ML-SI1 (Synonyms: DMSO : 100 mg/mL (222.53 mM; Need ultrasonic)) |
Catalog No.GC19764
One-Click Copy Product Info
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ML-SI1 is a racemic mixture and an inhibitor of transient receptor potential cation channel (TRPML), with an IC50 value of 15μM for TRPML1.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
ML-SI1 is a racemic mixture and an inhibitor of transient receptor potential cation channel (TRPML), with an IC50 value of 15μM for TRPML1[1, 2]. TRPML1 is a lysosomal cation channel involved in lysosomal biogenesis, endolysosomal trafficking (including trafficking in neuronal dendrites), and autophagy[3]. ML-SI1 and ML-SI3 are currently the only two published TRPML inhibitors[4].
In vitro, treatment of PANC1 cells with ML-SI1 (0-100μM) for 48h significantly reduced cell viability and induced significant changes in the metabolic profile[5]. Treatment of hippocampal neurons with ML-SI1 (20μM) for 2h blocked the lysosomal localization changes induced by LAMTOR1 knockdown[6]. Treatment of IPEC-J2 cells with ML-SI1 (1.25μM) for 24h significantly reduced ROS and Ca2+ levels induced by AFB1, and significantly decreased cell apoptosis and autophagy[7].
References:
[1] Reeks J, Mahajan P, Clark M, et al. High throughput cryo-EM provides structural understanding for modulators of the lysosomal ion channel TRPML1[J]. Structure, 2025.
[2] Leser C, Keller M, Gerndt S, et al. Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3[J]. European journal of medicinal chemistry, 2021, 210: 112966.
[3] Wang W, Zhang X, Gao Q, et al. TRPML1: an ion channel in the lysosome[J]. Mammalian Transient Receptor Potential (TRP) Cation Channels: Volume I, 2014: 631-645.
[4] Kriegler K, Leser C, Mayer P, et al. Effective chiral pool synthesis of both enantiomers of the TRPML inhibitor trans‐ML‐SI3[J]. Archiv der Pharmazie, 2022, 355(2): 2100362.
[5] Kim B, Jung J. Metabolomic approach to identify potential biomarkers in KRAS-Mutant pancreatic cancer cells[J]. Biomedicines, 2024, 12(4): 865.
[6] Sun J, Lin W, Hao X, et al. LAMTOR1 regulates dendritic lysosomal positioning in hippocampal neurons through TRPML1 inhibition[J]. Frontiers in Cellular Neuroscience, 2024, 18: 1495546.
[7] Cheng X, Liang J, Wu D, et al. Blunting ROS/TRPML1 pathway protects AFB1-induced porcine intestinal epithelial cells apoptosis by restoring impaired autophagic flux[J]. Ecotoxicology and Environmental Safety, 2023, 257: 114942.
| Cell experiment [1]: | |
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Cell lines |
PANC1 cells |
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Preparation Method |
Cells were treated with ML-SI1 for 48h, and then incubated with 2mg/mL MTT solution at 37°C in the dark for 3h. After incubation, DMSO was added to dissolve the formazan crystals produced by the living cells. Absorbance was then measured at 540nm using a microplate reader. |
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Reaction Conditions |
0-100μM; 48h |
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Applications |
Pharmacological inhibition of TRPML1 using ML-SI1 significantly decreased PANC1 cell viability. |
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References: |
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| Cas No. | SDF | ||
| Synonyms | DMSO : 100 mg/mL (222.53 mM; Need ultrasonic) | ||
| Canonical SMILES | O=C(N1C2=CC=C(C=C2C(C1C)CCN3CCOCC3)OC)C4=C(Cl)C(Cl)=CC=C4.[Mixture of diastereomers] | ||
| Formula | C₂₃H₂₆Cl₂N₂O₃ | M.Wt | 449.37 |
| Solubility | DMSO : 100 mg/mL (222.53 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2253 mL | 11.1267 mL | 22.2534 mL |
| 5 mM | 445.1 μL | 2.2253 mL | 4.4507 mL |
| 10 mM | 222.5 μL | 1.1127 mL | 2.2253 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)