1678515-13-3
Chemical Structure
TASIN-1 hydrochloride
- CAS No.: 1678515-13-3
- Formula:C18H29ClN2O3S
- Molecular Weight:388.95
IUPAC Name: 1'-((4-methoxyphenyl)sulfonyl)-4-methyl-1,4'-bipiperidine hydrochloride
InChIKey: TXDTUQPRRXNCLP-UHFFFAOYSA-N
SMILES: CC1CCN(C2CCN(S(=O)(C3=CC=C(OC)C=C3)=O)CC2)CC1.Cl
Biological Activity: TASIN-1 hydrochloride is a selective inhibitor of truncated APCTR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 hydrochloride specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 hydrochloride 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 hydrochloride can be used to prevent and intervene in APC mutant colorectal cancer[1][2][3].
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TASIN-1 hydrochloride | TASIN-1 hydrochloride is a selective inhibitor of truncated APCTR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 hydrochloride specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 hydrochloride 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 hydrochloride can be used to prevent and intervene in APC mutant colorectal cancer. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
