SL-327 |
Catalog No.GC15359
One-Click Copy Product Info
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SL-327 inhibe MEK1 y MEK2, con valores IC50 de 180 nM y 220 nM, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 305350-87-2
Sample solution is provided at 25 µL, 10mM.
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.
| 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 | |
| Chemical Name | (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 | ||
| Formula | C16H12F3N3S | M.Wt | 335.35 |
| Solubility | ≥ 16.75mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)