865565-29-3

865565-29-3 structure

Name: TC-E 5001
Chemical Name: 3-(4-methoxyphenyl)-5-(((4-(4-methoxyphenyl)-5-methyl-4H-1,2,4-triazol-3-yl)thio)methyl)-1,2,4-oxadiazole
CAS Number: 865565-29-3
Molecular Formula: C₂₀H₁₉N₅O₃S
Molecular Weight: 409.46
Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
Create Date: 2016-05-17 16:59:44
Modify Date: 2024-01-14 21:31:31
TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively[1][2].

Name	3-(4-methoxyphenyl)-5-(((4-(4-methoxyphenyl)-5-methyl-4H-1,2,4-triazol-3-yl)thio)methyl)-1,2,4-oxadiazole

Description	TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> PARP Signaling Pathways >> Cell Cycle/DNA Damage >> PARP
Target	TNKS1:79 nM (Ki) TNKS2:28 nM (Ki)
In Vitro	TC-E 5001 inhibits TNKS2, with an IC50 of 33 nM[1].
References	[1]. Shultz MD, et, al. [1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding. J Med Chem. 2012 Feb 9;55(3):1127-36. [2]. Lien VT, et, al. Towards dual inhibitors of the MET kinase and WNT signaling pathway; design, synthesis and biological evaluation. RSC Advances. 2019 Jour; 9(63): 37092-37100.

Hazard Codes	Xi