLD-2

CMLD-2 Chemical Structure

CAS No. : 958843-91-9

规格 价格 是否有货 数量
5 mg ￥3000 In-stock
10 mg ￥5000 In-stock
50 mg   询价  
100 mg   询价  

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CMLD-2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Anti-Lung Cancer Compound Library

生物活性

CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation[1][2].

IC50 & Target

HuR[1]
体外研究
(In Vitro)

CMLD-2 (1-75 μM; 24-72 h) inhibits thyroid cancer cell viability[2].
CMLD-2 (20-30 μM; 24-48 h) activates caspases and induces apoptotic cell death in H1299 and A549 cells[3].
CMLD-2 (30 μM; 24-48 h) induces G1 cell cycle arrest and mitochondrial perturbation in H1299 and A549 cell[3].
CMLD-2 (30 μM; 24-48 h) reduces expression of HuR and HuR-regulated mRNAs and proteins in H1299 cells[3].
CMLD-2 (35 μM; 72 h) decreases directional migration capability in SW1736, 8505C, BCPAP and K1 cells. CMLD-2 induces a strong decrease of MAD2 mRNA levels in SW1736, 8505C, BCPAP and K1 cells[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.

Cell Viability Assay[2]

Cell Line: SW1736, 8505C, BCPAP and K1 cells
Concentration: 1, 5, 10, 25, 35, 50, 75 μM
Incubation Time: 24, 48, 72 hours
Result: Reduced the viability of all the four cell lines when used at 35, 50 and 75 μM concentration and at different time points.

Apoptosis Analysis[3]

Cell Line: H1299, A549, H1975, HCC827, MRC-9 and CCD16 cells
Concentration: 20, 30 μM
Incubation Time: 24, 48 hours
Result: Marked activated the caspase-9 and -3 in lung tumor cells.
Induce the cleavage of PARP in lung tumor cells.
Significantly increased the annexin-V-positive staining in lung tumor cells.

Cell Cycle Analysis[3]

Cell Line: H1299, A549, MRC-9 and CCD16 cells
Concentration: 30 μM
Incubation Time: 24, 48 hours
Result: Induced greater G1 phase cell cycle arrest in H1299 and A549 cells than in MRC-9 and CCD16 cells.

Western Blot Analysis[3]

Cell Line: H1299, A549, H1975, HCC827, CCD16 and MRC-9 cells
Concentration: 20, 30 μM
Incubation Time: 24, 48 hours
Result: Diminished protein expression of HuR, Bcl-2, Cyclin E and Bcl-XL and increased expression of p27 and BAX in lung tumor cells.

分子量

513.58

Formula

C31H31NO6
CAS 号

958843-91-9
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 : 50 mg/mL (97.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9471 mL 9.7356 mL 19.4712 mL
5 mM 0.3894 mL 1.9471 mL 3.8942 mL
10 mM 0.1947 mL 0.9736 mL 1.9471 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 (4.87 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.87 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 (4.87 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.87 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 (4.87 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.87 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]. Wu X, et, al. Identification and validation of novel small molecule disruptors of HuR-mRNA interaction. ACS Chem Biol. 2015 Jun 19;10(6):1476-84.

    [2]. Allegri , et, al. The HuR CMLD-2 inhibitor exhibits antitumor effects via MAD2 downregulation in thyroid cancer cells. Sci Rep. 2019 May 14;9(1):7374.

    [3]. Muralidharan R, et, al. HuR-targeted small molecule inhibitor exhibits cytotoxicity towards human lung cancer cells. Sci Rep. 2017 Aug 30;7(1):9694.

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CMLD010509(Synonyms: SDS-1-021)

发表于由

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。

CMLD010509 (Synonyms: SDS-1-021)

CMLD010509 (SDS-1-021) 是支持多发性骨髓瘤 (MM) 致癌翻译程序 (oncogenic translation program) 的高度特异性抑制剂，包括关键癌蛋白，例如 MYC，MDM2，CCND1，MAF 和 MCL-1。CMLD010509 (SDS-1-021) 对大多数 MM 细胞系的 IC50 低于 10 nM，并诱导凋亡。CMLD010509 (SDS-1-021) 是一种有效且选择性的翻译抑制剂，通过 eIF4E 磷酸化独立机制发挥作用。

CMLD010509(Synonyms: SDS-1-021)

CMLD010509 Chemical Structure

CAS No. : 256497-58-2

规格 是否有货
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生物活性

CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism[1].

分子量

556.40

Formula

C27H26BrNO7
CAS 号

256497-58-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Manier S, et al. Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma. Sci Transl Med. 2017 May 10;9(389). pii: eaal2668.

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CMLD012072

发表于由

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。

CMLD012072 

CMLD012072 是一种 amidino-rocaglates，是一种有效的真核起始因子 4A (eIF4A) 抑制剂。CMLD012072 可以诱导 eIF4A1 和 eIF4A2 的 RNA 钳位，并具有有效的抗肿瘤活性。

CMLD012072

CMLD012072 Chemical Structure

CAS No. : 2368900-33-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

CMLD012072 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012072 can induce RNA clamping of eIF4A1 and eIF4A2 and possess potent anti-neoplastic activity[1].

IC50 & Target

eIF4A[1]
分子量

556.61

Formula

C32H32N2O7
CAS 号

2368900-33-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chu J, et al. Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors. Cell Chem Biol. 2019 Nov 21;26(11):1586-1593.

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

CMLD012073

发表于由

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。

CMLD012073 

CMLD012073 是一种 amidino-rocaglates，是一种有效的真核起始因子 4A (eIF4A) 抑制剂。CMLD012073 抑制 NIH/3T3 细胞生长，IC50 值为 10 nM。CMLD012073 通过修饰 RNA 解旋酶 eIF4A 来抑制真核细胞翻译起始。

CMLD012073

CMLD012073 Chemical Structure

CAS No. : 2368900-32-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

CMLD012073 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012073 inhibits the growth of NIH/3T3 cells with an IC50 of 10 nM. CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A)[1].

IC50 & Target

eIF4A[1]
体外研究
(In Vitro)

In in vitro translation assays, CMLD012073 is potent at inhibiting cap-dependent translation (FF). In ribosome recruitment experiments, CMLD012073 inhibits assembly of the 80S ribosome on the mRNA[1].

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

530.57

Formula

C30H30N2O7
CAS 号

2368900-32-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chu J, et al. Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors. Cell Chem Biol. 2019 Nov 21;26(11):1586-1593.

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