| Bioactivity | LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models. |
| Target | Ki: 1.34 μM (lymphotyrosine phosphatase, LYP)IC50: 3.52μM (lymphotyrosine phosphatase, LYP), 13.7 μM (PTP1B), 12.3 μM (PTPN1B) |
| Invitro | LYP-IN-4 (compound D14) 也抑制其他蛋白酪氨酸磷酸酶 (PTP)，IC50 分别为 13.7 μM (PTP1B)、12.3 μM (PTPN1B)[1]。 0 --> LYP-IN-4 相关抗体: |
| In Vivo | LYP-IN-4 (compound D14) (25 mg/kg；灌胃；每天两次，持续 14 天) 在 MC38 等基因模型中显着抑制肿瘤生长，减少肿瘤体积，而不减少小鼠体重[1]。 |
| Name | LYP-IN-4 |
| Formula | C29H21ClN2O8S |
| Molar Mass | 593.00 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Liang X, Zhao H, Du J, Li X, Li K, Zhao Z, Bi W, Zhang X, Yu D, Zhang J, Fang H, Hou X. Discovery of benzofuran-2-carboxylic acid derivatives as lymphoid tyrosine phosphatase (LYP) inhibitors for cancer immunotherapy. Eur J Med Chem. 2023 Oct 5;258:115599. |