BMS-5(Synonyms: LIMKi 3)

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。

BMS-5 (Synonyms: LIMKi 3) 纯度: 99.35%

BMS-5 (LIMKi 3) 是一种高效的 LIMK 抑制剂,抑制 LIMK1LIMK2IC50 分别为 7 nM 和 8 nM。

BMS-5(Synonyms: LIMKi 3)

BMS-5 Chemical Structure

CAS No. : 1338247-35-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥759 In-stock
5 mg ¥800 In-stock
10 mg ¥1200 In-stock
25 mg ¥1700 In-stock
50 mg ¥3200 In-stock
100 mg ¥6100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

BMS-5 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Targeted Diversity Library

生物活性

BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.

IC50 & Target[1]

LIMK1

7 nM (IC50)

LIMK2

8 nM (IC50)

体外研究
(In Vitro)

BMS-5 (LIMKi 3) inhibits cofilin-Ser3 phosphorylation in a dose-dependent manner in Nf2ΔEx2 mouse Schwann cells (MSCs) with an IC50 of ~2 µM. BMS-5 (LIMKi 3) reduces Nf2ΔEx2 MSC viability in a dose-dependent manner with an IC50 of 3.9 µM, but does not significantly reduce the viability of control Nf2flox2/flox2 MSCs at equivalent BMS-5 concentrations. At 10 µM BMS-5, Nf2ΔEx2 MSC viability is 40% compared to 83% for controls[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)

BMS-5 (LIMKi 3) (20 or 200 μM/side) is bilaterally infused into the hippocampus of rats immediately after contextual fear conditioning training. Rats are tested for memory consolidation 48 h after fear conditioning. Post hoc analysis shows that the group treated with 200 μM BMS-5 express lower freezing levels compared to the 20 μM and vehicle groups (P<0.01)[3].

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

431.29

Formula

C17H14Cl2F2N4OS

CAS 号

1338247-35-0

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 : ≥ 34 mg/mL (78.83 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 2.3186 mL 11.5931 mL 23.1863 mL
5 mM 0.4637 mL 2.3186 mL 4.6373 mL
10 mM 0.2319 mL 1.1593 mL 2.3186 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 (4.82 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.82 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.82 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 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.82 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]. Ross-Macdonald P, et al. Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors. Mol Cancer Ther. 2008 Nov;7(11):3490-8.

    [2]. Petrilli A, et al. LIM Domain Kinases as Potential Therapeutic Targets for Neurofibromatosis Type 2.Oncogene. Oncogene. 2014 Jul 3;33(27):3571-82.

    [3]. Lunardi P, et al. Effects of Hippocampal LIMK Inhibition on Memory Acquisition, Consolidation, Retrieval, Reconsolidation, and Extinction. Mol Neurobiol. 2017 Jan 13.

Kinase Assay
[1]

The protein kinase domains of human LIMK1 and LIMK2 are expressed as glutathione S-transferase fusion proteins using the Bac-to-Bac system in Sf9 cells. Compounds 1 to 6 (e.g., BMS-5) are assayed for inhibition of LIMK1 and LIMK2 protein kinase activity by radioactive phosphate incorporation into biotinylated full-length human destrin. Reactions are done with a concentration series of compound in 25 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 5 mM MnCl2, 1 μM total ATP, 83 μg/mL biotinylated destrin, 167 ng/mL glutathione S-transferase-LIMK1, or 835 ng/mL glutathione S-transferase-LIMK2 in a total volume of 60 μL at room temperature for 30 min (LIMK1) or 60 min (LIMK2). Reactions are terminated by addition of 140 μL of 20% TCA/100 mM sodium pyrophosphate, and the precipitates are harvested onto GF/C unifilter plates. The radioactivity incorporated is determined using a TopCount after addition of 35 μL Microscint scintillation fluid[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 Assay
[2]

Cell membrane asymmetry is measured. Nf2ΔEx2 MSCs plated in a 6-well format are incubated with 2 µM BMS-5 or DMSO vehicle for 24 hrs. Cell are harvested and assayed. Plasma membrane asymmetry is evaluated with the Violet ratiometric assay by flow cytometry[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.

Animal Administration
[3]

Rats [3]
Male Wistar rats (age 2-3 months, weight 290-350 g) are used. BMS-5 is prepared in a vehicle solution (1% DMSO in sterile isotonic saline). At the time of infusion, a 30-gauge infusion needle is fitted into a guide cannula, with its tip protruding 1.0 mm beyond the guide cannula end and aimed at the pyramidal cell layer of CA1 of the dorsal hippocampus. Avolume of 1 μL of BMS-5 (20 and 200 μM) or vehicle (DMSO 1%) is bilaterally infused in a time of 90 s. The doses of BMS-5 are based on its IC50 value and in vitro studies.

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]. Ross-Macdonald P, et al. Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors. Mol Cancer Ther. 2008 Nov;7(11):3490-8.

    [2]. Petrilli A, et al. LIM Domain Kinases as Potential Therapeutic Targets for Neurofibromatosis Type 2.Oncogene. Oncogene. 2014 Jul 3;33(27):3571-82.

    [3]. Lunardi P, et al. Effects of Hippocampal LIMK Inhibition on Memory Acquisition, Consolidation, Retrieval, Reconsolidation, and Extinction. Mol Neurobiol. 2017 Jan 13.

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

T56-LIMKi(Synonyms: T5601640)

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。

T56-LIMKi (Synonyms: T5601640) 纯度: 98.91%

T56-LIMKi是选择性的LIMK2抑制剂。抑制Panc-1细胞生长的IC50值为35.2 μM。

T56-LIMKi(Synonyms: T5601640)

T56-LIMKi Chemical Structure

CAS No. : 924473-59-6

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 ¥869 In-stock
5 mg ¥790 In-stock
10 mg ¥1370 In-stock
25 mg ¥2800 In-stock
50 mg ¥4800 In-stock
100 mg ¥8100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

T56-LIMKi 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Targeted Diversity Library

生物活性

T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.

IC50 & Target[1]

LIMK2

 

体外研究
(In Vitro)

T56-LIMKi efficiently inhibits the growth of ST88-14, U87, Panc-1 cells, A549 lung cancer cells with IC50 values of 18.3, 7.4, 35.2 and 90 μM, respectively. T56-LIMKi decreases phosphorylated cofilin (p-cofilin) levels and thus inhibits growth of several cancerous cell lines, including those of pancreatic cancer, glioma and schwannoma[1]. It blocks the phosphorylation of cofilin which leads to actin severance and inhibition of tumor cell migration, tumor cell growth, and anchorage-independent colony formation in soft agar. T56-LIMKi (10-50 μM) reduces p-cofilin in a dose-dependent manner in NF1−/−MEFs with an IC50 of 30 μM. Notably, the inhibitor does not affect the amounts of total cofil. 50μM T56-LIMKi causes a statistically significant reduction in the number of cells exhibiting stress fibers[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)

T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control[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

389.33

Formula

C19H14F3N3O3

CAS 号

924473-59-6

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 : ≥ 36 mg/mL (92.47 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 2.5685 mL 12.8426 mL 25.6852 mL
5 mM 0.5137 mL 2.5685 mL 5.1370 mL
10 mM 0.2569 mL 1.2843 mL 2.5685 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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.42 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]. Rak R, et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. eCollection 2014.

    [2]. Mashiach-Farkash E, et al. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39.

Cell Assay

T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control[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 Administration
[1]

Mice: T56-LIMKi is dissolved in 0.5% carboxymethylcellulose solution. Mice are implanted with xenografted Panc-1 cells. Treatment is started 7 days later. Mice in the two experimental groups are each treated with a daily oral non-toxic dose of T56-LIMKi (30 or 60 mg/kg in gavage) and mice in the control group receives only the vehicle (0.5% CMC) in the gavage[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.

参考文献
  • [1]. Rak R, et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. eCollection 2014.

    [2]. Mashiach-Farkash E, et al. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39.

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