Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
LSD1 25.3 ± 1.4 nM (IC50) MAO-A 1234.57 nM (IC50) MAO-B 3819.27 nM (IC50) Bcl-2 cIAP-1 Caspase-3 Caspase-9
|
---|---|
ln Vitro |
In comparison to GSK-LSD1 (IC50 > 64 μM) and GSK-2879552 (IC50 > 64 μM), LSD1-IN-26 (compound 12u) shown superior activity on MGC-803, KYSE450, and HCT-116 cells, with IC50 values of 14.3±1.18, 22.8±1.45, and 16.3±2.22 μM, respectively [1]. H3K4 Me1/2 and H3K9 Me2/3 accumulate, and Bcl-2 and c-IAP1 decrease, when exposed to LSD1-IN-26 (0-24 μM, 48 h) [1]. LSD1-IN-26 (0–24 μM, 48 h) suppresses migration and cell stemness while inducing apoptosis and differentiation in cells [1].
|
Cell Assay |
Western Blot Analysis[1]
Cell Types: MGC-803 cells Tested Concentrations: 0, 8, 16, 24 μM Incubation Duration: 48 h Experimental Results: Effectively up-regulated the substrate proteins of LSD1, thereby Dramatically increasing the expression levels of mono-/ bi-methylation of H3K4 and H3K9. Dose-dependently induced the decrease of expression levels of anti-apoptotic proteins Bcl-2 and c-IAP1, and the cleavage of apoptotic executive proteins Caspase3 and Caspase9. |
References |
[1]. Ma QS, et al. Discovery of novel tranylcypromine-based derivatives as LSD1 inhibitors for gastric cancer treatment. Eur J Med Chem. 2023 May 5;251:115228.
|
Molecular Formula |
C27H25CL2F2N3O
|
---|---|
Molecular Weight |
516.41
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
---|---|
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9364 mL | 9.6822 mL | 19.3645 mL | |
5 mM | 0.3873 mL | 1.9364 mL | 3.8729 mL | |
10 mM | 0.1936 mL | 0.9682 mL | 1.9364 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.