S 2101 |
| Catalog No.GC33339 |
S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1239262-36-2
Sample solution is provided at 25 µL, 10mM.
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S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s. S 2101 also displays much lower inhibition activity toward MAO-B (Ki=17 µM, Kinact/Ki=18 M/s) and MAO-A (Ki=110 µM, Kinact/Ki=60 M/s). The treatment of HEK293T cells with S 2101 results in a dose-dependent increase in the level of H3K4me2, which must have accumulated by the inactivation of LSD1. During the course of S 2101 treatment, the amounts of histone H3 and LSD1 in the nuclear extracts remain essentially unaffected. Because the treatment with 1 μM S 2101 generates a level of H3K4me2 similar to that elicited by 50 μM 2-PCPA, S 2101 is assumed to have approximately 50-fold stronger LSD1 inhibition activity than 2-PCPA in human cells[1].
[1]. Mimasu S, et al. Structurally designed trans-2-phenylcyclopropylamine derivatives potently inhibit histone demethylase LSD1/KDM1 . Biochemistry. 2010 Aug 3;49(30):6494-503.
Kinase experiment: | HEK293T cells are grown in 100 mm dishes in Dulbecco’s modified Eagle’s medium containing 10% FBS and a 100 units/mL penicillin, 100 μg/mL streptomycin antibiotic solution under a 5% CO2 atmosphere at 37°C. Cells at approximately 70% confluency are treated with S 2101 for 24 h, detached, and rinsed several times with ice-cold PBS. Nuclear extracts are prepared using a extraction kit, according to the manufacturer’s instructions. Each nuclear extract is electrophoresed on a 10 to 20% SDS-polyacrylamide gel and then transferred to a nitrocellulose membrane. The proteins on the membranes are probed with primary antibodies and then with a secondary antibody and are detected with a chemiluminescent system. The band intensities are visualized with an image analyzer[1]. |
References: [1]. Mimasu S, et al. Structurally designed trans-2-phenylcyclopropylamine derivatives potently inhibit histone demethylase LSD1/KDM1 . Biochemistry. 2010 Aug 3;49(30):6494-503. | |
| Cas No. | 1239262-36-2 | SDF | |
| Canonical SMILES | FC1=CC(F)=CC([C@H]2[C@H](N)C2)=C1OCC3=CC=CC=C3.Cl | ||
| Formula | C16H16ClF2NO | M.Wt | 311.75 |
| Solubility | Soluble 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 | 3.2077 mL | 16.0385 mL | 32.077 mL |
| 5 mM | 0.6415 mL | 3.2077 mL | 6.4154 mL |
| 10 mM | 0.3208 mL | 1.6038 mL | 3.2077 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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