PPM-3

Name: PPM-3
Brand: Tocris Bioscience
SKU: 8116

Tocris Bioscience, part of Bio-Techne | Catalog # 8116

COA / SDS

Potent and selective ERK5 Degrader (PROTAC®)

Key Product Details

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)
Molecular Weight:	1000.28

View Full Technical Details for PPM-3

Technical Data
Citations

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 for PPM-3

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.00 mL	5.00 mL	10.00 mL
5 mM	0.20 mL	1.00 mL	2.00 mL
10 mM	0.10 mL	0.50 mL	1.00 mL
50 mM	0.02 mL	0.10 mL	0.20 mL

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References for PPM-3

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

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