TASIN-30
Based on 1 publication(s) in Google Scholar
TASIN-30 is a selective EBP inhibitor with an EC50 of 0.097 μM. TASIN-30 blocks the production of 7-dehydrocholesterol (7-DHC) and downstream cholesterol biosynthesis processes. TASIN-30 depletes downstream sterols, disrupts the integrity of lipid rafts in tumor cells, accelerates intracellular cholesterol consumption, and inhibits tumor cell proliferation. TASIN-30 induces ferroptosis and apoptosis by reducing 7-DHC levels and increasing phospholipid peroxidation. TASIN-30 achieves tumor suppression in nude mice with osteosarcoma. TASIN-30 can be used in cancer-related research such as colorectal cancer and osteosarcoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.96%
- CAS. Nr.: 1678515-93-9
- Formel: C18H30N2O3S
- Molecular Weight:354.51
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Ferroptosis Compound Library
HY-L051
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Bioactive Compound Library Max
HY-L181
-
Anti-Aging Compound Library Mini
HY-L034M
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) TASIN-30
More
Biologische Aktivität
TASIN-30 selectively binds to EBP but not DHCR7 in DLD-1 cells, with an EC50 of 97 nM for competitive binding to EBP, and inhibits EBP activity in DLD-1 cells[1].
The cytotoxicity induced by TASIN-30 (1.85 μM; 2.5 μM lathosterol-MCD) in DLD-1 cells results from downstream sterol depletion (reversible by lanosterol) rather than the accumulation of upstream EBP substrates[1].
TASIN-30 potently inhibits the proliferation of DLD-1 cells, with a cytotoxic IC50 value of 0.169 μM[1].
TASIN-30 significantly reduces the level of 7-DHC in 143B osteosarcoma cells, inhibits the biosynthesis of 7-DHC, decreases total cholesterol levels, disrupts cholesterol biosynthesis, and suppresses the activity or expression of EBP in cells[2].
TASIN-30 slightly inhibits the invasive behavior of 143B osteosarcoma cells, induces cellular apoptosis, and increases the apoptosis rate to approximately 22.56%[2].
TASIN-30 (24 h) induces ferroptosis in human SU-DHL-8 diffuse large B-cell lymphoma (DLBCL) cells[3].
TASIN-30 (1-10 μM; 16 h) induces concentration-dependent lipid peroxidation in human SU-DHL-8 diffuse large B-cell lymphoma (DLBCL) cells[3].
TASIN-30 (3 μM; 24 h) significantly reduces the intracellular 7-DHC level in human diffuse large B-cell lymphoma (SU-DHL-8) cells[3].
TASIN-30 (10 μM; 4 h) increases the sensitivity of various human cancer cell lines to RSL3-induced ferroptosis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:multiple human cancer cell lines (786-O, U2OS, MDA-MB-231, DLD1, HepG2, Hep3B, HuH-7, PLC/PRF/5, SK-Hep1)
-
Concentration:10 μM
-
Incubation Time:4 h (pretreatment; followed by RSL3 treatment for 8-24 h)
-
Result:Significantly increased the sensitivity of all tested cancer cell lines to RSL3-induced ferroptosis, as measured by reduced cell viability.
TASIN-30 blocked lung metastasis promotion in B16F10 melanoma model by reducing 7-DHC levels[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude mice[2]
-
Dosage:7.5 mg/kg
-
Administration:i.v.; on days 0, 3, and 6; 18 days
-
Result:Achieved an in vivo tumor inhibition rate of approximately 82.5%.
Resulted in minimal increases in tumor volume throughout the study.
Reduced final tumor weights compared to control groups.
Induced extensive areas of cell death on H&E staining.
Markedly reduced Ki-67 staining, indicating suppressed proliferation.
Induced abundant TUNEL staining, indicating widespread apoptosis.
Decreased EBP expression.
Downregulated GPX4 expression.
Increased cleaved caspase-3 expression.
Elevated MDA levels significantly compared to control groups.
Reduced GSH-Px activity notably compared to control groups.
Chemical Information
-
CAS. Nr. 1678515-93-9
-
Appearance Solid
-
Molecular Weight 354.51
-
Formel C18H30N2O3S
-
Color White to off-white
-
SMILES
O=S(C1=C(C)C=C(C)C=C1C)(N2CCC(CC2)NCCC(C)O)=O
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (282.08 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (7.05 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.
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.
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.
Reinheit & Dokumentation
-
Data Sheet (277 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Theodoropoulos PC, et al. A Medicinal Chemistry-Driven Approach Identified the Sterol Isomerase EBP as the Molecular Target of TASIN Colorectal Cancer Toxins. J Am Chem Soc. 2020 Apr 1;142(13):6128-6138. [Content Brief]
[3]. Li Y, et al. 7-Dehydrocholesterol dictates ferroptosis sensitivity. Nature. 2024;626(7998):411-418. [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, 6 months; -20°C, 1 month. 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 | 2.8208 mL | 14.1040 mL | 28.2079 mL | 70.5199 mL |
| 5 mM | 0.5642 mL | 2.8208 mL | 5.6416 mL | 14.1040 mL | |
| 10 mM | 0.2821 mL | 1.4104 mL | 2.8208 mL | 7.0520 mL | |
| 15 mM | 0.1881 mL | 0.9403 mL | 1.8805 mL | 4.7013 mL | |
| 20 mM | 0.1410 mL | 0.7052 mL | 1.4104 mL | 3.5260 mL | |
| 25 mM | 0.1128 mL | 0.5642 mL | 1.1283 mL | 2.8208 mL | |
| 30 mM | 0.0940 mL | 0.4701 mL | 0.9403 mL | 2.3507 mL | |
| 40 mM | 0.0705 mL | 0.3526 mL | 0.7052 mL | 1.7630 mL | |
| 50 mM | 0.0564 mL | 0.2821 mL | 0.5642 mL | 1.4104 mL | |
| 60 mM | 0.0470 mL | 0.2351 mL | 0.4701 mL | 1.1753 mL | |
| 80 mM | 0.0353 mL | 0.1763 mL | 0.3526 mL | 0.8815 mL | |
| 100 mM | 0.0282 mL | 0.1410 mL | 0.2821 mL | 0.7052 mL |
TASIN-30 Related Classifications
HY-164561 Related Classifications
Powered by Bioz
- TASIN-30
- 1678515-93-9
- TASIN30
- TASIN 30
- Emopamil Binding Protein
- Ferroptosis
- Apoptosis
- emopamil binding protein
- DLD-1 cells
- 143B osteosarcoma cells
- colorectal cancer
- 7-dehydrocholesterol
- DHCR24
- SU-DHL-8 human DLBCL cells
- DHCR7
- APC mutant colorectal cancer cells
- ferroptosis
- EBP inhibitor
- osteosarcoma
- Inhibitor
- inhibitor
- inhibit