TNKS 22 (Synonyms: TNKS-IN-22)

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TNKS 22 (compound 22) is an orally active and selective tankyrase inhibitor. TNKS 22 inhibits TNKS1 and TNKS2 with IC₅₀s of 0.1 and 4.1 nM, respectively.

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TNKS 22 Chemical Structure

CAS No. : 1507362-00-6

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Biological Activity
Purity & Documentation
References
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Description

TNKS 22 (compound 22) is an orally active and selective tankyrase inhibitor. TNKS 22 inhibits TNKS1 and TNKS2 with IC₅₀s of 0.1 and 4.1 nM, respectively^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
DLD-1	IC₅₀	0.6 nM Compound: 22	Inhibition of TNKS in human DLD1 cells expressing APC mutant assessed as inhibition of super-Topflash reporter gene transcription after 40 to 48 hrs by dual-glo luciferase reporter gene assay Inhibition of TNKS in human DLD1 cells expressing APC mutant assessed as inhibition of super-Topflash reporter gene transcription after 40 to 48 hrs by dual-glo luciferase reporter gene assay	[PMID: 24294969]
SW480	IC₅₀	0.004 μM Compound: 22	Inhibition of TNKS in human SW480 cells assessed as degradation of total pool of beta-catenin after 40 to 48 hrs Inhibition of TNKS in human SW480 cells assessed as degradation of total pool of beta-catenin after 40 to 48 hrs	[PMID: 24294969]
SW480	EC₅₀	3.9 nM Compound: 22	Inhibition of TNKS in human SW480 cells assessed as accumulation of axin-2 into cytoplasmic foci after 24 hrs by Hoechst dye-based assay Inhibition of TNKS in human SW480 cells assessed as accumulation of axin-2 into cytoplasmic foci after 24 hrs by Hoechst dye-based assay	[PMID: 24294969]

Molecular Weight

475.56

Formula

C₂₅H₂₅N₅O₃S

CAS No.

1507362-00-6

SMILES

O=C1C2=CC=CC=C2NC(SCCC(N[C@@H]3CC[C@@H](C4=NN=C(C5=CC=CC=C5)O4)CC3)=O)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hua Z, et al. Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors. J Med Chem. 2013 Dec 27;56(24):10003-15. [Content Brief]

TNKS 22 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TNKS 221507362-00-6TNKS-IN-22TNKS22TNKS-22PARPpoly ADP ribose polymerasetankyraseTNKS1TNKS2Inhibitorinhibitorinhibit

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