| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
LSD1 0.291 μM (IC50)
LSD1-IN-30 targets lysine-specific demethylase 1 (LSD1, also known as KDM1A), a flavin-dependent histone demethylase that plays a critical role in epigenetic regulation. LSD1 specifically demethylates mono- and di-methylated histone H3 lysine 4 (H3K4me1/2) and H3K9me1/2, thereby regulating gene expression. LSD1 is overexpressed in various cancers and is involved in stem cell biology, differentiation, and development, making it an attractive target for cancer therapy. By inhibiting LSD1, LSD1-IN-30 modulates the epigenetic landscape and can alter gene expression programs that drive cancer cell proliferation and survival. |
|---|---|
| ln Vitro |
LSD1-IN-30 shows potent in vitro activity as an LSD1 inhibitor, with an IC50 of 0.291 μM. This potency makes it suitable for studying LSD1 biology in various cellular contexts. The compound is expected to increase the levels of H3K4me1/2 and H3K9me1/2 in cells, leading to changes in gene expression that can be measured by Western blot, immunofluorescence, or chromatin immunoprecipitation (ChIP). LSD1-IN-30 has been evaluated in cellular models of cancer, where it demonstrates antiproliferative effects.
|
| ln Vivo |
In vivo activity of LSD1-IN-30 has been suggested for research applications in cancer and other diseases where LSD1 plays a pathogenic role. By inhibiting LSD1 and modulating the epigenetic landscape, the compound has the potential to suppress tumor growth and alter disease progression. However, detailed in vivo efficacy data have not been extensively reported in the available literature, and the compound is primarily used as a research tool for in vitro studies.
|
| Enzyme Assay |
Non-cell-based enzyme assays for LSD1-IN-30 typically involve measuring the inhibition of recombinant LSD1 activity using a demethylase assay. A standard protocol includes: incubating purified LSD1 enzyme with a biotinylated histone H3 peptide substrate (H3K4me2) in assay buffer (pH 7.5) at 37°C. LSD1-IN-30 is added at various concentrations (typically 0.001–100 μM), and the reaction is initiated by the addition of the substrate. After incubation, the demethylated product is detected using an anti-H3K4me1 antibody in an ELISA or AlphaLISA format, and IC50 values are calculated from dose-response curves.
|
| Cell Assay |
Cellular assays for LSD1-IN-30 typically involve cancer cell lines with elevated LSD1 expression. A representative protocol includes: culturing cells (e.g., leukemia or solid tumor cell lines) in appropriate medium, treating with LSD1-IN-30 at various concentrations (0.01–100 μM) for 48–72 hours, and assessing cell viability using MTT or CellTiter-Glo assays. To confirm on-target activity, H3K4me1/2 and H3K9me1/2 levels are measured by Western blot, and global gene expression changes are assessed by RNA-seq or qRT-PCR. Cell cycle analysis and apoptosis assays can be performed to characterize the mechanism of antiproliferative effects.
|
| Animal Protocol |
In vivo animal studies with LSD1-IN-30 have not been extensively reported in the available literature. If conducted, a typical protocol would involve xenograft mouse models of LSD1-dependent tumors, with administration of the compound via oral gavage or intraperitoneal injection at doses determined from pharmacokinetic studies. Tumor growth and body weight would be monitored, and tumors would be harvested for histopathological analysis and pharmacodynamic assessment of H3K4me1/2 and H3K9me1/2 levels. The compound is primarily used as a research tool for in vitro studies.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of LSD1-IN-30 have not been extensively reported in the available literature. As a small molecule with a molecular weight of 270.28 g/mol and moderate lipophilicity, it is expected to have reasonable oral bioavailability and tissue penetration. The compound is soluble in DMSO at 100 mg/mL (369.99 mM) and is stored as a powder at -20°C for up to 3 years. Further PK studies are needed to fully characterize its absorption, distribution, metabolism, and excretion profile.
|
| Toxicity/Toxicokinetics |
As a research compound, LSD1-IN-30 is not intended for human therapeutic use, and comprehensive toxicological data are limited to preclinical studies. Standard safety assessments would include cytotoxicity screening in normal and cancer cell lines, hERG channel inhibition testing, and preliminary toxicology studies in animal models to determine maximum tolerated dose and identify potential target organs of toxicity. The compound is stored as a powder at -20°C for up to 3 years.
|
| References | |
| Additional Infomation |
LSD1-IN-30 (Compound 3) is a potent LSD1 inhibitor with an IC50 of 0.291 μM. The compound is referenced in the primary literature for its LSD1 inhibitory activity and is used as a research tool for studying the role of LSD1 in epigenetic regulation, cancer, and other diseases. LSD1 is an attractive target for cancer therapy, and LSD1-IN-30 provides researchers with a tool to investigate the therapeutic potential of LSD1 inhibition. The compound is available in high purity and is suitable for a variety of assay formats.
|
| Molecular Formula |
C15H14N2O3
|
|---|---|
| Molecular Weight |
270.283263683319
|
| Exact Mass |
270.1
|
| CAS # |
1289575-45-6
|
| PubChem CID |
135442596
|
| Appearance |
Off-white to yellow solid powder
|
| LogP |
2.3
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
20
|
| Complexity |
362
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C/C(=N\NC(=O)C1=CC=C(C=C1)O)/C2=CC=CC=C2O
|
| InChi Key |
LVGDDYSLMCRYJE-MHWRWJLKSA-N
|
| InChi Code |
InChI=1S/C15H14N2O3/c1-10(13-4-2-3-5-14(13)19)16-17-15(20)11-6-8-12(18)9-7-11/h2-9,18-19H,1H3,(H,17,20)/b16-10+
|
| Chemical Name |
4-hydroxy-N-[(E)-1-(2-hydroxyphenyl)ethylideneamino]benzamide
|
| 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) |
DMSO :~100 mg/mL (~369.99 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.25 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
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 and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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 (9.25 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. 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 and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6999 mL | 18.4993 mL | 36.9987 mL | |
| 5 mM | 0.7400 mL | 3.6999 mL | 7.3997 mL | |
| 10 mM | 0.3700 mL | 1.8499 mL | 3.6999 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
