erk-5-in-2

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 values of 0.82 μM for ERK5 and 3 μM for ERK5 (MEF2D).

PROTACHPK1 Degrader-5 is a potent, orally active HPK1 PROTAC degrader with a DC50 of 5.0 nM and a Dmax of at least 99%. It significantly inhibits HPK1 by degrading it, reducing SLP76 phosphorylation, and enhancing ERK pathway activation, which in turn stimulates the release of IL-2 and IFN-γ. This compound effectively counteracts immune suppression induced by PGE2, NECA, or TGF-β. Alone, PROTACHPK1 Degrader-5 is capable of suppressing tumor growth in MC38 syngeneic mouse models. It is used in research for immunotherapy applications in cancers such as colorectal cancer.

Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation. [2] Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg/kg every other day.[1]

Resolvin D5 is an oxidised lipid mediator derived from docosahexaenoic acid (DHA) with anti-inflammatory properties. It inhibits the production of interleukin-6 (IL-6) and chemokine CCL5 in LPS-stimulated THP-1 cells via the ERK-NF-κB signalling pathway.

KRAS inhibitor-13 (compound 5-6) is a potent inhibitor of KRAS G12C (IC50: 0.883 μM) and demonstrates a p-ERK inhibitory effect in MIA PaCA-2 and A549 cells with IC50 values of 5.9 μM and >100 μM respectively. KRAS inhibitor-13 has potential applications in pancreatic, colorectal, and lung cancer studies.

ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2, with potential applications in investigating or preventing cancer, inflammation, and other proliferative diseases.

Anticanceragent 231 (compound P5) is a tyrosine kinase inhibitor with an IC50 value of 3.95 μM. It targets the EGFR-ERK1/2 signaling pathway, reducing cell viability, proliferation, migration, and cancer stemness in triple-negative breast cancer (TNBC) cells, potentially playing a significant role in the treatment of TNBC.