Tankyrase Inhibitors (TNKS) 49
TNKS 49 (TNKS-IN-4, CAS 1507362-06-2) is a small-molecule inhibitor targeting tankyrase enzymes (TNKS1 and TNKS2). It is designed to inhibit tankyrase activity, thereby modulating protein stability and regulating the Wnt signaling pathway.
TNKS 49 exerts its biological activity primarily through inhibition of tankyrase-mediated ADP-ribosylation, leading to stabilization of AXIN protein levels and suppression of β-catenin-dependent transcription. In biochemical and cellular assays, TNKS 49 demonstrates nanomolar potency by inhibiting tankyrase autoparsylation and affecting Wnt pathway-driven cell models.
TNKS 49 is utilized in mechanistic studies of tumor biology and regulation of Wnt signaling.
References:
[1] Hua Z, Bregman H, Buchanan J L, et al. Development of Novel Dual Binders as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors. Journal of medicinal chemistry, 2013, 56(24): 10003-10015.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 448.54 |
| Formula | C24H24N4O3S |
| Synonyms | TNKS 49;TNKS49;TNKS-49 |
| Solubility | ≥22.45 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | N-((1r,4r)-4-(4-cyanophenoxy)cyclohexyl)-3-((4-oxo-3,4-dihydroquinazolin-2-yl)thio)propanamide |
| SDF | Download SDF |
| Canonical SMILES | N#Cc(cc1)ccc1O[C@H](CC1)CC[C@@H]1NC(CCSC(N1)=Nc(cccc2)c2C1=O)=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
|
Cell lines |
SW480-TBC cell lines |
|
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
24 h; IC50=1.9 nM |
|
Applications |
Tankyrase Inhibitors (TNKS) 49, phenoxy compounds, has a good enzymatic potency and cellular potency with IC50 value of 1.9 nM in the SW480-TBC cellular assay. The compound demonstrated excellent potencies in TNKS2 autoparsylation assay and the two additional functional cellular assays. |
| Animal experiment [1]: | |
|
Animal models |
Athymic nude mice. |
|
Dosage form |
10 and 50 mg/kg; q.d.; oral taken |
|
Applications |
Tankyrase Inhibitors (TNKS) 49 was evaluated for Wnt-pathway specific pharmacological activity in mouse tumor pharmacodynamic (PD) models. Upon once daily oral administration (at 10 and 50 mg/kg) to mice (n=4) bearing human DLD-1 tumors for 3 days, both compounds exhibited statistically significant, dose-dependent axin2 accumulation (2.1- to 3-fold) and inhibition of STF (70−79%) at day 3 (24 h after the last dose) . |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1] Hua Z, Bregman H, Buchanan J L, et al. Development of Novel Dual Binders as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors[J]. Journal of medicinal chemistry, 2013, 56(24): 10003-10015. |
|
Quality Control & MSDS
- View current batch:
Chemical structure
