TASIN-1

Research use only, not for human use.

TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC).

TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC).(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.(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 .

1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine

Others

Other Targets

HBV;CYP1A2

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792927-06-1

352.5

C18H28N2O3S

>98% (HPLC)

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COc1ccc(cc1)S(=O)(=O)N1CCC(CC1)N1CCC(C)CC1

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(-20℃)

With Ice Pack

≥ 2 years