TASIN-1

• 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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  Caspase 3; Caspase 7

• CAS Number:

  [792927-06-1]