Cat. No.: HY-18632

GSK2879552

20 Cited Publications

Customer Review

Based on 20 publication(s) in Google Scholar

GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.

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

Purity: 99.98%
CAS No.: 1401966-69-5
Formula: C₂₃H₂₈N₂O₂
Molecular Weight:364.48

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

GSK2879552 Chemical Structure

CAS No.: 1401966-69-5

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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 (20)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity^[1]^[2].

IC₅₀ & Target

KDM1/LSD1

All Histone Demethylase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	GI₅₀	>10 μM Compound: GSk2879552; 2	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
ECa-109 cell line	IC₅₀	>50 μM Compound: GSK2879552	Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay	[PMID: 27769034]
HCT-116	IC₅₀	>64 μM Compound: GSK-2879552	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]
Kasumi 1	GI₅₀	0.02 μM Compound: 3; GSK2879552	Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay	[PMID: 32551003]
KYSE-450	IC₅₀	>64 μM Compound: GSK-2879552	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	>125 μM Compound: GSK2879552	Antiproliferative activity against human MGC803 cells after 5 days by MTT assay Antiproliferative activity against human MGC803 cells after 5 days by MTT assay	[PMID: 28435523]
MGC-803	IC₅₀	>50 μM Compound: GSK2879552	Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay	[PMID: 27769034]
MGC-803	IC₅₀	>64 μM Compound: GSK-2879552	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]
MV4-11	EC₅₀	0.023 μM Compound: 5; GSK2879552	Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis	[PMID: 35200034]
MV4-11	EC₅₀	0.054 μM Compound: 3; GSK2879552	Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method	[PMID: 32551003]
MV4-11	IC₅₀	1.16 μM Compound: GSK2879552	Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay	[PMID: 30713023]
MV4-11	IC₅₀	1.19 μM Compound: 5; GSK2879552	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay	[PMID: 35200034]
NCI-H1417	EC₅₀	0.8 mg/kg Compound: Chemical Probe: GSK2879552	Antitumor activity against human NCI-H1417 cells xenografted in nude mouse assessed as decrease in GRP expression single administration measured after 24 hrs by by qRT-PCR analysis Antitumor activity against human NCI-H1417 cells xenografted in nude mouse assessed as decrease in GRP expression single administration measured after 24 hrs by by qRT-PCR analysis	[PMID: 26175415]
PC-3	GI₅₀	>10 μM Compound: GSk2879552; 2	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
RPMI-8226	IC₅₀	>20 μM Compound: 5; GSK2879552	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay	[PMID: 35200034]
Small cell lung cancer cell line	IC₅₀	24 nM Compound: GSK2879552	Antiproliferative activity against human SCLC cell Antiproliferative activity against human SCLC cell	[PMID: 35820351]

In Vitro

GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of Sorafenib (HY-10201)-resistant cells and attenuating stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in Sorafenib-resistant cells^[1].

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

Cell Proliferation Assay^[2].

Cell Line:

9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines.
Concentration:

0-10000 nM.
Incubation Time:

6 days.
Result:

Inhibited cell proliferation.

RT-PCR^[1].

Cell Line:

Resistant HCC cells (PLC/PRF/5 and Huh7).
Concentration:

0, 1, 2 μM.
Incubation Time:

24 h.
Result:

Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9, Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.

In Vivo

GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft-bearing mice^[2].

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

Animal Model:

NCI-H526 and NCI-H1417 xenografts^[2].
Dosage:

1.5 mg/kg.
Administration:

PO daily for 25-35 days.
Result:

There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.

Chemical Information

CAS No. 1401966-69-5
Appearance Solid
Molecular Weight 364.48
Formula C₂₃H₂₈N₂O₂
Color White to off-white
SMILES

O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (20)

All Histological Imaging/StainingIn Vivo Efficacy StudyBio/Physico-chemical AssayFlow CytometryWB

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Journal Impact Factor

Natl Sci Rev

Counteracting lineage-specific transcription factor network finely tunes lung adeno-to-squamous transdifferentiation through remodeling tumor immune microenvironment. [Abstract]

2023 Feb 14;10(4):nwad028. PMID: 37051524

GSK2879552 purchased from MedChemExpress. Usage Cited in: Natl Sci Rev. 2023 Feb 14;10(4):nwad028. [Abstract]

Images of H&E staining for individual lungs of KL mice treated with vehicle or GSK2879552.

GSK2879552 purchased from MedChemExpress. Usage Cited in: Natl Sci Rev. 2023 Feb 14;10(4):nwad028. [Abstract]

Representative H&E staining in KL mice treated with vehicle (n = 5) or GSK2879552.

GSK2879552 purchased from MedChemExpress. Usage Cited in: Natl Sci Rev. 2023 Feb 14;10(4):nwad028. [Abstract]

Quantification of AST incidence and tumor burden of KL mice treated with vehicle (n = 5) or GSK2879552 (1.5 mg/kg, ip, daily, 4 weeks).
Mol Cell

CPT1A induction following epigenetic perturbation promotes MAVS palmitoylation and activation to potentiate antitumor immunity. [Abstract]

2023 Dec 7;83(23):4370-4385.e9. PMID: 38016475
Nat Commun

Priming with LSD1 inhibitors promotes the persistence and antitumor effect of adoptively transferred T cells. [Abstract]

2024 May 21;15(1):4327. PMID: 38773088

GSK2879552 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 May 21;15(1):4327. [Abstract]

Principal component analysis (PCA) of RNA-seq data of mouse CD8⁺ T cells activated and expanded in vitro for 5 days with the treatment of GSK2879552 (GSK) or vehicle control (Veh) (n = 3 mice per group).

GSK2879552 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 May 21;15(1):4327. [Abstract]

Flow cytometry analysis of frequencies of CD44⁺CD62L⁺ cells in GSK2879552- or Veh-treated CD8⁺ T cells (n = 3).
Nat Commun

LSD1 inhibition sustains T cell invigoration with a durable response to PD-1 blockade. [Abstract]

2021 Nov 24;12(1):6831. PMID: 34819502
Adv Sci (Weinh)

GNL3 Orchestrates AR Transcriptional Programs to Drive Castration-Resistant Prostate Cancer and Immune Evasion. [Abstract]

2026 Mar 2:e16411. PMID: 41772945
Nat Chem Biol

Uncoupling histone modification crosstalk by engineering lysine demethylase LSD1. [Abstract]

2025 Feb;21(2):227-237. PMID: 38965385
Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
Cell Rep

GABA regulates IL-1β production in macrophages. [Abstract]

2022 Dec 6;41(10):111770. PMID: 36476877
Eur J Med Chem

HSP90/LSD1 dual inhibitors against prostate cancer as well as patient-derived colorectal organoids. [Abstract]

2024 Aug 28:278:116801. PMID: 39241481
Biochem Pharmacol

GSK2879552 inhibits NLRP3 inflammasome-mediated pyroptosis and acute lung injury through NOX2-ROS signalling axis. [Abstract]

2026 May 2;250(Pt 2):118021. PMID: 42082119
Eur J Pharmacol

METTL3 aggravates renal fibrogenesis in obstructive nephropathy via the miR-199a-3p/PAR4 axis. [Abstract]

2024 Aug 23:176931. PMID: 39182553
Bioorg Chem

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

2024 Jul 1:150:107603. PMID: 38968905
Mol Cancer Res

Epigenetic Silencing of BMP6 by the SIN3A-HDAC1/2 Repressor Complex Drives Melanoma Metastasis via FAM83G/PAWS1. [Abstract]

2022 Feb;20(2):217-230. PMID: 34610961
J Endocrinol

Propionate promotes intestinal lipolysis and metabolic benefits via AMPK/LSD1 pathway in mice. [Abstract]

2019 Sep 1;JOE-19-0188.R1. PMID: 31505463
Mol Cell Biochem

Inhibition of LSD1 enhances T cells anti-tumor immunity by promoting TNFSF14 expression in gastric cancer. [Abstract]

2025 Oct 15. PMID: 41091427
Cytokine

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

2022 Mar:151:155789. PMID: 34998158
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
Mol Carcinog

PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]

2023 Aug;62(8):1119-1135. PMID: 37144835
Cancer Chemother Pharmacol

Knockdown of long non-coding HOTAIR enhances the sensitivity to progesterone in endometrial cancer by epigenetic regulation of progesterone receptor isoform B. [Abstract]

2019 Feb;83(2):277-287. PMID: 30443761

GSK2879552 purchased from MedChemExpress. Usage Cited in: Cancer Chemother Pharmacol. 2019 Feb;83(2):277-287. [Abstract]

The protein expression of LSD1, PRB and H3K4me2 is detected through Western blot with GSK2879552 treatment in different cells.
bioRxiv

The CoREST-complex regulates MYC stability and promotes post-transcriptional mRNA splicing in melanoma. [Abstract]

2024 Dec 23:2024.12.23.630174. PMID: 39764010

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (68.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.7436 mL

13.7182 mL

27.4363 mL

5 mM

0.5487 mL

2.7436 mL

5.4873 mL

10 mM

0.2744 mL

1.3718 mL

2.7436 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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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: ≥ 2.75 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 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 (27.5 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Huang M, et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Apr 2;398:12-21 [Content Brief]

[2]. 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]

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

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7436 mL	13.7182 mL	27.4363 mL	68.5909 mL
	5 mM	0.5487 mL	2.7436 mL	5.4873 mL	13.7182 mL
	10 mM	0.2744 mL	1.3718 mL	2.7436 mL	6.8591 mL
	15 mM	0.1829 mL	0.9145 mL	1.8291 mL	4.5727 mL
	20 mM	0.1372 mL	0.6859 mL	1.3718 mL	3.4295 mL
	25 mM	0.1097 mL	0.5487 mL	1.0975 mL	2.7436 mL
	30 mM	0.0915 mL	0.4573 mL	0.9145 mL	2.2864 mL
	40 mM	0.0686 mL	0.3430 mL	0.6859 mL	1.7148 mL
	50 mM	0.0549 mL	0.2744 mL	0.5487 mL	1.3718 mL
	60 mM	0.0457 mL	0.2286 mL	0.4573 mL	1.1432 mL

Keywords

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GSK2879552

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Cancer Metabolism Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GSK2879552

All Histone Demethylase Isoforms

Biological Activity

Chemical Information

Publications (20)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK2879552

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Cancer Metabolism Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GSK2879552

All Histone Demethylase Isoforms

Biological Activity

Chemical Information

Publications (20)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK2879552 Related Classifications

HY-18632 Related Classifications