Enpp-1-IN-1 is a potent and selective ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor[1-2]. Enpp-1-IN-1 is primarily employed in research to explore tumor immunotherapy[3].
In vitro, treatment of various RAS-mutant cancer cell lines (such as A549, H460, and H2030) with Enpp-1-IN-1 (11 or 33μM) for 72–96 hours significantly inhibits cell viability and proliferation[4]. Treating peripheral blood mononuclear cells (PBMCs) derived from small cell lung cancer (SCLC) patients with Enpp-1-IN-1 (2μM) for 72 hours significantly upregulates the mRNA expression levels of STING, MAVS, and IFI16[6].
References:
[1] Ji H, Jiang W, Zhang J, et al. ENPP1 governs the metabolic regulation of effector T cells in autoimmunity by detecting cytosolic mitochondrial DNA. Cell Rep. 2025 Jun 24;44(6):115851.
[2] Liu Q, Wang R, Hou S, et al. Chondrocyte-derived exosomes promote cartilage calcification in temporomandibular joint osteoarthritis. Arthritis Res Ther. 2022 Feb 14;24(1):44.
[3] Ng DYX, Li Z, Lee E, et al. Therapeutic and immunomodulatory potential of pazopanib in malignant phyllodes tumor. NPJ Breast Cancer. 2022 Apr 1;8(1):44.
[4] Xia RX, Zou PC, Xie JT, et al. Dependence of NPPS creates a targetable vulnerability in RAS-mutant cancers. Acta Pharmacol Sin. 2025 Mar;46(3):728-739. doi: 10.1038/s41401-024-01409-2.
[5] De Rosa C, Morgillo F, Amato L, et al. DNA-PK inhibition sustains the antitumor innate immune response in small cell lung cancer. iScience. 2025 Feb 1;28(3):111943.
Enpp-1-IN-1是一种有效的选择性Ectonucleotide pyrophosphatase-phosphodiesterase 1（enpp-1）抑制剂[1-2]。Enpp-1-IN-1主要被运用于探索肿瘤免疫治疗的相关研究[3]。
在体外，Enpp-1-IN-1（11–33μM）处理多种RAS突变癌细胞（如A549、H460、H2030等）72–96小时，可显著抑制细胞活力与增殖[4]。Enpp-1-IN-1（2μM）处理小细胞肺癌（SCLC）患者来源的外周血单个核细胞（PBMCs）72小时，Enpp-1-IN-1可显著上调STING、MAVS和IFI16的mRNA表达水平[5]。