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Cat. No.: HY-12602

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TNKS-IN-4

TNKS-IN-4 (compound 49) is an orally active tankyrase (TNKS) inhibitor with IC₅₀ values of 0.1 nM and 7.6nM for TNKS1 and TNKS2, respectively. TNKS-IN-4 can be used for study of APC-mutant colorectal cancer.

For research use only. We do not sell to patients.

CAS No.: 1507362-06-2
Formula: C₂₄H₂₄N₄O₃S
Molecular Weight:448.54

Storage:

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

Data Sheet (264 KB)

TNKS-IN-4 Chemical Structure

CAS No.: 1507362-06-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

TNKS1

0.1 nM (IC₅₀)

TNKS2

7.6 nM (IC₅₀)

All PARP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
DLD-1	IC₅₀	0.3 nM Compound: 49	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	EC₅₀	4 nM Compound: 49	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]
SW480	IC₅₀	1.9 nM Compound: 49	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]

Chemical Information

CAS No. 1507362-06-2
Molecular Weight 448.54
Formula C₂₄H₂₄N₄O₃S
SMILES

O=C1C2=CC=CC=C2NC(SCCC(N[C@@H]3CC[C@@H](OC4=CC=C(C#N)C=C4)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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (264 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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