GSK2879552
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.98%
- CAS No.: 1401966-69-5
- Formule: C23H28N2O2
- Masse moléculaire:364.48
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
HY-L061
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Anti-Cancer Metabolism Compound Library
HY-L083
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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Epigenetics Compound Library Mini
HY-L005M
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Methylation Compound Library
HY-L203
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) GSK2879552
More- Natl Sci Rev. 2023 Feb 14;10(4):nwad028. [Abstract]
- Mol Cell. 2023 Dec 7;83(23):4370-4385.e9. [Abstract]
- Nat Commun. 2024 May 21;15(1):4327. [Abstract]
- Nat Commun. 2021 Nov 24;12(1):6831. [Abstract]
- Adv Sci (Weinh). 2026 Mar 2:e16411. [Abstract]
- Nat Chem Biol. 2025 Feb;21(2):227-237. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- Cell Rep. 2022 Dec 6;41(10):111770. [Abstract]
- Eur J Med Chem. 2024 Aug 28:278:116801. [Abstract]
- Biochem Pharmacol. 2026 May 2;250(Pt 2):118021. [Abstract]
- Eur J Pharmacol. 2024 Aug 23:176931. [Abstract]
- Bioorg Chem. 2024 Jul 1:150:107603. [Abstract]
- Mol Cancer Res. 2022 Feb;20(2):217-230. [Abstract]
- J Endocrinol. 2019 Sep 1;JOE-19-0188.R1. [Abstract]
- Mol Cell Biochem. 2025 Oct 15. [Abstract]
- Cytokine. 2022 Mar:151:155789. [Abstract]
- Clin Exp Med. 2025 Nov 25;26(1):33. [Abstract]
- Mol Carcinog. 2023 Aug;62(8):1119-1135. [Abstract]
- Cancer Chemother Pharmacol. 2019 Feb;83(2):277-287. [Abstract]
- bioRxiv. 2024 Dec 23:2024.12.23.630174. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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Flow Cytometry
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Histological Imaging/Staining
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Histological Imaging/Staining
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In Vivo Efficacy Study
Activité biologique
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KDM1/LSD1 |
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Cell Line
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Type | Value | Description | References |
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| DU-145 | GI50 |
>10 μM
Compound: GSk2879552; 2
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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
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[PMID: 34908406] |
| ECa-109 cell line | IC50 |
>50 μM
Compound: GSK2879552
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Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay
Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay
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[PMID: 27769034] |
| HCT-116 | IC50 |
>64 μM
Compound: GSK-2879552
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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
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[PMID: 36881982] |
| Kasumi 1 | GI50 |
0.02 μM
Compound: 3; GSK2879552
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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
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[PMID: 32551003] |
| KYSE-450 | IC50 |
>64 μM
Compound: GSK-2879552
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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
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[PMID: 36881982] |
| MGC-803 | IC50 |
>125 μM
Compound: GSK2879552
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Antiproliferative activity against human MGC803 cells after 5 days by MTT assay
Antiproliferative activity against human MGC803 cells after 5 days by MTT assay
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[PMID: 28435523] |
| MGC-803 | IC50 |
>50 μM
Compound: GSK2879552
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Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay
Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay
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[PMID: 27769034] |
| MGC-803 | IC50 |
>64 μM
Compound: GSK-2879552
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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
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[PMID: 36881982] |
| MV4-11 | EC50 |
0.023 μM
Compound: 5; GSK2879552
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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
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[PMID: 35200034] |
| MV4-11 | EC50 |
0.054 μM
Compound: 3; GSK2879552
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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
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[PMID: 32551003] |
| MV4-11 | IC50 |
1.16 μM
Compound: GSK2879552
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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
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[PMID: 30713023] |
| MV4-11 | IC50 |
1.19 μM
Compound: 5; GSK2879552
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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
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[PMID: 35200034] |
| NCI-H1417 | EC50 |
0.8 mg/kg
Compound: Chemical Probe: GSK2879552
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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
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[PMID: 26175415] |
| PC-3 | GI50 |
>10 μM
Compound: GSk2879552; 2
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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
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[PMID: 34908406] |
| RPMI-8226 | IC50 |
>20 μM
Compound: 5; GSK2879552
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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
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[PMID: 35200034] |
| Small cell lung cancer cell line | IC50 |
24 nM
Compound: GSK2879552
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Antiproliferative activity against human SCLC cell
Antiproliferative activity against human SCLC cell
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[PMID: 35820351] |
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.
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Cell Line:9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines.
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Concentration:0-10000 nM.
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Incubation Time:6 days.
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Result:Inhibited cell proliferation.
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Cell Line:Resistant HCC cells (PLC/PRF/5 and Huh7).
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Concentration:0, 1, 2 μM.
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Incubation Time:24 h.
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCI-H526 and NCI-H1417 xenografts[2].
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Dosage:1.5 mg/kg.
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Administration:PO daily for 25-35 days.
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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
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CAS No. 1401966-69-5
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Appearance Solid
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Masse moléculaire 364.48
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Formule C23H28N2O2
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (20)
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Journal Impact Factor
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Most Recent
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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).
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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).
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Nat Commun
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
2025 Feb;21(2):227-237. PMID: 38965385 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Cell Rep
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
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.
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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
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (274 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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]
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, 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 |
GSK2879552 Related Classifications
HY-18632 Related Classifications
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