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Cat. No.: HY-100546

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GSK-LSD1

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

GSK-LSD1, a chemical probe, is a LSD1 inhibitor. GSK-LSD1 reduces food intake and body weight, and improves insulin sensitivity and glycemic control in mouse models of obesity. GSK-LSD1 also ameliorates NAFLD. GSK-LSD1 inhibits SARS-CoV-2-triggered cytokine release in COVID-19 PBMCs. GSK-LSD1 also inhibits cancer growth and metastasis.

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CAS No.: 1431368-48-7
Formule: C₁₄H₂₀N₂
Masse moléculaire:216.32

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (267 KB)

GSK-LSD1 Chemical Structure

CAS No.: 1431368-48-7

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Fluorescent Dye

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

Activité biologique
- Description
- Cellular Effect
Chemical Information
Publications (14)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Histone Demethylase :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	>64 μM Compound: GSK-LSD1	Antiproliferative activity against human HCT-116 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]
KYSE-450	IC₅₀	>64 μM Compound: GSK-LSD1	Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]
MGC-803	IC₅₀	>64 μM Compound: GSK-LSD1	Antiproliferative activity against human MGC-803 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human MGC-803 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]

Chemical Information

CAS No. 1431368-48-7
Masse moléculaire 216.32
Formule C₁₄H₂₀N₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (14)

All Bio/Physico-chemical AssayCell Imaging/Staining

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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 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 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 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 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 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.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (267 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)
Instruction de manipulation (2659 KB)

Références

[1]. Ramms B, et al. Systemic LSD1 Inhibition Prevents Aberrant Remodeling of Metabolism in Obesity. Diabetes. 2022 Dec 1;71(12):2513-2529. [Content Brief]

[2]. Hong KS, et al. GSK-LSD1, an LSD1 inhibitor, quashes SARS-CoV-2-triggered cytokine release syndrome in-vitro. Signal Transduct Target Ther. 2020 Nov 17;5(1):267. [Content Brief]

[3]. Alsaqer SF, et al. Inhibition of LSD1 epigenetically attenuates oral cancer growth and metastasis. Oncotarget. 2017 Jul 27;8(43):73372-73386. [Content Brief]

Calculators

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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.

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GSK-LSD1

14 Cited Publications

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Activité biologique
- Description
Chemical Information
Publications (14)
Pureté et documentation
Références

1/16
1/16

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

Customer Validation
PCA of RNA-seq of THP-1 cells treated with vehicle, GSK-LSD1 dihydrochloride, LY2090314 or combination of both inhibitors.
1/16

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

Customer Validation
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.
1/16

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

Customer Validation
Wright-Giemsa-stained cytospins for primary AML samples treated with DMSO, GSK-LSD1 dihydrochloride (50 nM), LY2090314 (100 nM) and combination of both inhibitors.
1/16

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

Customer Validation
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).
1/16

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

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

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GSK-LSD1

Publications Citing Use of MedChemExpress (MCE) GSK-LSD1

Voir tous les produits spécifiques à Isoform Histone Demethylase

Activité biologique

Chemical Information

Publications (14)

Pureté et documentation

Références

Calculators

Help & FAQs

GSK-LSD1 Related Classifications

HY-100546 Related Classifications