Ortho AP 1867

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Description: Selective binding ligand for FKBP12F36V; precursor for dTAG compounds
Chemical Name: 2-(2-((R)-3-(3,4-Dimethoxyphenyl)-1-(((S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carbonyl)oxy)propyl)phenoxy)acetic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity for Ortho AP 1867

Ortho AP 1867 is a selective binding ligand for the single point mutant of FKBP12F36V. Functionalized with a carboxylic acid group in the ortho-position to enable onward chemistry. The position of the carboxylic acid group represents an 'exit vector' allowing modification without interfering with compound binding ability. Ortho AP 1867 is a precursor for the dTAG compounds.

Technical Data for Ortho AP 1867

M. Wt 693.79
Formula C38H47NO11
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2230613-03-1
PubChem ID 133080821
InChI Key UYXSZUBFOQLRNQ-BTIIJPOSSA-N
Smiles CC[C@@H](C1=CC(OC)=C(C(OC)=C1)OC)C(N2CCCC[C@H]2C(O[C@@H](C3=CC=CC=C3OCC(O)=O)CCC4=CC(OC)=C(C=C4)OC)=O)=O

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.

Solubility Data for Ortho AP 1867

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 69.38 100

Preparing Stock Solutions for Ortho AP 1867

The following data is based on the product molecular weight 693.79. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.44 mL 7.21 mL 14.41 mL
5 mM 0.29 mL 1.44 mL 2.88 mL
10 mM 0.14 mL 0.72 mL 1.44 mL
50 mM 0.03 mL 0.14 mL 0.29 mL

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Product Datasheets for Ortho AP 1867

References for Ortho AP 1867

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

Nabet et al (2018) The dTAG system for immediate and target-specific protein degradation. Nat.Chem.Biol. 14 431 PMID: 29581585


If you know of a relevant reference for Ortho AP 1867, please let us know.

Keywords: Ortho AP 1867, Ortho AP 1867 supplier, ortho, AP1867, FKBP12, F36V, dTAG, selective, binding, ligand, carboxylic, acid, functionalized, TAG, Degradation, Platform, 7787, Tocris Bioscience

Citations for Ortho AP 1867

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Literature in this Area

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
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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

Validating Targets for TPD Using dTAG Poster

Validating Targets for TPD Using dTAG Poster

The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple WesternTM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.