GSK-LSD1 dihydrochloride

Name: GSK-LSD1 dihydrochloride
Brand: MedChemExpress
SKU: HY-100546A
Rating: 5.0 (7 reviews)

Cat. No.: HY-100546A Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 16 nM.

For research use only. We do not sell to patients.

GSK-LSD1 dihydrochloride Chemical Structure

CAS No. : 2102933-95-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 143	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 143	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 45	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 288	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of GSK-LSD1 dihydrochloride:

GSK-LSD1-d4 dihydrochloride Get quote
GSK-LSD1 Get quote

7 Publications Citing Use of MCE GSK-LSD1 dihydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Demethylase Isoform Specific Products:

View All Isoforms

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

View All Monoamine Oxidase Isoform Specific Products:

View All Isoforms

MAO-A MAO-B

Biological Activity
Purity & Documentation
References
Customer Review

Description

GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 16 nM.

IC₅₀ & Target

IC50: 16 nM (LSD1)^[1]

In Vitro

GSK-LSD1 shows more than 1000 fold selectivity over other closely related FAD utilizing enzymes including LSD2, and monoamine oxidases MAO-A, MAO-B^[1]. GSK-LSD1 can inhibit KDM1A/LSD1 enzyme activity. GSK-LSD1 induces the formation of LC3-II in U2OS cells. The electronic microscopy shows the formation of autophagosome with GSK-LSD1 treatment. GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

289.24

Formula

C₁₄H₂₂Cl₂N₂

CAS No.

2102933-95-7

Appearance

Solid

Color

White to light yellow

SMILES

C1(N[C@H]2[C@H](C3=CC=CC=C3)C2)CCNCC1.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 62.5 mg/mL (216.08 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4573 mL	17.2867 mL	34.5734 mL
5 mM	0.6915 mL	3.4573 mL	6.9147 mL
10 mM	0.3457 mL	1.7287 mL	3.4573 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (248 KB) HNMR (187 KB)

Handling Instructions (2659 KB)

References

[1]. Purich D. The Inhibitor Index A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads. ISBN 9781138739215

[2]. Wang Z, et al. Inhibition of H3K4 demethylation induces autophagy in cancer cell lines. Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4573 mL	17.2867 mL	34.5734 mL	86.4334 mL
	5 mM	0.6915 mL	3.4573 mL	6.9147 mL	17.2867 mL
	10 mM	0.3457 mL	1.7287 mL	3.4573 mL	8.6433 mL
	15 mM	0.2305 mL	1.1524 mL	2.3049 mL	5.7622 mL
	20 mM	0.1729 mL	0.8643 mL	1.7287 mL	4.3217 mL
	25 mM	0.1383 mL	0.6915 mL	1.3829 mL	3.4573 mL
	30 mM	0.1152 mL	0.5762 mL	1.1524 mL	2.8811 mL
	40 mM	0.0864 mL	0.4322 mL	0.8643 mL	2.1608 mL
	50 mM	0.0691 mL	0.3457 mL	0.6915 mL	1.7287 mL
	60 mM	0.0576 mL	0.2881 mL	0.5762 mL	1.4406 mL
	80 mM	0.0432 mL	0.2161 mL	0.4322 mL	1.0804 mL
	100 mM	0.0346 mL	0.1729 mL	0.3457 mL	0.8643 mL