SL-327 |
Catalog No.GC15359
One-Click Copy Product Info
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SL-327은 MEK1과 MEK2의 선택적 억제제로 IC50 값은 각각 0.18μM과 0.22μM이다.
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Cas No.: 305350-87-2
Sample solution is provided at 25 µL, 10mM.
SL-327은 MEK1과 MEK2의 선택적 억제제로 IC50 값은 각각 0.18μM과 0.22μM이다. SL-327은 뇌전증 쥐의 발작 간기 첨파 및 행동에서 MAPK 신호 전달 경로의 역할을 연구하기 위해 사용될 수 있다[2]. SL-327은 혈액-뇌 장벽을 관통해서 허혈성 뇌 손상 쥐에서 신경 보호 효과를 나타낼 수 있다[3].
체외 실험에서 SL-327(1.25µM)으로 흑색종 세포(MV3 및 A375 세포)를 48시간 처리하면 TBMS1 처리에 의해 억제된 세포 성장 곡선을 회복시키고 TBMS1에 의해 억제된 세포 집락 형성 능력을 회복시키고 TBMS1에 의해 유도된 LC3B-II 및 p62의 높은 발현 수준을 역전시켰다[4].
체내 실험에서 수컷 스위스 백색 CD1 중년 쥐에게 복강 내 주사로 SL-327(20mg/kg)을 투여하면 방사형 팔 미로 테스트에서 성장 호르몬(GH)이 쥐에 미치는 긍정적 효과를 차단하였다[5]. 스위스 쥐에게 복강 내 주사로 SL-327(1, 5mg/kg)을 투여한 후 행동학적 테스트를 실시하면 쥐에서 항불안 행동을 유도하였고 고가 십자 미로(EPM) 테스트에서 디아제팜과 병용할 때 항불안 특성이 특히 현저하였다[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.
| 동물 실험 [1]: | |
동물 모형 | 수컷 스위스 백색 CD1 중년 쥐 |
제조 방법 | 수컷 스위스 백색 CD1 중년 쥐를 사용하였습니다. 쥐 그룹은 작업 기억 테스트 1시간 전에 생리 식염수와 성장 호르몬(GH)(1mg/kg 복강 내)으로 처리하였습니다. 다른 쥐 그룹은 GH 투여 30분 전에 MEK 억제제 SL-327(20mg/kg, 디메틸설폭시드에 용해, 복강 내)을 주사해서 단독 GH 처리 쥐의 효과와 비교하였습니다. |
제형 | 20mg/kg; i.p. |
응용 분야 | GH로 처리한 쥐는 방사형 팔 미로 테스트에서 오류 횟수(미방문 팔 또는 재방문 팔) 감소를 보였습니다. 그런데 GH 투여 30분 전에 MEK 억제제 SL-327을 복강 내 주사하면 방사형 팔 미로 테스트에서 GH의 긍정적 효과를 차단하였습니다. |
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 |
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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.
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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.)