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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 33.00 | |
5 mg | In stock | $ 76.00 | |
10 mg | In stock | $ 133.00 | |
25 mg | In stock | $ 283.00 | |
50 mg | In stock | $ 455.00 | |
100 mg | In stock | $ 672.00 | |
500 mg | In stock | $ 1,430.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 84.00 |
Description | TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC). |
Targets&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]. |
Synonyms | 1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine |
Molecular Weight | 352.49 |
Formula | 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. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
TASIN-1 792927-06-1 Cell Cycle/Checkpoint APC Inhibitor TASIN1 1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine TASIN 1 inhibit inhibitor