2. Immunology/Inflammation MAPK/ERK Pathway NF-κB Metabolic Enzyme/Protease Apoptosis
  3. Reactive Oxygen Species Caspase Apoptosis JNK
  4. TASIN-1

TASIN-1 is a selective inhibitor of truncated APCTR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 can be used to prevent and intervene in APC mutant colorectal cancer.

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TASIN-1 Chemical Structure

TASIN-1 Chemical Structure

CAS No. : 792927-06-1

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Based on 1 publication(s) in Google Scholar

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TASIN-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

TASIN-1 is a selective inhibitor of truncated APCTR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 can be used to prevent and intervene in APC mutant colorectal cancer[1][2][3].

IC50 & Target

Caspase 3

 

Caspase-7

 

Cellular Effect
Cell Line Type Value Description References
DLD-1 IC50
63 nM
Compound: 6; TASIN-1
Antiproliferative activity against human DLD1 cells after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against human DLD1 cells after 72 hrs by Celltiter-Glo assay
[PMID: 31070915]
HCT-116 IC50
> 5 μM
Compound: 6; TASIN-1
Cytotoxicity against human HCT116 cells harboring wild-type APC after 72 hrs by Celltiter-Glo assay
Cytotoxicity against human HCT116 cells harboring wild-type APC after 72 hrs by Celltiter-Glo assay
[PMID: 31070915]
HT-29 IC50
53 nM
Compound: 6; TASIN-1
Antiproliferative activity against human HT-29 cells after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against human HT-29 cells after 72 hrs by Celltiter-Glo assay
[PMID: 31070915]
In Vitro

TASIN-1 selectively inhibits adenomatous polyposis coli truncated (APCTR) in DLD1 cells with IC50=70 nM[1].
TASIN-1 (70 nM; 72 h) significantly inhibits the proliferation of human colon cancer cells DLD1 (APCTR) with IC50 of 70 nM, and has a high selectivity against HCT116 (APCWT) cells with IC50 >50 μM[1].
TASIN-1 (2.5 μM; 7 d) inhibits soft agar colony formation of DLD1 cells, but has no significant effect on HCT116[1].
TASIN-1 (2.5 μM; 2-48 h) reduced the cholesterol synthesis rate and endogenous cholesterol levels in DLD1 cells, but had no effect on HCT116 cells[1].
TASIN-1 (2.5 μM; 24 h) induced the expression of endoplasmic reticulum stress marker CHOP and JNK phosphorylation, and activated caspase 3/7 activity in DLD1 cells, but no significant changes were observed in HCT116 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TASIN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: DLD1 (APCTR), HCT116 (APCWT)
Concentration: 0.01-100 μM
Incubation Time: 72 h
Result: Showed an IC50 of 70 nM in DLD1 cells and >50 μM in HCT116 cells, demonstrating >700-fold selectivity for APCTR cells.
In Vivo

TASIN-1 (40 mg/kg; ip; twice daily; 18 days) significantly inhibits tumor growth and induced tumor cell apoptosis in the nude mouse DLD1/HT29 (APCTR) subcutaneous xenograft model, without inhibitory effect on HCT116 (APCWT) tumors[1].
TASIN-1 (20, 40 mg/kg; ip; twice weekly; 90 or 100 days) reduces the number and size of colon polyps and inhibits tumor progression in the CPC;Apc mouse genetic colorectal cancer model without significant liver and kidney damage or weight loss[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (5-6 weeks old, ~20 g) with DLD1/HT29 (APCTR) or HCT116 (APCWT) subcutaneous xenograft model[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal (i.p.) injection, twice daily (bid), 18 days
Result: Reduced DLD1 and HT29 tumor volumes by 40%-60% compared to vehicle control, with increased cleaved caspase 3 and PARP in tumor lysates.
Showed no significant growth inhibition against HCT116 tumors.
Tumor histology revealed fragmented nuclei and increased apoptotic cells in treated groups.
Molecular Weight

352.49

Formula

C18H28N2O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1CCN(C2CCN(S(=O)(C3=CC=C(OC)C=C3)=O)CC2)CC1
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 : 25 mg/mL (70.92 mM; ultrasonic and warming and heat to 60°C; 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 2.8370 mL 14.1848 mL 28.3696 mL
5 mM 0.5674 mL 2.8370 mL 5.6739 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.09 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (7.09 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:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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+
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%
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
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 2.8370 mL 14.1848 mL 28.3696 mL 70.9240 mL
5 mM 0.5674 mL 2.8370 mL 5.6739 mL 14.1848 mL
10 mM 0.2837 mL 1.4185 mL 2.8370 mL 7.0924 mL
15 mM 0.1891 mL 0.9457 mL 1.8913 mL 4.7283 mL
20 mM 0.1418 mL 0.7092 mL 1.4185 mL 3.5462 mL
25 mM 0.1135 mL 0.5674 mL 1.1348 mL 2.8370 mL
30 mM 0.0946 mL 0.4728 mL 0.9457 mL 2.3641 mL
40 mM 0.0709 mL 0.3546 mL 0.7092 mL 1.7731 mL
50 mM 0.0567 mL 0.2837 mL 0.5674 mL 1.4185 mL
60 mM 0.0473 mL 0.2364 mL 0.4728 mL 1.1821 mL
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TASIN-1 Related Classifications

Help & FAQs
  • 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-1792927-06-1TASIN1TASIN 1Reactive Oxygen SpeciesCaspaseApoptosisJNKc-Jun N-terminal kinaseInhibitorinhibitorinhibit

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