T-3775440 hydrochloride
Based on 3 publication(s) in Google Scholar
T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
For research use only. We do not sell to patients.
- Purity: 99.13%
- CAS No.: 1422535-52-1
- Formula: C18H23ClN4O
- Molecular Weight:346.85
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Storage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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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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Anti-Cancer Metabolism Compound Library
HY-L083
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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MCE Bioactive Compound Library
HY-L001V
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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) T-3775440 hydrochloride
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Biological Activity
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KDM1/LSD1 |
T-3775440 demonstrates irreversible inhibition of recombinant human LSD1, with a kinact/KI value of 1.7×105 (sec 1 M 1). T-3775440 is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nM). T-3775440 blocks the proliferation of several cell lines as quickly as day 3 of treatment. Notably, the granulocyte/macrophage markers CD86 and CD11b are commonly upregulated on both TF-1a and HEL92.1.7 cells in response to T-3775440 treatment, whereas the erythroid markers CD235a and CD71 are downregulated by this treatment. In CMK11-5 cells, CD86 mRNA expression is also clearly upregulated by T-3775440 in a concentration-dependent manner, although only a modest increase in cell surface CD86 expression is observed. T-3775440 treatment disrupts the LSD1-GFI1B association in a concentration-dependent manner. T-3775440 decreases LSD1 binding but not GFI1B binding and increases the level of dimethylated H3K4 at the PI16 locus[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1422535-52-1
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Appearance Solid
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Molecular Weight 346.85
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Formula C18H23ClN4O
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=C([C@@H]2C[C@H]2NCC3CC3)C=C1)C4=CN(C)N=C4.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Mechanisms of Progression of Myeloid Preleukemia to Transformed Myeloid Leukemia in Children with Down Syndrome. [Abstract]2019 Aug 12;36(2):123-138.e10. PMID: 31303423 -
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 -
Elife
LSD1 defines the fiber type-selective responsiveness to environmental stress in skeletal muscle. [Abstract]2023 Jan 25:12:e84618. PMID: 36695573
Solvent & Solubility
DMSO : ≥ 30.18 mg/mL (87.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 8.33 mg/mL (24.02 mM; ultrasonic and warming and heat to 60°C)
* "≥" 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 (stored under nitrogen, 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (stored under nitrogen, 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.5 mg/mL (7.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, 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.
Protocol
The human leukemia cell lines TF-1a, HEL92.1.7, CMK11-5 and M07e are used. All cells are grown in RPMI1640 plus 10% FBS and maintained in a humidified incubator at 37°C and 5% CO2. To assess cell proliferation and viability in human leukemia cell lines, compounds (e.g T-3775440) are added with different concentrations (T-3775440: 0, 10, 50 nM) at 24 h after cell seeding. After the incubation period, cells are lysed with CellTiter-Glo, and luminescent signals are detected using an ARVO MX1420 microplate reader. For cell-cycle analysis, cells are fixed overnight with 70% ethanol. Fixed cells are stained with propidium iodide and analyzed on a FACSCalibur or FACSVerse flow cytometer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female C.B17/Icr-scid/scid Jcl mice are used and maintained under specific pathogen-free conditions. AML cells (2×106 cells) in Matrigel are inoculated subcutaneously into the left flanks of 6- to 7-week-old mice (day 0). Mice are randomized when the mean tumor volume reached approximately 150 to 350 mm3. Subsequently, mice are administrated with vehicle or T-3775440 single doses ranging from 3 to 30 mg/kg once daily on 5 days on/2 days off schedule for 2 weeks. Twice weekly, tumors are measured with vernier calipers, and tumor volumes are calculated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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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)
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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 (stored under nitrogen, 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.8831 mL | 14.4155 mL | 28.8309 mL | 72.0773 mL |
| 5 mM | 0.5766 mL | 2.8831 mL | 5.7662 mL | 14.4155 mL | |
| 10 mM | 0.2883 mL | 1.4415 mL | 2.8831 mL | 7.2077 mL | |
| 15 mM | 0.1922 mL | 0.9610 mL | 1.9221 mL | 4.8052 mL | |
| 20 mM | 0.1442 mL | 0.7208 mL | 1.4415 mL | 3.6039 mL | |
| DMSO | 25 mM | 0.1153 mL | 0.5766 mL | 1.1532 mL | 2.8831 mL |
| 30 mM | 0.0961 mL | 0.4805 mL | 0.9610 mL | 2.4026 mL | |
| 40 mM | 0.0721 mL | 0.3604 mL | 0.7208 mL | 1.8019 mL | |
| 50 mM | 0.0577 mL | 0.2883 mL | 0.5766 mL | 1.4415 mL | |
| 60 mM | 0.0481 mL | 0.2403 mL | 0.4805 mL | 1.2013 mL | |
| 80 mM | 0.0360 mL | 0.1802 mL | 0.3604 mL | 0.9010 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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