2580941-64-4
Chemical Structure
TNKS-2-IN-3
- CAS No.: 2580941-64-4
- Formula:C24H26N6O2S2
- Molecular Weight:494.63
InChIKey: RHCZTJJJLXGIDT-UHFFFAOYSA-N
SMILES: O=C1NC(SCCN2CCN(CC2)CCSC(NC3=O)=NC4=C3C=CC=C4)=NC5=C1C=CC=C5
Biological Activity: TNKS-2-IN-3 (Compound 5) is a selective competitive tankyrase 2 (TNKS2) inhibitor with an IC50 value of 0.3 nM, showing over 20-fold selectivity over TNKS1 and more than 100-fold selectivity over PARP1/2. TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway by inhibiting TNKS2-mediated ADP-ribosylation, exhibiting antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 is proming for rasearch of solid tumors with aberrant Wnt pathway activation, such as colorectal cancer[1].
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TNKS-2-IN-3 | TNKS-2-IN-3 (Compound 5) is a selective competitive tankyrase 2 (TNKS2) inhibitor with an IC50 value of 0.3 nM, showing over 20-fold selectivity over TNKS1 and more than 100-fold selectivity over PARP1/2. TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway by inhibiting TNKS2-mediated ADP-ribosylation, exhibiting antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 is proming for rasearch of solid tumors with aberrant Wnt pathway activation, such as colorectal cancer. | |||||||||||||||||||||
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