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Purity: ≥98%
Sal003 is a potent, selective and cell-permeable eIF-2α phosphatase inhibitor. Sal003 increases eIF2α phosphorylation status by blocking eIF2a phosphatases in cells. In mouse embryonic fibroblasts (MEFs), Sal003 causes dissociation of polysomes by increasing eIF2a phosphorylation. Sal003 impairs late-long-term potentiation (L-LTP) in an ATF4-dependent mode in hippocampal slices from WT mice. In addition, eIF2α phosphorylation by Sal003 also enhances apoptotic signaling induced by subtilase cytotoxin (SubAB).
| ln Vitro |
Mouse embryonic fibroblasts (MEFs) exhibit a considerable increase in eIF2α phosphorylation upon exposure to Sal003 (20 μM; 1-12 hours) [2]. Sal003 (10 μM; 1 hour) stimulates subtilisin (SubAB)-induced apoptotic signaling, and this is enhanced by eukaryotic translation initiation factor 2α (eIF2α) [1]. Sal003 phosphorylates eIF2α, which impairs memory and synaptic plasticity [1].
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| ln Vivo |
Contextual memory is impaired in vivo by Sal003 (20 μM; intrahippocampal injection; 8 min) [1].
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| Cell Assay |
Apoptosis Analysis[2]
Cell Types: HeLa cells Tested Concentrations: 10 μM Incubation Duration: 1 hour Experimental Results: Phosphorylated eIF2α and thus enhanced SubAB-induced apoptotic signaling. Western Blot Analysis[1] Cell Types: Mouse embryonic fibroblasts (MEFs) Tested Concentrations: 20 μM Incubation Duration: 1 hour, 3 hrs (hours), 6 hrs (hours), 12 hrs (hours) Experimental Results: Sharply increased eIF2α phosphorylation in mouse MEFs. |
| Animal Protocol |
Animal/Disease Models: Rats (300-325g)[1]
Doses: 20 μM Route of Administration: Intrahippocampal injection; 8 minutes Experimental Results: Impaired contextual memory. |
| References |
[1]. Costa-Mattioli M, et al. eIF2alpha phosphorylation bidirectionally regulates the switch from short- to long-term synaptic plasticity and memory. Cell. 2007 Apr 6;129(1):195-206.
[2]. Yahiro K, et al. Regulation of subtilase cytotoxin-induced cell death by an RNA-dependent protein kinase-like endoplasmic reticulum kinase-dependent proteasome pathway in HeLa cells. Infect Immun. 2012 May;80(5):1803-14. |
| Molecular Formula |
C18H15CL4N3OS
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| Molecular Weight |
463.21
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| Exact Mass |
460.97
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| Elemental Analysis |
C, 46.68; H, 3.26; Cl, 30.61; N, 9.07; O, 3.45; S, 6.92
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| CAS # |
1164470-53-4
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
ClC(C([H])(N([H])C(/C(/[H])=C(\[H])/C1C([H])=C([H])C([H])=C([H])C=1[H])=O)N([H])C(N([H])C1C([H])=C([H])C(=C([H])C=1[H])Cl)=S)(Cl)Cl
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| InChi Key |
TVNBASWNLOIQML-IZZDOVSWSA-N
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| InChi Code |
InChI=1S/C18H15Cl4N3OS/c19-13-7-9-14(10-8-13)23-17(27)25-16(18(20,21)22)24-15(26)11-6-12-4-2-1-3-5-12/h1-11,16H,(H,24,26)(H2,23,25,27)/b11-6+
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| Chemical Name |
3--Phenyl-N-(2,2,2-trichloro-1-((((4-chlorophenyl)amino)carbonothioyl)amino)ethyl)acrylamide
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| Synonyms |
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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 (5.40 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1588 mL | 10.7942 mL | 21.5885 mL | |
| 5 mM | 0.4318 mL | 2.1588 mL | 4.3177 mL | |
| 10 mM | 0.2159 mL | 1.0794 mL | 2.1588 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.
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