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LSD1-IN-20

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Catalog No. T63140Cas No. 1239589-91-3

Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.

LSD1-IN-20

LSD1-IN-20

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Purity: 99.57%
Catalog No. T63140Cas No. 1239589-91-3
Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$397In StockIn Stock
5 mg$970In StockIn Stock
10 mg$1,180In StockIn Stock
25 mg$1,580In StockIn Stock
50 mg$1,980In StockIn Stock
100 mg$2,500-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Batch Information

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Purity:99.57%
Appearance:Solid
Color:White
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Product Introduction

LSD1-IN-20 AI Summary
LSD1-IN-20 exhibits potent inhibition of human G9a with an IC50 value of 123.0 nM but shows low selectivity for Plasmodium falciparum 3D7, with an IC50 value greater than 1000.0 nM. The compound has notable binding affinity to LSD1/CoREST, with a dissociation constant (Kd) of 243.0 nM, and inhibits LSD1/CoREST with a Ki of 440.0 nM using histone H3 as a substrate. Additionally, LSD1-IN-20 exhibits significant antiproliferative activities against various human cancer cell lines: THP-1 cells with IC50 values between 380.0 nM and 690.0 nM across different time points, MDA-MB-231 cells with an IC50 of 1600.0 nM at 72 hours, RD cells with IC50 values ranging from 2820.0 nM to 6400.0 nM depending on the duration, and Rh30 cells with IC50 values between 2570.0 nM and 4330.0 nM. It also shows cytotoxicity against human derived mesenchymal stem cells, with 85.0% residual viability at 2.5 μM after 72 hours. The compound also manifests antiproliferative activity against human MV4-11 cells with an IC50 of 890.0 nM..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.
Targets&IC50
LSD1:0.440 μM (Ki), G9a:0.68 μM
Chemical Properties
Molecular Weight478.63
FormulaC27H38N6O2
Cas No.1239589-91-3
SmilesN(C=1C2=C(N=C(NCCCN(C)C)N1)C=C(OC)C(OC)=C2)C3CCN(CC4=CC=CC=C4)CC3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (94.02 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0893 mL10.4465 mL20.8930 mL104.4648 mL
5 mM0.4179 mL2.0893 mL4.1786 mL20.8930 mL
10 mM0.2089 mL1.0446 mL2.0893 mL10.4465 mL
20 mM0.1045 mL0.5223 mL1.0446 mL5.2232 mL
50 mM0.0418 mL0.2089 mL0.4179 mL2.0893 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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