PL120131 acetate 

PL120131 acetate is a PD-1 antagonist, can specifically blocking the interaction between PD-1 and PD-L1, thereby effectively inhibiting the PD-1-mediated apoptosis signaling pathway. PL120131 acetate rescues lymphocytes from apoptosis, maintains the survival and activity of T cells, and induces cytotoxic T lymphocytes to exert killing effects and recognize macrophages and dendritic cells. PL120131 acetate can be used in research related to breast cancer and various malignant tumors^[1][2][3][4].

PL120131 acetate (32.0-33.4 μM) 可逆转 PD-L1 诱导的 Jurkat 细胞凋亡，使凋亡信号降低 25%，其 IC₅₀ 在 Annexin V 检测中为 32.0 μM，在 Caspase 3/7 检测中为 33.4 μM^[2]。
PL120131 acetate (11.6 μM; 24 h) 可挽救 4T1 共培养体系中原代小鼠 T 细胞的凋亡，增加 4T1 细胞的死亡，并诱导 CD3⁺/CD8⁺ T 细胞中颗粒酶 B 的产生呈显著的剂量依赖性升高^[2]。
PL120131 acetate (0.2-12.5 μg/mL; 24 h) 在原代小鼠淋巴细胞与 4T1 细胞的共培养体系中可诱导 IFNγ 呈剂量依赖性升高，同时诱导 IL-12p70 和 IL-10 呈剂量依赖性降低，表明 T 细胞功能被激活^[2]。
PL120131 acetate (30 μM; 30 min; 24 h) 可使 Jurkat 细胞浸润 3D MDA-MB-231 肿瘤环境，诱导更显著的肿瘤细胞死亡，且相比抗 PD-1 抗体处理，Jurkat 细胞存活率更高^[2]。

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

1404.61 (free base)

C₆₂H₁₀₅N₁₉O₁₈·xC₂H₄O₂

固体

Ac-Gly-Ala-Asp-Tyr-Lys-Arg-Ile-Thr-Val-Lys-Val-Asn-NH2

Ac-GADYKRITVKVN-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Tseng T S, et al. Structure-guided discovery of PD-1/PD-L1 interaction inhibitors: peptide design, screening, and optimization via computation-aided phage display engineering[J]. Journal of Chemical Information and Modeling, 2024, 64(5): 1615-1627.

  [2]. Boohaker R J, et al. Rational design and development of a peptide inhibitor for the PD-1/PD-L1 interaction[J]. Cancer letters, 2018, 434: 11-21.  [Content Brief]

  [3]. Gu W, et al. Undo the brake of tumour immune tolerance with antibodies, peptide mimetics and small molecule compounds targeting PD‐1/PD‐L1 checkpoint at different locations for acceleration of cytotoxic immunity to cancer cells[J]. Clinical and Experimental Pharmacology and Physiology, 2019, 46(2): 105-115.

  [4]. Sun M, et al. Fibroblast Activation Protein-α Responsive Peptide Assembling Prodrug Nanoparticles for Remodeling the Immunosuppressive Microenvironment and Boosting Cancer Immunotherapy. Small. 2022;18(9):e2106296.  [Content Brief]