Name: GSK-LSD1 2HCl
Brand: Selleck Chemicals
SKU: S7574
Availability: InStock
Rating: 5 (25 reviews)

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Quality Control

Batch: S757401 DMSO]57 mg/mL]false]Water]57 mg/mL]false]]]false Purity: 99.78%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.78

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
Other Histone Demethylase Inhibitors	GSK-J4 Hydrochloride SP2509 CPI-455 HCl Ladademstat (ORY-1001) Dihydrochloride JIB-04 OG-L002 ML324 IOX1 GSK J1 CP2

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
A549	Function assay	10 uM	1 hr	Binding affinity to LSD1 in human A549 cells assessed as increase in stability of cellular LSD1 protein at 10 uM pre-incubated for 1 hr followed by heating at 49 degC for 3 mins by Western blot-based CESTA	30780087
A549	Function assay	10 uM	1 hr	Binding affinity to LSD1 in human A549 cells assessed as increase in stability of cellular LSD1 protein at 10 uM pre-incubated for 1 hr followed by heating at 52 degC for 3 mins by Western blot-based CESTA	30780087
A549	Function assay		96 hrs	Down regulation of snail levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis	30780087
A549	Function assay		96 hrs	Down regulation of N-cadherin levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis	30780087
A549	Function assay		96 hrs	Down regulation of slug levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis	30780087
A549	Function assay		96 hrs	Up regulation of claudin-1 levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis	30780087
A549	Function assay		96 hrs	Up regulation of E-cadherin levels in human A549 cells up to 16 uM after 96 hrs by Western blot analysis	30780087
THP1	Function assay	4 uM	3 days	Inhibition of LSD1 in human THP1 cells assessed as increase in CD86 expression at 4 uM incubated for 3 days by flow cytometric analysis	31096156
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (197.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 57 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.850mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 57 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.470mg/ml (1.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	289.24	Formula	C₁₄H₂₂Cl₂N₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2102933-95-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CNCCC1NC2CC2C3=CC=CC=C3.Cl.Cl

Mechanism of Action

Targets/IC₅₀/Ki	LSD1 (Cell-free assay) 16 nM
In vitro	GSK-LSD1 induces gene expression changes in cancer cell lines with average EC50 of < 5 nM and inhibits cancer cell line growth with average EC50 of < 5 nM.
In vivo	GSK-LSD1, a highly selective inhibitor of KDM1A, significantly inhibits thyroid cancer progression and enhances the sensitivity of thyroid cancer to chemotherapy.
References	[1] http://www.thesgc.org/chemical-probes/GSK-LSD1 [2] https://pubmed.ncbi.nlm.nih.gov/28800922/ [3] https://pubmed.ncbi.nlm.nih.gov/35198054/

Applications

Methods	Biomarkers	Images	PMID
Western blot	LSD1 / H3K4me2		29088714

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Handling Instructions

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GSK-LSD1 2HCl Histone Demethylase inhibitor

Chemical Structure

Molecular Weight: 289.24