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Purity: ≥98%
SW-100 (SW100), a tetrahydroquinoline-based compound, is a novel, potent, brain penetrant and selective histone deacetylase 6 (HDAC6) inhibitor (IC50 = 2.3 nM) with neuroprotective effects.HDAC6 exhibits selectivity that is at least 1000 times greater than that of all other HDAC isozymes. The ability of SW-100 to cross the blood-brain barrier is noticeably better. Since there are currently no effective treatments or cures for fragile X syndrome (FXS), disease-modifying therapies are required. SW-100 can enhance memory function in an FXS mouse model using Fmr1-/-mice. This tiny molecule exhibits at least a thousand-fold selectivity over all other class I, II, and IV HDAC isoforms, good brain penetration, and low-nanomolar potency for the inhibition of HDAC6 (IC50 = 2.3 nM). Furthermore, SW-100 selectively restores the reduced levels of acetylated α-tubulin in the hippocampus of Fmr1-/- mice by inhibiting the α-tubulin deacetylase domain of HDAC6 (CD2), which in turn increases α-tubulin acetylation in cells without affecting histone acetylation. Finally, by improving a number of memory and learning deficits in Fmr1-/-mice, SW-100 models the intellectual deficiencies linked to FXS, which is compelling evidence to support the development of HDAC6-based treatments for this uncommon illness.
| Targets |
HDAC1 (IC50 = 5.23 μM); HDAC2 (IC50 = 32.8 μM); HDAC3 (IC50 = 29.5 μM); HDAC4 (IC50 = 10.9 μM); HDAC5 (IC50 = 4.07 μM); HDAC6 (IC50 = 2.3 nM); HDAC7 (IC50 = 4.55 μM); HDAC8 (IC50 = 3.72 μM); HDAC9 (IC50 = 3.46 μM); HDAC10 (IC50 = 26.2 μM); HDAC11 (IC50 = 5.72 μM)
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| ln Vitro |
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| ln Vivo |
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| Cell Assay |
Cell Line: HEK293 cells
Concentration: 0.01, 0.1, 1, 10 µM Incubation Time: 48 hours Result: Showed obvious increase in the acetylated α-tubulin levels in a dose-dependent manner. |
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| Animal Protocol |
8-10 weeks old C57BL/6 mice (Fmr1-/- mice)[1]
20 mg/kg Intraperitoneal injection; twice a day for two days |
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| References |
| Molecular Formula |
C17H17CLN2O2
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|---|---|
| Molecular Weight |
316.782083272934
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| Exact Mass |
316.10
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| Elemental Analysis |
C, 64.46; H, 5.41; Cl, 11.19; N, 8.84; O, 10.10
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| CAS # |
2126744-35-0
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| Related CAS # |
2126744-35-0
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| Appearance |
Solid powder
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| SMILES |
C1CC2=C(C=CC(=C2)Cl)N(C1)CC3=CC=C(C=C3)C(=O)NO
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| InChi Key |
MNAYBFFSFQRSIT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17ClN2O2/c18-15-7-8-16-14(10-15)2-1-9-20(16)11-12-3-5-13(6-4-12)17(21)19-22/h3-8,10,22H,1-2,9,11H2,(H,19,21)
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| Chemical Name |
4-[(6-chloro-3,4-dihydro-2H-quinolin-1-yl)methyl]-N-hydroxybenzamide
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| Synonyms |
SW-100; SW 100; SW100
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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 |
| 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) |
DMSO: ≥ 125 mg/mL (~394.6 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.57 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 20.8 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: ≥ 2.08 mg/mL (6.57 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 20.8 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: ≥ 2.08 mg/mL (6.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1568 mL | 15.7838 mL | 31.5676 mL | |
| 5 mM | 0.6314 mL | 3.1568 mL | 6.3135 mL | |
| 10 mM | 0.3157 mL | 1.5784 mL | 3.1568 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.
 ACS Chem Neurosci.2019 Mar 20;10(3):1679-1695. |
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