erk-5-in-1

ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM) and also inhibits LRRK2[G2019S] (IC50: 26 nM).

XMD17-109 (ERK5-IN-1) is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells).

SOS1-IN-18 (Compound 8) is an inhibitor of the Son of Sevenless 1 protein (SOS1) with a dissociation constant (KD) of 2.6 nM. It disrupts the SOS1-KRAS G12C interaction with an IC50 of 3.4 nM, inhibits ERK phosphorylation in H358 cells with an IC50 of 31 nM, and curtails the proliferation of H358 cells with an IC50 of 5 nM.

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]

ERK1 2 Inhibitor 5, a potent suppressant of the ERK1 2 pathway, is instrumental in the mitogen-activated protein kinase (MAPK) signal transduction pathway, where extracellular signal-regulated kinase (ERK) serves as a critical component of the MAPK family. This compound holds promise for the investigation or mitigation of cancer, inflammation, or various proliferative diseases[1].

SHP2-IN-23 (compound 30) is an orally active inhibitor of SHP2, exhibiting potent activity with an IC50 value of 38 nM and demonstrating favorable pharmacokinetic profiles and in vivo efficacy. Additionally, it robustly inhibits ERK phosphorylation, achieving an IC50 of 5 nM [1].

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.

JIP-1 (153-163) acetate(438567-88-5 free base) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). JIP-1 (153-163) acetate(438567-88-5 free base) binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.