TASIN-1

SKU: orb1305865

Description

TASIN-1 is a research compound that selectively inhibits adenomatous polyposis coli (APC) mutants. It is utilized in vitro and in vivo to study Wnt/β-catenin signaling in colorectal cancer models, providing a tool for investigating oncogenic pathways driven by APC dysfunction.

Research Area

Cell Biology, Immunology & Inflammation, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 792927-06-1
• MW: 352.492
• Purity: 99.86% (May vary between batches)
• Formula: C₁₈H₂₈N₂O₃S
• SMILES: COC1=CC=C(C=C1)S(=O)(=O)N1CCC(CC1)N1CCC(C)CC1
• Target: Caspase,JNK,ROS,APC/C,Apoptosis
• Solubility: H2O:2.45 mg/mL (6.95 mM);Ethanol:12.02 mg/mL (34.1 mM);DMSO:55 mg/mL (156.03 mM)

Bioactivity

• Target IC50:
  APC:50 μM(HCT116 cells)|APC:70 nM(DLD1 cells)
• In Vivo:
  In nude mice with established DLD1 and HT29 tumors, intraperitoneal injection of TASIN-1 twice daily for 18 days reduced the size of tumor xenografts and tumor growth rates. TASIN-1 resulted in the appearance of apoptotic cells with fragmented nuclei and induced an increase in cleaved caspase 3 and cleaved PARP1. However, TASIN-1 did not inhibit tumor growth in HCT116 xenografts. In a genetically engineered CRC mouse model, TASIN-1 significantly reduced tumor formation in the colons of CPC .
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• In Vitro:
  In two authentic human CRC cell lines HCT116 (WT APC) and DLD1 (truncated APC1417), TASIN-1 exhibited potent and selective toxicity toward DLD1 cells (IC50: 70 nM but not toward HCT116 cells (IC50 >50 μM)). TASIN-1 also reduced the endogenous cholesterol biosynthesis rate. TASIN-1 exerted its killing effects primarily by depleting cholesterol through inhibition of emopamil-binding protein (EBP) activity. However, knockdown of truncated APC (>90%) expression desensitized DLD1 cells to TASIN-1, suggesting that APC is required for TASIN-1’s cytotoxicity .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TASIN 1, TASIN1, TASIN-1, 1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine, APC, inhibit, Inhibitor

Compound Identifiers

PubChem CID

1329829