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TC-E 5001

Names

[ CAS No. ]:
865565-29-3

[ Name ]:
TC-E 5001

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H19N5O3S

[ Molecular Weight ]:
409.46

[ Exact Mass ]:
409.12100

[ PSA ]:
113.39000

[ LogP ]:
3.93520

Safety Information

[ Hazard Codes ]:
Xi


Related Compounds