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]}.

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].

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

514.64

C₂₅H₃₄N₆O₄S

1350549-36-8

Solid

White to off-white

O[C@H]1CC[C@H](N2N=C(C3=CC=C(S(=O)(N4CCOCC4)=O)C=C3)C5=CN=C(NCCCC)N=C52)CC1

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Schlegel J, et al. MERTK receptor tyrosine kinase is a therapeutic target in melanoma. J Clin Invest. 2013;123(5):2257-2267.  [Content Brief]

  [2]. Koda Y, Itoh M, Tohda S. Effects of MERTK Inhibitors UNC569 and UNC1062 on the Growth of Acute Myeloid Leukaemia Cells. Anticancer Res. 2018 Jan;38(1):199-204.  [Content Brief]

  [3]. Yi JH, et al. MerTK is a novel therapeutic target in gastric cancer. Oncotarget. 2015 Apr 20;8(57):96656-96667.  [Content Brief]

  [4]. von Mässenhausen A, et al. MERTK as a novel therapeutic target in head and neck cancer. Oncotarget. 2016 May 31;7(22):32678-94.  [Content Brief]

  [5]. Lu N, et al. Modulation of oxidized low-density lipoprotein-affected macrophage efferocytosis by mitochondrial calcium uniporter in a murine model. Immunol Lett. 2023 Nov;263:14-24.  [Content Brief]