Cat. No.: HY-100546

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GSK-LSD1

Name: GSK-LSD1
Brand: MedChemExpress
SKU: HY-100546
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14 Cited Publications

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Based on 14 publication(s) in Google Scholar

GSK-LSD1 is a selective irreversible LSD1/KDM1A histone demethylase inhibitor with a K_i of 0.16 μM. GSK-LSD1 decreases NF-κB p65 stability and pro-inflammatory cytokine expression/secretion. GSK-LSD1 in combination with Ruxolitinib (HY-50856) or BCL2 inhibition reduces leukemia burden in ETP-ALL models. GSK-LSD1 can be used in research on medulloblastoma, autism spectrum disorders, small cell lung cancer, glioblastoma, and obesity.

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

CAS No.: 1431368-48-7
Formula: C₁₄H₂₀N₂
Molecular Weight:216.32

Storage:

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

Data Sheet (284 KB)

GSK-LSD1 Chemical Structure

CAS No.: 1431368-48-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[9]

LSD1

0.16 μM (Ki)

All Histone Demethylase Isoforms :

All NF-κB Isoforms :

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]

In Vitro

Anti-cancerApoptosisCytokines & ChemokinesCell Cycle RegulationInnate ImmunityMitochondrial FunctionOxidative StressViral InfectionOthers

Anti-cancer

GSK-LSD1 (48 h) potently inhibits the proliferation of MG medulloblastoma cells (IC₅₀ = 0.05 nM), whereas MP cells show markedly lower sensitivity (IC₅₀ = 440.2 nM)^[1].
GSK-LSD1 (1-250 nM) in combination with LY2090314 induces CD11b expression in 11 of 16 primary AML samples and inhibits colony formation in DNMT3A-mutant primary AML cells^[7].

Anti-cancer

Apoptosis

Cytokines & Chemokines

GSK-LSD1 (100 nM) increases the transcription of the pro-apoptotic gene Bcl2l11/BIM and decreases the BCL2/BCL2L11 ratio in Zeb2Tg ETP-ALL TG-50 cells in the absence of IL-7^[3].

Anti-cancer

Cell Cycle Regulation

Apoptosis

GSK-LSD1 (200 µM; 24 h) reprograms the transcriptome of TBD0220 glioblastoma cells, altering 1125 genes and sharing a cell cycle/apoptosis signature of 405 genes with AQB and the combination condition^[6].
GSK-LSD1 increases H3K4me2 at the CDKN1A and BBC3 promoters in TBD0220 cells, and in combination with AQB also increases H3K27me3 and decreases it at these sites^[6].

Anti-cancer

Cytokines & Chemokines

GSK-LSD1 does not activate interferon pathway gene expression in MC38 colon cancer cells^[8].

Innate Immunity

Mitochondrial Function

Oxidative Stress

GSK-LSD1 does not induce mitochondrial superoxide production and does not reduce mitochondrial mass in expanded NK cells or T cells^[9].

Viral Infection

GSK-LSD1 improves the viability of PBMCs from severe COVID-19 donors^[2].

Viral Infection

Innate Immunity

GSK-LSD1 reduces LSD1 S112 phosphorylation and nuclear NF-κB p65 in PBMCs from severe COVID-19 donors^[2].
GSK-LSD1 inhibits LSD1-dependent NF-κB p65 demethylation in PBMCs from severe COVID-19 donors and reduces NF-κB p65 acetylation^[2].

Viral Infection

Innate Immunity

Cytokines & Chemokines

GSK-LSD1 attenuates NF-κB-dependent pro-inflammatory cytokine gene expression in PBMCs from severe COVID-19 donors^[2].

Others

GSK-LSD1 (0.05-5000 nM; 48 h) does not adversely affect the viability of postmitotic cerebellar granule neurons^[1].
GSK-LSD1 is a time-dependent irreversible inactivator of LSD1 in cell-free enzyme assays, with a K_I^app of 0.16 μM and a k_inact/K_I^app of 0.81 min^-1 μM^-1^[5].
GSK-LSD1 is selective among the GPCRs, ion channels, nuclear receptors, kinases, and transporters tested^[5].
GSK-LSD1 binds to the LSD1 catalytic site with a K_i of 0.16 µM^[9].

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

Cell Proliferation Assay^[1]

Cell Line:

mouse MG (Myc+Gfi1) and MP (Myc+DNp53) medulloblastoma tumor cells
Concentration:

concentration series
Incubation Time:

48 h (assay); 16-18 h ([3H]thymidine pulse)
Result:

Inhibited proliferation of MG tumor cells with IC₅₀ = 0.05 nM.
MP tumor cells were much less sensitive, with IC₅₀ = 440.2 nM.

In Vivo

Anti-cancerCell Cycle RegulationCarbohydrate MetabolismLipid MetabolismInnate ImmunityCytokines & ChemokinesGlutamate Release or Receptors

Anti-cancer

GSK-LSD1 (10 mg/kg; i.p.; each week, 4 consecutive days of dosing followed by a 3-day holiday; from 1 week after tumor cell implantation until endpoint) inhibits subcutaneous Gfi1-driven medulloblastoma growth but does not affect intracranial MG tumor growth or survival in NSG mice^[1].
GSK-LSD1 (1.5 mg/kg/day; daily; 2 consecutive weeks) plus Ruxolitinib (HY-50856) reduces splenomegaly and prolongs survival in mice bearing ZEB2^Tg ETP-ALL^[3].
GSK-LSD1 (1.5 mg/kg; once daily) inhibits tumor growth in primary SCLC PDX models, with greater TGI in LX44 and LX48 than in LX36^[5].

Anti-cancer

Cell Cycle Regulation

GSK-LSD1 (10 mg/kg; i.p.; every 2 days) reduces intracranial TBD0220 glioblastoma burden and prolongs survival in nude mice^[6].

Carbohydrate Metabolism

Lipid Metabolism

Innate Immunity

Cytokines & Chemokines

GSK-LSD1 (500 mg/kg/mouse; i.p.; once daily; 6 weeks) prevents hyperglycemia and improves adipose and liver metabolism in db/db obesity^[10].
GSK-LSD1 (500 mg/kg/mouse; i.p.; once daily; 6 weeks) improves glycemia, liver health, and adipose inflammation in db/db mice independently of reduced food intake^[10].

Glutamate Release or Receptors

GSK-LSD1 (5 mg/kg; i.p.; once daily; 3 consecutive days (one round)) restores PFC H3K4me2 and rescues social deficits, repetitive grooming, and synaptic dysfunction in Shank3^+/ΔC mice^[4].

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

Animal Model:

NOD-scid IL2Rgamma-deficient (NSG)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; each week, 4 consecutive days of dosing followed by a 3-day holiday; from 1 week after tumor cell implantation until endpoint
Result:

Inhibited growth of flank MG tumors.
In the parallel intracranial MG tumor study, did not affect tumor growth or survival.

Animal Model:

C57BL/6J (wild-type recipients; primary tumor cells from C57BL/6J ZEB2Tg ETP-ALL)^[3]
Dosage:

1.5 mg/kg/day
Administration:

daily; 2 consecutive weeks
Result:

Reduced splenomegaly and enhanced mouse survival compared with either single agent.\nReduced GFP+ leukemic cells in blood, thymus, bone marrow, and spleen compared with single agents.
Enhanced differentiation in blood (higher levels of DN4 T cells) and thymus (enhanced SP CD4+CD8− levels); no such changes were observed in bone marrow and spleen.

Animal Model:

Shank3+/ΔC mutant line (male; 5-6 weeks old at dosing)^[4]
Dosage:

5 mg/kg
Administration:

i.p.; once daily; 3 consecutive days (one round)
Result:

Elevated PFC neuronal H3K4me2 fluorescence to the control level in Shank3+/ΔC mice; H3K4me2 was increased in PFC on day 1 but not day 8 or day 14 after dosing cessation.
Increased social interaction time and the social preference index, with social improvement lasting ~8 days.
Reduced repetitive self-grooming, with improvement lasting ~21 days and disappearing by 28 days.
Restored NMDAR-EPSC in L5 PFC pyramidal neurons to the control level and elevated mEPSC frequency in striatal medium spiny neurons to the control level without altering mEPSC amplitude.
RNAseq showed that 93 of 544 downregulated genes were elevated and 137 of 698 upregulated genes were normalized.
Elevated Egr1 and Egr4 mRNA in PFC, restored H3K4me2 occupancy at the Egr1 enhancer, and partially reversed global H3K4me2 occupancy around transcription start sites.

Related Protocols :

Chemical Information

CAS No. 1431368-48-7
Molecular Weight 216.32
Formula C₁₄H₂₀N₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (14)

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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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 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]. Lee C, et al. Lsd1 as a therapeutic target in Gfi1-activated medulloblastoma. Nature communications. 2019 Jan 18;10(1):332.

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

[3]. Benyoucef A, et al. JAK/BCL2 inhibition acts synergistically with LSD1 inhibitors to selectively target ETP-ALL. Leukemia. 2022 Dec;36(12):2802-16.

[4]. Rapanelli M, et al. Targeting histone demethylase LSD1 for treatment of deficits in autism mouse models. Molecular psychiatry. 2022 Aug;27(8):3355-3366.

[5]. Mohammad HP, et al. A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC. Cancer cell. 2015 Jul 13;28(1):57-69. [Content Brief]

[6]. Zhao J, et al. Combination LSD1 and HOTAIR-EZH2 inhibition disrupts cell cycle processes and induces apoptosis in glioblastoma cells. Pharmacological research. 2021 Sep;171:105764.

[7]. Hosseini A, et al. Perturbing LSD1 and WNT rewires transcription to synergistically induce AML differentiation. Nature. 2025 Jun 12;642(8067):508-18. [Content Brief]

[8]. Liu Y, et al. LSD1 inhibition sustains T cell invigoration with a durable response to PD-1 blockade. Nature communications. 2021 Nov 24;12(1):6831. [Content Brief]

[9]. Bailey CP, et al. Scaffolding LSD1 inhibitors impair NK cell metabolism and cytotoxic function through depletion of glutathione. Frontiers in immunology. 2020 Sep 17;11:2196.

[10]. Ramms B, et al. Systemic LSD1 Inhibition Prevents Aberrant Remodeling of Metabolism in Obesity. Diabetes. 2022 Dec 01;71(12):2513-2529. [Content Brief]

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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

Publications Citing Use of MedChemExpress (MCE) GSK-LSD1

All Histone Demethylase Isoforms

All NF-κB Isoforms