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[1][2][3].

Product Specifications

CAS Number

[792927-06-1]

UNSPSC

12352005

Target

Apoptosis; Caspase; JNK; Reactive Oxygen Species (ROS)

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation; MAPK/ERK Pathway; Metabolic Enzyme/Protease; NF-κB

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/tasin-1.html

Concentration

10mM

Purity

98.09

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC1CCN(C2CCN(S(=O)(C3=CC=C(OC)C=C3)=O)CC2)CC1

Molecular Formula

C18H28N2O3S

Molecular Weight

352.49

References & Citations

[1]Zhang L, et al. Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer. Sci Transl Med. 2016 Oct 19;8 (361) :361ra140.|[2]Zhang L, et al. Cholesterol Depletion by TASIN-1 Induces Apoptotic Cell Death through the ER Stress/ROS/JNK Signaling in Colon Cancer Cells. Mol Cancer Ther. 2018 May;17 (5) :943-951.|[3]Wang W, et al. Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC) . J Med Chem. 2019 May 23;62 (10) :5217-5241.