UNC1062

UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC₅₀ of 1.1 nM (Morrison K_i = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC₅₀ = 60 nM, AXL IC₅₀ = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis^{[1][2][3][4][5]}. In Vitro:UNC1062 (0.5-10 μM, 72 h-21 d) inhibits acute myeloid leukemia (AML) cell lines (OCI/AML5, TMD7, THP-1 and HEL cells) and gastric cancer cell lines (HSC-60 and SNU-5) proliferation and inhibits melanoma cell lines (HMCB and G361 cells) and gastric cancer cells colony formation^[1][2][3].
UNC1062 (0.5-2 μM, 48 h) induces apoptosis of melanoma cell lines (HMCB and G361 cells), AML cell lines (OCI/AML5, TMD7, THP-1 and HEL cells) and gastric cancer cell lines (HSC-60 and SNU-5)^[1][2][3].
UNC1062 (1-5 μM, 24-72 h) causes G2 arrest in gastric cancer cell lines and HNSCC cell lines (G2 arrest cells and NC cells)^[3][4].
UNC1062 (0.25-1 μM, 16-96 h) significantly weakens the migration and invasion ability of SKMEL119 cells and Detroit 562 cells^[1][4].
UNC1062 (0.1-2 μM, 90-100 min) inhibits MERTK phosphorylation and significantly attenuates GAS6-induced activation of STAT6, AKT, and ERK1/2^[1].
UNC1062 (20 μg/L, 18.5 h) attenuates the effects of Ru360 (a mitochondrial calcium uniporter (MCU) inhibitor) in reducing inflammatory cytokines and intracytoplasmic lipid content in primary mouse macrophages, it was confirmed that MCU affects inflammatory response by regulating efferocytosis^[5].