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[1].
Product Specifications
CAS Number
2580941-64-4
UNSPSC
12352211
Target
PARP
Related Pathways
Cell Cycle/DNA Damage; Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Smiles
O=C1NC(SCCN2CCN(CC2)CCSC(NC3=O)=NC4=C3C=CC=C4)=NC5=C1C=CC=C5
Molecular Formula
C24H26N6O2S2
Molecular Weight
494.63
References & Citations
[1]Tomassi S, et al. From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. ACS Med Chem Lett. 2020 Feb 3;11 (5) :862-868.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PARP1; PARP2; TNKS1/PARP5A; TNKS2/PARP5B
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