2. Metabolic Enzyme/Protease Apoptosis
  3. Emopamil Binding Protein Ferroptosis Apoptosis
  4. TASIN-30

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.

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TASIN-30

TASIN-30 Chemical Structure

CAS No. : 1678515-93-9

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Based on 1 publication(s) in Google Scholar

TASIN-30 Related Antibodies

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1 Publications Citing Use of MCE TASIN-30

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Description

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[1][2][3].

In Vitro

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.

TASIN-30 Related Antibodies

Cell Viability Assay[3]

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.
In Vivo

TASIN-30 (7.5 mg/kg; i.v.; on days 0, 3, and 6; 18 days) delivers an in vivo tumor inhibition rate of approximately 82.5% in BALB/c nude mice with subcutaneous 143B osteosarcoma, exerting potent antitumor effects by combining ferroptosis induction and apoptosis activation while inhibiting EBP to overcome ferroptosis resistance[2].
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.
Molecular Weight

354.51

Formula

C18H30N2O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=C(C)C=C(C)C=C1C)(N2CCC(CC2)NCCC(C)O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8208 mL 14.1040 mL 28.2079 mL
5 mM 0.5642 mL 2.8208 mL 5.6416 mL
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.96%

SDS (251 KB)

COA (246 KB) HNMR (386 KB) RP-HPLC (253 KB) LCMS (97 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. 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
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TASIN-30 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TASIN-301678515-93-9TASIN30TASIN 30Emopamil Binding ProteinFerroptosisApoptosisemopamil binding proteinDLD-1 cells143B osteosarcoma cellscolorectal cancer7-dehydrocholesterolDHCR24SU-DHL-8 human DLBCL cellsDHCR7APC mutant colorectal cancer cellsferroptosisEBP inhibitorosteosarcomaInhibitorinhibitorinhibit

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