PeptideDB

LYP-IN-4

CAS: F: C29H21ClN2O8S W: 593.00

LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3
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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.