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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $33 | In Stock | In Stock | |
| 5 mg | $76 | In Stock | In Stock | |
| 10 mg | $133 | In Stock | In Stock | |
| 25 mg | $283 | In Stock | In Stock | |
| 50 mg | $455 | In Stock | In Stock | |
| 100 mg | $672 | In Stock | In Stock | |
| 500 mg | $1,430 | Inquiry | Inquiry | |
| 1 mL x 10 mM (in DMSO) | $84 | In Stock | In Stock |
| 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 |
| Smiles | COc1ccc(cc1)S(=O)(=O)N1CCC(CC1)N1CCC(C)CC1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (156.03 mM), Sonication is recommended. Ethanol: 12.02 mg/mL (34.1 mM), Sonication is recommended. H2O: 2.45 mg/mL (6.95 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||||||||||||
H2O/Ethanol/DMSO
Ethanol/DMSO
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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