GSK-LSD1 dihydrochloride
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.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 2102933-95-7
- Formula: C14H22Cl2N2
- Molecular Weight:289.24
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Epigenetics Compound Library
HY-L005
-
Neuronal Signaling Compound Library
HY-L013
-
Histone Modification Research Compound Library
HY-L024
-
Anti-Cancer Compound Library
HY-L025
-
Reprogramming Compound Library
HY-L039
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Mitochondria-Targeted Compound Library
HY-L089
-
Targeted Diversity Library
HY-L099
-
Antidepressant Compound Library
HY-L108
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
Epigenetics Compound Library Mini
HY-L005M
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Methylation Compound Library
HY-L203
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) GSK-LSD1 dihydrochloride
More- Signal Transduct Target Ther. 2022 Apr 13;7(1):102. [Abstract]
- Nature. 2025 Jun;642(8067):508-518. [Abstract]
- Adv Mater. 2021 May;33(18):e2100949. [Abstract]
- Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]
- Nat Commun. 2025 Jan 2;16(1):212. [Abstract]
- Nat Commun. 2021 Dec 8;12(1):7142. [Abstract]
- Bioorg Chem. 2024 Jul 1:150:107603. [Abstract]
- Sci Rep. 2026 Mar 2;16(1):8917. [Abstract]
- Clin Exp Med. 2025 Nov 25;26(1):33. [Abstract]
- Cytokine. 2022 Mar:151:155789. [Abstract]
- Amino Acids. 2026 May 19. [Abstract]
- Res Sq. 2025 Apr 01.
- bioRxiv. 2024 Aug 19:2024.08.17.607802. [Abstract]
- Patent. US20180263995A1.
Customer Validation & Images
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
-
Cell Imaging/Staining
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
Biological Activity
|
KDM1/LSD1 |
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
-
Molecular Weight 289.24
-
Formula C14H22Cl2N2
-
Color White to light yellow
-
SMILES
C1(N[C@H]2[C@H](C3=CC=CC=C3)C2)CCNCC1.Cl.Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (14)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
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 Jul 1:150:107603. 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
2022 Mar:151:155789. PMID: 34998158 -
Amino Acids
2026 May 19. PMID: 42156569 -
-
bioRxiv
The CoREST complex is a therapeutic vulnerability in malignant peripheral nerve sheath tumors. [Abstract]2024 Aug 19:2024.08.17.607802. PMID: 39229179 -
Solvent & Solubility
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.
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.
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.
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: ≥ 2.08 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.
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: ≥ 2.08 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.
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:
-
-
-
-
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
-
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)
-
Handling Instructions (2659 KB)
References
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, 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.
| 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 |
GSK-LSD1 dihydrochloride Related Classifications
HY-100546A Related Classifications
Powered by Bioz