TSI-01 |
Catalog No.GC41638
One-Click Copy Product Info
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TSI-01 is a selective inhibitor of lysophosphatidylcholine acyltransferase 2 (LPCAT2) with IC50 values of 0.47 and 3.02 µM for human LPCAT2 and LPCAT1, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 704878-75-1
Sample solution is provided at 25 µL, 10mM.
TSI-01 is a selective inhibitor of lysophosphatidylcholine acyltransferase 2 (LPCAT2) with IC50 values of 0.47 and 3.02 µM for human LPCAT2 and LPCAT1, respectively. LPLAT selectively incorporates fatty chains into lysophospholipids to affect the fatty acid composition of membrane glycerophospholipids [1, 2]. TSI-01 can inhibit the production of platelet-activating factor (PAF) in macrophages, which is rapidly biosynthesized by lyso-PAF acetyltransferase (lyso-PAFAT) [3].
In vitro, treatment of HT29 cells with TSI-01 (10 μM) for 48 h significantly prevented lipid droplet accumulation caused by 5-fluorouracil (5-Fu) and oxaliplatin (Oxa) alone or in combination [4]. TSI-01 (0-30 μM) treated endometrial cancer cell lines, inhibited cell proliferation in a dose-dependent manner, with IC50 values of 7.56 μM and 9.31 μM in Ishikawa cell lines and HEC-1A cell lines, respectively, and promoted cell apoptosis[5].
References:
[1] Tarui M, Shindou H, Kumagai K, et al. Selective inhibitors of a PAF biosynthetic enzyme lysophosphatidylcholine acyltransferase 2 [S][J]. Journal of lipid research, 2014, 55(7): 1386-1396.
[2] Valentine W J, Hashidate–Yoshida T, Yamamoto S, et al. Biosynthetic enzymes of membrane glycerophospholipid diversity as therapeutic targets for drug development[J]. Druggable Lipid Signaling Pathways, 2020: 5-27.
[3] Shindou H, Shiraishi S, Tokuoka S M, et al. Relief from neuropathic pain by blocking of the platelet-activating factor–pain loop[J]. The FASEB Journal, 2017, 31(7): 2973.
[4] Cotte A K, Aires V, Fredon M, et al. Lysophosphatidylcholine acyltransferase 2-mediated lipid droplet production supports colorectal cancer chemoresistance[J]. Nature communications, 2018, 9(1): 322.
[5] Zhao T, Sun R, Ma X, et al. Overexpression of LPCAT1 enhances endometrial cancer stemness and metastasis by changing lipid components and activating TGF-β/Smad2/3 signaling pathway: Tumor-promoting effect of LPCAT1 in endometrial cancer[J]. Acta Biochimica Et Biophysica Sinica, 2022, 54(7): 904.
| Cell experiment [1]: | |
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Cell lines |
HT29 cells |
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Preparation Method |
HT29 cells treated with vehicle (DMSO) or selective LPCAT2 inhibitor TSI-01 (10µM) for 48 h. |
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Reaction Conditions |
10μM; 48h |
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Applications |
TSI-01 in HT29 cells significantly prevented lipid droplet (LD) accumulation especially induced by 5-fluorouracil (5-Fu) and oxaliplatin (Oxa) alone or in combination (FOX) treatments. |
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References: |
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| Cas No. | 704878-75-1 | SDF | |
| Canonical SMILES | O=C(C(Cl)=C1Cl)N(C2=CC=C(C(OC(C)C)=O)C=C2)C1=O | ||
| Formula | C14H11Cl2NO4 | M.Wt | 328.2 |
| Solubility | DMF: 50 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml,DMSO: 30 mg/ml,Ethanol: 1 mg/ml | 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 | 3.0469 mL | 15.2346 mL | 30.4692 mL |
| 5 mM | 609.4 μL | 3.0469 mL | 6.0938 mL |
| 10 mM | 304.7 μL | 1.5235 mL | 3.0469 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)