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PPM-3

Cat. No. 8116 Submit a Review Datasheet / COA / SDS
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Description: Potent and selective ERK5 Degrader (PROTAC®)
Chemical Name: (2S,4R)-1-((S)-2-(7-(4-(4-((5,11-Dimethyl-6-oxo-6,11-dihydro-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-2-yl)amino)-3-methoxyphenyl)piperazin-1-yl)heptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for PPM-3

PPM-3 is a potent and selective ERK5 Degrader (PROTAC®) (IC50 = 62.4 nM). PPM-3 degrades ERK5 in HCT116, h1975, HepG2, MDA-MB-231, PC-3, and A375 tumor cell lines (DC50 values are 5.6, 11.5, 13.7, 22.7, 23.5 and 41.4 nM respectively). PPM-3 has no effect on tumor cell growth directly but influences tumor development by affecting the differentiation of macrophages.

Technical Data for PPM-3

M. Wt 1000.28
Formula C54H69N11O6S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 3032388-42-1
PubChem ID 168679766
InChI Key QGJQNPNZAYRDMS-OESUUHGFSA-N
Smiles O=C1C2=CC=CC=C2N(C3=NC(NC4=CC=C(N5CCN(CCCCCCC(N[C@H](C(N6C[C@H](O)C[C@H]6C(N[C@@H](C)C7=CC=C(C8=C(C)N=CS8)C=C7)=O)=O)C(C)(C)C)=O)CC5)C=C4OC)=NC=C3N1C)C

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 PPM-3

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100.03 100

Preparing Stock Solutions for PPM-3

The following data is based on the product molecular weight 1000.28. 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 mL 5 mL 10 mL
5 mM 0.2 mL 1 mL 2 mL
10 mM 0.1 mL 0.5 mL 1 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

Molarity Calculator

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

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Dilution Calculator

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References for PPM-3

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

Pan et al (2023) Design, synthesis, and biological evaluation of proteolysis-targeting chimeras as highly selective and efficient degraders of extracellular signal-regulated kinase 5. J.Med.Chem. 66 13568 PMID: 37751283

If you know of a relevant reference for PPM-3, please let us know.

View Related Products by Target

Keywords: PPM-3, PPM-3 supplier, PPM3, Potent, selective, ERK, active, degraders, degrades, Extracellular, Signal-Regulated, Kinases, 5, PROTAC, PROTACs, targeted, protein, degradation, tpd, macrophage, Kinase, Degraders, 8116, Tocris Bioscience

Citations for PPM-3

Citations are publications that use Tocris products.

Currently there are no citations for PPM-3. Do you know of a great paper that uses PPM-3 from Tocris? Please let us know.

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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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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
  • Induced Proximity Tools
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