SL-327
目录号 : GC15359
SL-327是MEK1和MEK2的选择性抑制剂，IC50值分别为0.18μM和0.22μM。
Cas No.:305350-87-2
Sample solution is provided at 25 µL, 10mM.
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SL-327 is a selective inhibitor of MEK1 and MEK2, with IC50 values of 0.18μM and 0.22μM, respectively[1]. SL-327 can be used to study the role of the MAPK signaling pathway in interictal spikes and behavior in epileptic rats[2]. SL-327 can penetrate the blood-brain barrier and produce neuroprotective effects in mice with ischemic brain injury[3].
In vitro, treatment of melanoma cells (MV3 and A375 cells) with SL-327 (1.25µM) for 48h restored the cell growth curve inhibited by TBMS1 treatment, restored the cell colony formation ability inhibited by TBMS1, and reversed the high expression levels of LC3B-II and p62 induced by TBMS1[4].
In vivo, SL-327 (20mg/kg) administered by intraperitoneal injection to male Swiss albino CD1 middle-aged mice blocked the positive effects of growth hormone (GH) on the mice in the radial arm maze test[5]. SL-327 (1, 5mg/kg) administered by intraperitoneal injection to Swiss mice followed by behavioral testing induced anxiolytic behavior in the mice, and the anxiolytic properties were particularly significant in combination with diazepam in the elevated plus maze (EPM) test[6].
References:
[1] Moranta D, Esteban S, García‐Sevilla J A. Acute, chronic and withdrawal effects of the cannabinoid receptor agonist WIN55212‐2 on the sequential activation of MAPK/Raf‐MEK‐ERK signaling in the rat cerebral frontal cortex: short‐term regulation by intrinsic and extrinsic pathways[J]. Journal of neuroscience research, 2007, 85(3): 656-667.
[2] Glazova M V, Nikitina L S, Hudik K A, et al. Inhibition of ERK 1/2 signaling prevents epileptiform behavior in rats prone to audiogenic seizures[J]. Journal of neurochemistry, 2015, 132(2): 218-229.
[3] Wang X, Wang H, Xu L, et al. Significant neuroprotection against ischemic brain injury by inhibition of the MEK1 protein kinase in mice: exploration of potential mechanism associated with apoptosis[J]. The Journal of pharmacology and experimental therapeutics, 2003, 304(1): 172-178.
[4] Du J, Dong Z, Tan L, et al. Tubeimoside I inhibits cell proliferation and induces a partly disrupted and cytoprotective autophagy through rapidly hyperactivation of MEK1/2-ERK1/2 cascade via promoting PTP1B in melanoma[J]. Frontiers in cell and developmental biology, 2020, 8: 607757.
[5] Ramis M, Sarubbo F, Sola J, et al. Cognitive improvement by acute growth hormone is mediated by NMDA and AMPA receptors and MEK pathway[J]. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2013, 45: 11-20.
[6] Michalak A, Wnorowski A, Berardinelli A, et al. Diazepam and SL-327 synergistically attenuate anxiety-like behaviours in mice–Possible hippocampal MAPKs specificity[J]. Neuropharmacology, 2020, 180: 108302.
SL-327是MEK1和MEK2的选择性抑制剂，IC50值分别为0.18μM和0.22μM[1]。SL-327能够用于研究MAPK信号通路在癫痫大鼠发作间期棘波和行为中的作用[2]。SL-327能够穿透血脑屏障，在缺血性脑损伤小鼠中产生神经保护作用[3]。
在体外，SL-327（1.25µM）处理黑色素瘤细胞（MV3和A375细胞）48h，恢复了被TBMS1处理抑制的细胞生长曲线，恢复了被TBMS1抑制的细胞克隆形成能力，逆转了TBMS1诱导的LC3B-II和p62的高表达水平[4]。
在体内，SL-327（20mg/kg）通过腹腔注射处理雄性瑞士白化CD1中年小鼠，阻断了生长激素（GH）对小鼠在放射状迷宫测试中的积极作用[5]。SL-327（1, 5mg/kg）通过腹腔注射处理Swiss小鼠随后进行行为学测试，诱导了小鼠的抗焦虑行为，且与地西泮联合使用的抗焦虑特性在高架十字迷宫（EPM）测试中尤为显著[6]。
| Animal experiment [1]: | |
Animal models | Male Swiss albino CD1 middle-age mice |
Preparation Method | Male Swiss albino CD1 middle-age mice were used. Groups of mice were treated with saline and Growth hormone (GH) (1mg/kg i.p.) 1h before the working memory tests. A different group of mice was injected with the MEK inhibitor SL-327 (20mg/kg dissolved in dimethyl sulfoxide, i.p.) 30min before the administration of GH to compare with the effect of GH alone in mice. |
Dosage form | 20mg/kg; i.p. |
Applications | Mice treated with GH showed a reduction in the number of errors (unvisited arms or re-visited arms) in the radial arm maze test. However, intraperitoneal injection of the MEK inhibitor SL-327 30min before GH administration blocked the positive effects of GH on the radial arm maze test. |
References: | |
| Cas No. | 305350-87-2 | SDF | |
| 化学名 | (Z)-3-amino-3-(4-aminophenyl)sulfanyl-2-[2-(trifluoromethyl)phenyl]prop-2-enenitrile | ||
| Canonical SMILES | C1=CC=C(C(=C1)C(=C(N)SC2=CC=C(C=C2)N)C#N)C(F)(F)F | ||
| 分子式 | C16H12F3N3S | 分子量 | 335.35 |
| 溶解度 | ≥ 16.75mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.982 mL | 14.9098 mL | 29.8196 mL |
| 5 mM | 596.4 μL | 2.982 mL | 5.9639 mL |
| 10 mM | 298.2 μL | 1.491 mL | 2.982 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet