T8758

Poziotinib hydrochloride irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. It is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.

Tubulin/NRP1-IN-1 (compound TN-2) serves as a dual inhibitor targeting both Tubulin and NRP1, exhibiting IC50 values of 0.71 μM and 0.85 μM, respectively. This compound notably reduces the viability of prostate tumor cell lines and triggers apoptosis [1].

Tuspetinib (HM43239) hydrate is a selectively active FLT3 inhibitor for oral administration, demonstrating IC₅₀ values of 1.1 nM for FLT3 WT, 1.8 nM for FLT3 internal tandem duplication (ITD), and 1.0 nM for FLT3 D835Y kinases. As a reversible type I inhibitor, it suppresses FLT3 kinase activity and influences signaling pathways including p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Additionally, Tuspetinib hydrate inhibits leukemic cell proliferation and triggers apoptosis [1] [2] [3].

Tyk2-IN-14, a small molecule inhibitor of TYK2, is significant in treating inflammatory diseases and conditions linked to hypersecretion of IFNa and interferons [1].

Tyk2-IN-15 (Compound 97) is a selective inhibitor of tyrosine kinase 2 (Tyk2) with an IC50 value ≤ 10 nM for Tyk2-JH2. It is utilized in the research of inflammatory and autoimmune diseases [1].

Tyk2-IN-16 is a potent and selective TYK2 inhibitor with an IC50 of less than 10 nM for TYK2-JH2. It inhibits pSTAT4 in NK92 cells with an IC50 of under 10 nM (WO2023220046A1; compound 184) [1].

Tyk2-IN-17 (compound 185) effectively inhibits TYK2 [1].

Tyrosinase-IN-27 (compound 6f), a tyrosinase (TYR) inhibitor with an IC50 of 0.88 μM, binds to TYR, significantly increasing the enzyme's microenvironment hydrophobicity. This interaction alters the secondary structure of TYR, diminishing its α-helix content and effectively inhibiting enzymatic activity. Tyrosinase-IN-27 has practical applications in the food industry, notably in preventing the browning of lotus root slices. [18] [1]