| Identification | Back Directory | [Name]
1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine | [CAS]
792927-06-1 | [Synonyms]
1'-bipiperidine
1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4
1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine
1,4'-Bipiperidine, 1'-[(4-methoxyphenyl)sulfonyl]-4-methyl- | [Molecular Formula]
C18H28N2O3S | [MDL Number]
MFCD03992224 | [MOL File]
792927-06-1.mol | [Molecular Weight]
352.49 |
| Chemical Properties | Back Directory | [solubility ]
≥35.2 mg/mL in DMSO; ≥12.02 mg/mL in EtOH with ultrasonic; ≥2.45 mg/mL in H2O with gentle warming and ultrasonic | [form ]
solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
TASIN-1 is a selective inhibitor of truncated APC gene (adenomatous polyposis coli gene) and exerts cytotoxic effects through inhibition of cholesterol biosynthesis. TASIN-1 represents a potential therapeutic strategy for prevention and intervention in CRC with mutant APC[1]. | [Biological Activity]
tasin-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (apc) [1].adenomatous polyposis coli (apc) is a multifunctional tumor suppressor gene that is mutated in more than 80% of colon tumors. apc plays an important role in the negative regulation of canonical wnt signaling pathway through proteasomal degradation of b-catenin. apc is involved in cell cycle control, migration, differentiation, and apoptosis [1].tasin-1 is a selective inhibitor of mutant apc. in two authentic human crc cell lines hct116 (wt apc) and dld1 (truncated apc1417), tasin-1 exhibited potent and selective toxicity toward dld1 cells with ic50 value of 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 [1].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 (wt apc) xenografts. in a genetically engineered crc mouse model, tasin-1 significantly reduced tumor formation in the colons of cpc;apc mice [1].1.lu zhang, panayotis c. theodoropoulos, ugur eskiocak, et al. selective targeting of mutant adenomatous polyposis coli (apc) in colorectal cancer. science translational medicine 19 oct 2016: vol. 8, issue 361, pp. 361ra140. | [References]
[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. DOI:10.1126/scitranslmed.aaf8127 |
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