A 410099.1, amine

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Description: Functionalized IAP ligand for PROTACs
Chemical Name: tert-Butyl [(S)-1-[[(S)-2-[(2S,4S)-4-amino-2-[[(R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]pyrrolidin-1-yl]-1-cyclohexyl-2-oxoethyl]amino]-1-oxopropan-2-yl](methyl)carbamate hydrochloride
Purity: ≥98% (HPLC)
Citations (2)
Literature (1)

Biological Activity for A 410099.1, amine

A 410099.1, amine is a functionalized IAP ligand for PROTAC® research and development. Boc protected A 410099.1 (Cat.No. 6470). Supplied with an amine functional handle for ready conjugation to a linker/target protein ligand. NanoBRET assays show EC50 values of 4.6, 9.2 and 15.6 nM for cIAP1, cIAP2 and XIAP proteins, respectively. Part of a range of functionalized tool molecules for PROTAC R&D.

Please contact us for SD files of our available Degrader Building Blocks.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Usage Guidelines for A 410099.1, amine

This product is provided for use in onward chemistry. Suitable solvents can be used.

Technical Data for A 410099.1, amine

M. Wt 620.22
Formula C32H49N5O5.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2374122-37-7
Smiles C[C@@H](C(N[C@H](C(N1C[C@H](C[C@H]1C(N[C@@H]2CCCC3=CC=CC=C23)=O)N)=O)C4CCCCC4)=O)N(C(OC(C)(C)C)=O)C.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets for A 410099.1, amine

Certificate of Analysis / Product Datasheet
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References for A 410099.1, amine

References are publications that support the biological activity of the product.

Tinworth et al (2019) PROTAC-mediated degradation of Bruton's tyrosine kinase is inhibited by covalent binding. ACS Chem.Biol. 14 342 PMID: 30807093

Schwalm et al (2022) A toolbox for the generation of chemical probes for baculovirus IAP repeat containing proteins. Front.Cell.Dev.Biol. 10 886537 PMID: 35721509

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Keywords: A 410099.1, amine, A 410099.1, amine supplier, A410099.1, amine, functionalized, boc, protected, E3, ligase, ligands, targeted, protein, degradation, building, blocks, components, TPD, degraders, PROTACs, IAP, inhibitor, of, apoptosis, XIAP, BIRC2, BIRC3, BIRC4, Functionalized, Ligase, Ligands, 6471, Tocris Bioscience

2 Citations for A 410099.1, amine

Citations are publications that use Tocris products. Selected citations for A 410099.1, amine include:

Schwalm et al (2022) A toolbox for the generation of chemical probes for baculovirus IAP repeat containing proteins. Front.Cell.Dev.Biol. 10 886537 PMID: 35721509

Oskar et al (2018) Perfluorooctanoic acid (PFOA) exposure promotes proliferation, migration and invasion potential in human breast epithelial cells. Arch Toxicol 92 1729-1739 PMID: 29502166

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia