PPM-3 

PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC₅₀ of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages^[1].

PPM-3 (200 nM, 0-72 h, A375 cells)-mediated degradation of ERK5 begins within 2-4 h and that degradation peaks at 12 h and lasts at least 72 h^[1].
PPM-3 (0-1 μM, 12 h) shows ERK5 degradation activity in H1975, HepG2, MDA-MB-231, PC-3, HCT116, and A375 cancer cell lines, with DC₅₀ values of 11.5+2.5, 13.7+8.2, 22.7+13.3, 23.5+10.3, 5.6+1.9, and 41.4+22.3 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1000.26

C₅₄H₆₉N₁₁O₆S

3032388-42-1

Solid

White to off-white

O=C(C1=CC=CC=C1N(C)C2=NC(NC3=CC=C(C=C3OC)N4CCN(CC4)CCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(N[C@H](C6=CC=C(C=C6)C7=C(N=CS7)C)C)=O)O)=O)=O)=NC=C28)N8C

Room temperature in continental US; may vary elsewhere.

• [1]. Pan P, et al. 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 Oct 12;66(19):13568-13586.  [Content Brief]