PROTAC®(H-PGDS)-7

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Description: Potent hematopoietic prostaglandin D2 synthase Degrader (PROTAC®)
Chemical Name: N-[4-[4-[[4-[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-1-piperazinyl]carbonyl]-1-piperidinyl]phenyl]-2-phenoxy-5-pyrimidinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for PROTAC®(H-PGDS)-7

PROTAC®(H-PGDS)-7 is a potent Degrader of hematopoietic prostaglandin D2 synthase (H-PGDS; DC50 = 17pM after 24 hours). Comprises the H-PGDS inhibitor TFC-007 (Cat. No. 5108) directly linked to E3 ligase cereblon. Suppresses prostaglandin D2 production in vitro and in vivo.

PROTAC®(H-PGDS)-8 negative control (Cat. No. 8005) also available.

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

Licensing Information

Sold under license from National Institute of Health Sciences, Japan and Tsuzuki Gakuen.

Technical Data for PROTAC®(H-PGDS)-7

M. Wt 742.79
Formula C40H38N8O7
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2761281-50-7
PubChem ID 162679258
InChI Key KQNXUQJGOJWQGL-UHFFFAOYSA-N
Smiles O=C(C1=CN=C(OC2=CC=CC=C2)N=C1)NC3=CC=C(N4CCC(CC4)C(N5CCN(CC5)C(C=CC=C6C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)=O)C=C3

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 PROTAC®(H-PGDS)-7

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 74.28 100

Preparing Stock Solutions for PROTAC®(H-PGDS)-7

The following data is based on the product molecular weight 742.79. 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 1.35 mL 6.73 mL 13.46 mL
5 mM 0.27 mL 1.35 mL 2.69 mL
10 mM 0.13 mL 0.67 mL 1.35 mL
50 mM 0.03 mL 0.13 mL 0.27 mL

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Product Datasheets for PROTAC®(H-PGDS)-7

References for PROTAC®(H-PGDS)-7

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

Osawa et al (2023) CRBN ligand expansion for hematopoietic prostaglandin D2 synthase (H-PGDS) targeting PROTAC design and their in vitro ADME profiles. Bioorg.Med.Chem. 84 117259 PMID: 37018877

Murakami et al (2022) Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase. RSC Med.Chem. 13 1495 PMID: 36561070

Yokoo et al (2021) Discovery of a highly potent and selective Degrader targeting hematopoietic prostaglandin D synthase via in silico design. J.Med.Chem. 64 15868 PMID: 34652145


If you know of a relevant reference for PROTAC®(H-PGDS)-7, please let us know.

Keywords: PROTAC®(H-PGDS)-7, PROTAC®(H-PGDS)-7 supplier, PROTACHPGDS7, PROTAC, protacs, active, degrader, degraders, hematopoietic, prostaglandin, D2, synthase, cereblon, E3, ligase, proteolysis, targeting, chimera, HPGDS, Other, Synthases/Synthetases, Degraders, 8004, Tocris Bioscience

Citations for PROTAC®(H-PGDS)-7

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

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

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
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