Cat. No.: HY-100546A

GSK-LSD1 dihydrochloride

Name: GSK-LSD1 dihydrochloride
Brand: MedChemExpress
SKU: HY-100546A
Price: 45.00 USD
Availability: InStock
Rating: 5 (14 reviews)

14 Cited Publications

고객리뷰

Based on 14 publication(s) in Google Scholar

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.45%
CAS No.: 2102933-95-7
화학식: C₁₄H₂₂Cl₂N₂
분자량:289.24

보관:

4°C, sealed storage, away from moisture

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

GSK-LSD1 dihydrochloride Chemical Structure

CAS No.: 2102933-95-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (14)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

IC₅₀ & Target

KDM1/LSD1

All Histone Demethylase Isoforms :

All Monoamine Oxidase Isoforms :

MAO-A
MAO-B

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.

Chemical Information

CAS No. 2102933-95-7
Appearance Solid
분자량 289.24
화학식 C₁₄H₂₂Cl₂N₂
Color White to light yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture

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

Publications (14)

All Bio/Physico-chemical AssayCell Imaging/Staining

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Journal Impact Factor

Signal Transduct Target Ther

LSD1 is required for euchromatic origin firing and replication timing. [Abstract]

2022 Apr 13;7(1):102. PMID: 35414135

GSK-LSD1 dihydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2022 Apr 13;7(1):102. [Abstract]

Comparison of genome-wide replication timing after LSD1 was depleted or inhibited. HeLa cells were transfected with LSD1 siRNAs or treated with GSK-LSD1 dihydrochloride prior to synchronization in early S phase for Repli-seq. The results from a representative region of chromosome 2 spanning 49 Mb are illustrated. Regions with decreased Repli-seq reads density after LSD1 depletion/inhibition are shaded in pink, and regions with increased reads density shaded in gray. Replication profiles from public data representing early (G1b) and late (G2) S phases and the distribution of H3K4me2 and H3K27ac are shown. Numbers in square brackets indicate the data range of corresponding track. Statistical analysis of Repli-seq reads density around the summits of LSD1 binding sites is shown (right panel).

GSK-LSD1 dihydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2022 Apr 13;7(1):102. [Abstract]

Statistical analysis of the Repli-seq results showed that the reads density around LSD1 summits decreased in LSD1 knockdown and GSK-LSD1 dihydrochloride groups.
Nature

Perturbing LSD1 and WNT rewires transcription to synergistically induce AML differentiation. [Abstract]

2025 Jun;642(8067):508-518. PMID: 40240608

GSK-LSD1 dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2025 Jun;642(8067):508-518. [Abstract]

PCA of RNA-seq of THP-1 cells treated with vehicle, GSK-LSD1 dihydrochloride, LY2090314 or combination of both inhibitors.

GSK-LSD1 dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2025 Jun;642(8067):508-518. [Abstract]

Quantification of colonies formed by a NPM1-mutant primary AML sample treated with DMSO, GSK-LSD1 dihydrochloride (50 nM, 7-10 days), LY2090314 (100 nM) or combination of both inhibitors.

GSK-LSD1 dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2025 Jun;642(8067):508-518. [Abstract]

Wright-Giemsa-stained cytospins for primary AML samples treated with DMSO, GSK-LSD1 dihydrochloride (50 nM), LY2090314 (100 nM) and combination of both inhibitors.
Adv Mater

Epigenetic Remodeling Hydrogel Patches for Multidrug-Resistant Triple-Negative Breast Cancer. [Abstract]

2021 May;33(18):e2100949. PMID: 33792093
Nat Commun

Copy number amplification of FLAD1 promotes the progression of triple-negative breast cancer through lipid metabolism. [Abstract]

2025 Feb 1;16(1):1241. PMID: 39890808
Nat Commun

Mitochondrial-cytochrome c oxidase II promotes glutaminolysis to sustain tumor cell survival upon glucose deprivation. [Abstract]

2025 Jan 2;16(1):212. PMID: 39747079
Nat Commun

Growth differentiation factor 1-induced tumour plasticity provides a therapeutic window for immunotherapy in hepatocellular carcinoma. [Abstract]

2021 Dec 8;12(1):7142. PMID: 34880251
Bioorg Chem

Discovery of TCP-(MP)-caffeic acid analogs as a new class of agents for treatment of osteoclastic bone loss. [Abstract]

2024 Sep:150:107603. PMID: 38968905
Sci Rep

Discovery of natural apigenin analogues as lysine-specific demethylase 1 inhibitors against tumoral testicular germ cells. [Abstract]

2026 Mar 2;16(1):8917. PMID: 41772063
Clin Exp Med

Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]

2025 Nov 25;26(1):33. PMID: 41286164
Cytokine

The CBL-LSD1-CXCL8 axis regulates methionine metabolism in glioma. [Abstract]

2022 Mar:151:155789. PMID: 34998158
Amino Acids

Methionine concentration regulates LSD1 acetylation in glioma cells. [Abstract]

2026 May 19. PMID: 42156569
Res Sq

2025 Apr 01.
bioRxiv

The CoREST complex is a therapeutic vulnerability in malignant peripheral nerve sheath tumors. [Abstract]

2024 Aug 19:2024.08.17.607802. PMID: 39229179
Patent

US20180263995A1.

용액&용해도

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

Bioz

Keywords

GSK-LSD1 dihydrochloride

14 Cited Publications

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GSK-LSD1 dihydrochloride

Publications Citing Use of MedChemExpress (MCE) GSK-LSD1 dihydrochloride

All Histone Demethylase Isoforms

All Monoamine Oxidase Isoforms