1239262-36-2
1239262-36-2 structure
- Name: S 2101
- Chemical Name: S 2101
- CAS Number: 1239262-36-2
- Molecular Formula: C16H16ClF2NO
- Molecular Weight: 311.75
- Catalog: Signaling Pathways Epigenetics Histone Demethylase
- Create Date: 2018-01-11 19:41:33
- Modify Date: 2024-01-14 11:17:58
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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.
| Name | S 2101 |
|---|
| Description | 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. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.99 μM (LSD1)[1] Ki: 0.61 μM (LSD1)[1] |
| In Vitro | 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]. |
| Kinase Assay | 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 |
| Molecular Formula | C16H16ClF2NO |
|---|---|
| Molecular Weight | 311.75 |
| Storage condition | 2-8℃ |