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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
BMS-5
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1338247-35-0
- 规格：
50mg/25mg/10mg/1mg/5mg
| 规格： | 50mg | 产品价格： | ￥3190.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥1690.0 |
| 规格： | 10mg | 产品价格： | ￥1190.0 |
| 规格： | 1mg | 产品价格： | ￥367.0 |
| 规格： | 5mg | 产品价格： | ￥790.0 |
| 基本信息 | |
| CAS | No.1338247-35-0 |
| 英文名称 | BMS-5 |
| 别名 | LIMKi3 |
| 分子式 | C17H14Cl2F2N4OS |
| 分子量 | 431.29 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD17019327 |
| SMILES | CC(C)C(=O)NC1=NC=C(S1)C2=CC(=NN2C3=C(C=CC=C3Cl)Cl)C(F)F |
| InChIKey | IVUGBSGLHRJSSP-UHFFFAOYSA-N |
| InChI | InChI=1S/C17H14Cl2F2N4OS/c1-8(2)16(26)23-17-22-7-13(27-17)12-6-11(15(20)21)24-25(12)14-9(18)4-3-5-10(14)19/h3-8，15H，1-2H3，(H，22，23，26) |
| PubChem CID | 56965901 |
| 靶点 | LIM Kinase (LIMK) |
| 通路 | Cytoskeleton |
| 背景说明 | BMS-5是一种高效的 LIMK 抑制剂，抑制 LIMK1 和 LIMK2。 |
| 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.[1-3] |
| 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] |
| 细胞实验 | 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[3]. |
| 细胞实验 | 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]. |
| 动物实验 | 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. |
| 激酶实验 | 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]. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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