| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| 1g | |||
| Other Sizes |
| Targets |
LSD1-IN-24 targets lysine-specific demethylase 1 (LSD1/KDM1A), an epigenetic enzyme that demethylates histone H3 at lysine 4 (H3K4me1/2) and lysine 9 (H3K9me1/2). By inhibiting LSD1 with an IC50 of 0.247 μM, LSD1-IN-24 alters the methylation status of histones, leading to changes in gene expression. It mediates the expression of PD-L1, a key immune checkpoint protein, thereby enhancing T cell-mediated killing of cancer cells.
|
|---|---|
| ln Vitro |
LSD1-IN-24 (compound 3S) (0–20 μM, 5 days) does not influence BGC-823 and MFC cell proliferation, but it can decrease PD-L1 levels in an LSD1-dependent manner and improve the T cell killing response of BGC-823 cells in a dose-dependent manner. Moreover, it shields H3K4me1/2 from demethylation in a dose-dependent manner while H3K4me3 is not protected [1].
In vitro, LSD1-IN-24 (0-20 μM, 5 days) reduces PD-L1 levels in an LSD1-dependent manner and enhances the T cell killing response of BGC-823 cells in a dose-dependent manner. It dose-dependently protects H3K4me1/2 but not H3K4me3 from demethylation. LSD1-IN-24 does not affect BGC-823 and MFC cell proliferation. These in vitro activities support its use in cancer immunotherapy research by modulating the tumor immune microenvironment. |
| ln Vivo |
In a subcutaneous tumor model containing MFC cells, LSD1-IN-24 (compound 3S) (0-50 mg/kg, oral gavage; daily for 2 weeks) significantly lowered Ki67 in tumor tissue and had no overt adverse effects on mice. It also suppresses MFC cell growth in vivo in a dose-dependent manner [1].
In vivo data for LSD1-IN-24 is not extensively reported in publicly available sources. As a selective LSD1 inhibitor that induces PD-L1 expression and enhances T cell killing, the compound has potential applications in animal models of cancer, particularly for studying combination therapies with immune checkpoint inhibitors. However, specific published in vivo efficacy studies are not detailed in the current literature. LSD1-IN-24 is primarily used as a research tool for studying epigenetic regulation and cancer immunotherapy. |
| Enzyme Assay |
The in vitro LSD1 inhibition assay for LSD1-IN-24 uses recombinant LSD1 enzyme and a histone H3 peptide substrate. Demethylase activity is measured using fluorescence-based or mass spectrometry-based detection methods, and IC50 values are calculated from dose-response curves. PD-L1 expression is assessed in cancer cell lines treated with LSD1-IN-24 using qPCR or Western blotting. T cell killing assays are performed by co-culturing T cells with cancer cells treated with the compound.
|
| Cell Assay |
Cellular assays for LSD1-IN-24 are conducted in cancer cell lines such as BGC-823 and MFC cells. Cells are treated with varying concentrations of LSD1-IN-24 (0-20 μM) for up to 5 days. PD-L1 levels are measured by Western blotting or flow cytometry. H3K4me1/2 and H3K4me3 levels are assessed by Western blotting using specific antibodies. T cell killing responses are evaluated using co-culture assays. Cell proliferation is measured using standard assays such as MTT.
|
| Animal Protocol |
Animal/Disease Models: Male 615 mice with MFC cell[1]
Doses: 0, 10, 25, and 50 mg/kg Route of Administration: po (oral gavage); daily for 2 weeks Experimental Results: Dramatically diminished intratumoral PD-L1 expression, increased CD3+, CD4+, CD8+ cell numbers, interleukin-2 (IL2) and IFNγ mRNA and protein levels were also upregulated. In vivo studies for LSD1-IN-24 would typically involve syngeneic or xenograft mouse models of cancer. The compound would be administered via oral or intraperitoneal routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring tumor growth inhibition, immune cell infiltration, and PD-L1 expression in tumor tissues. However, specific published in vivo protocols for LSD1-IN-24 are not available in the current literature. The compound is currently used as a research tool. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for LSD1-IN-24 is not extensively reported in publicly available sources. The compound has a CAS number of 4734-59-2. It is available as a solid and can be prepared as a 10 mM solution in DMSO. As a small molecule LSD1 inhibitor, it is expected to have moderate oral bioavailability. Detailed PK parameters such as half-life and bioavailability are not available in the current literature for this research compound.
|
| Toxicity/Toxicokinetics |
Toxicity data for LSD1-IN-24 is limited in publicly available sources. The compound does not affect BGC-823 and MFC cell proliferation in vitro, suggesting a favorable safety profile in these cell lines. As with all research compounds, LSD1-IN-24 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
|
| References | |
| Additional Infomation |
LSD1-IN-24 (compound 3S) is a selective LSD1 inhibitor with an IC50 of 0.247 μM. It induces PD-L1 expression and enhances T cell killing responses in an LSD1-dependent manner. LSD1-IN-24 dose-dependently protects H3K4me1/2 but not H3K4me3 from demethylation. It has a CAS number of 4734-59-2. LSD1-IN-24 is a valuable research tool for studying epigenetic regulation, cancer immunotherapy, and the role of LSD1 in the tumor immune microenvironment.
|
| Molecular Formula |
C18H20N2OS
|
|---|---|
| Molecular Weight |
312.429203033447
|
| Exact Mass |
312.13
|
| Elemental Analysis |
C, 69.20; H, 6.45; N, 8.97; O, 5.12; S, 10.26
|
| CAS # |
4734-59-2
|
| PubChem CID |
458780
|
| Appearance |
Pale purple to purple solid powder
|
| LogP |
3.8
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
22
|
| Complexity |
339
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=C2C(SC3=C(N2CCN2CCOCC2)C=CC=C3)=CC=C1
|
| InChi Key |
VJQXIWLVJMDRGV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H20N2OS/c1-3-7-17-15(5-1)20(10-9-19-11-13-21-14-12-19)16-6-2-4-8-18(16)22-17/h1-8H,9-14H2
|
| Chemical Name |
4-(2-(10H-phenothiazin-10-yl)ethyl)morpholine
|
| Synonyms |
LSD1-IN-24; J 3-54; J-3-54; J3-54; J 354; J-354; J354;
|
| 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 | 3.2007 mL | 16.0036 mL | 32.0072 mL | |
| 5 mM | 0.6401 mL | 3.2007 mL | 6.4014 mL | |
| 10 mM | 0.3201 mL | 1.6004 mL | 3.2007 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
