UNC1062

UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 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].

Product Specifications

CAS Number

[1350549-36-8]

UNSPSC

12352005

Target

Akt; Apoptosis; ERK; JAK; p38 MAPK; PI3K; STAT; TAM Receptor

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/unc1062.html

Purity

98.92

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C25H34N6O4S

Molecular Weight

514.64

References & Citations

[1]Schlegel J, et al. MERTK receptor tyrosine kinase is a therapeutic target in melanoma. J Clin Invest. 2013;123 (5) :2257-2267. |[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.|[3]Yi JH, et al. MerTK is a novel therapeutic target in gastric cancer. Oncotarget. 2015 Apr 20;8 (57) :96656-96667.|[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. |[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.