Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC).
説明 | TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC). |
ターゲット&IC50 | APC:50 μM(HCT116 cells), APC:70 nM(DLD1 cells) |
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 [1]. |
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]. |
別名 | 1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine |
分子量 | 352.49 |
分子式 | C18H28N2O3S |
CAS No. | 792927-06-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35.2 mg/mL
EtOH: 12.02 mg/mL (with ultrasonic)
H2O: 2.45 mg/mL (with gentle warming and ultrasonic)
You can also refer to dose conversion for different animals. 詳細
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TASIN-1 792927-06-1 Cell Cycle/Checkpoint APC Inhibitor TASIN1 1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine TASIN 1 inhibit inhibitor