| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
| Targets |
MEK1 (IC50 = 0.18 μM); MEK2 (IC50 = 0.22 μM); AP-1 (IC50 = 2.03 μM)
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|---|---|
| ln Vitro |
SL327 is a structural homologue of the specific MKK1/2 inhibitor U0126 with IC50 of 0.18 μM and 0.22 μM for MEK1 and MEK2 respectively. Other kinases such as PKA, PKC, or CamKII are unaffected by SL327. [1]
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| ln Vivo |
SL327 (50 mg/kg) crosses the blood-brain barrierand and blocks fear conditioning by inhibiting MAPK/ERK phosphorylation. [2] SL327 (30 mg/kg) significantly reduces spatial learning in mice. [3] SL327 (50 mg/kg) inhibits the effects of cocaine. [4]
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| Enzyme Assay |
Assays for protein kinases are carried out. In the beginning of each kinase assay, enzyme is added to a mixture of substrate and [γ-32P]ATP. Then, this mixture is incubated for 10 minutes at 30 or 37 degrees Celsius. By aliquoting the reaction mixture and sprinkling it on Whatman P-81 phosphocellulose filter paper, the reaction can be stopped. The papers are then dried, scintillation counted, and washed in 150 mM H3PO4. By monitoring [32P]phosphate incorporation into the substrate Kemptide (100 μM), the catalytic subunit of PKA is evaluated. The phosphorylation of the synthetic peptide Autocamtide (100 M) in the presence of 100 M Calcium and 10 μg/mL Calmodulin is used to measure the activity of CaMKII. The catalytic subunit of PKC has a preferred substrate in the form of NG(28-43) (10 μM), a synthetic peptide analog of a neurogranin fragment. Substrate phosphorylation was always a linear function of both time and enzyme concentration.
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| Animal Protocol |
Fear conditioning experiments in male Spague-Dawley rats.
10-100 mg/Kg i.p. |
| References | |
| Additional Infomation |
SL-327 is a nitrile that is acrylonitrile in which the hydrogen attached to the same carbon as the cyano group has been replaced by an o-(trifluoromethyl)phenyl group, while the remaining hydrogens of the ethenyl group have been replaced by amino and (4-aminophenyl)sulfanyl groups. The configuration of the double bond is not specified. It is an inhibitor of MEK1 and MEK2. It has a role as an EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor and a neuroprotective agent. It is a member of (trifluoromethyl)benzenes, a nitrile, an enamine, an organic sulfide, a substituted aniline and a primary amino compound.
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| Molecular Formula |
C16H12F3N3S
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|---|---|---|
| Molecular Weight |
335.35
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| Exact Mass |
335.07
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| Elemental Analysis |
C, 57.31; H, 3.61; F, 17.00; N, 12.53; S, 9.56
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| CAS # |
305350-87-2
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| Related CAS # |
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| PubChem CID |
9549284
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| Appearance |
white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
512.6±50.0 °C at 760 mmHg
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| Melting Point |
127-128.2ºC
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| Flash Point |
263.8±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.631
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| LogP |
1.95
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
487
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(F)(F)C1=C(/C(C#N)=C(N)/SC2=CC=C(N)C=C2)C=CC=C1
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| InChi Key |
JLOXTZFYJNCPIS-FYWRMAATSA-N
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| InChi Code |
InChI=1S/C16H12F3N3S/c17-16(18,19)14-4-2-1-3-12(14)13(9-20)15(22)23-11-7-5-10(21)6-8-11/h1-8H,21-22H2/b15-13+
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| Chemical Name |
(Z)-3-amino-3-(4-aminophenyl)sulfanyl-2-[2-(trifluoromethyl)phenyl]prop-2-enenitrile
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| Synonyms |
SL 327; SL-327; SL327
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9820 mL | 14.9098 mL | 29.8196 mL | |
| 5 mM | 0.5964 mL | 2.9820 mL | 5.9639 mL | |
| 10 mM | 0.2982 mL | 1.4910 mL | 2.9820 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Brain Res Bull.2016 Jun;124:40-7. |
Brain Res Bull.2016 Jun;124:40-7. |
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