LATS1/2-IN-1 is a potent and selective inhibitor of LATS1 and LATS2. In the r33P functional assay, it demonstrates strong inhibitory activity with IC50 values of 4.4 nM for LATS1 and 5.5 nM for LATS2. The NanoBRET assay determined the cellular IC50 values as 136 nM for LATS1 and 36.0 nM for LATS2. This compound reduces YAP1 phosphorylation levels in mouse liver. Additionally, LATS1/2-IN-1 shows wound healing activity in HT-1080 scratch assays and in vivo SKH1 mouse punch biopsy models. It is applicable for research into regenerative medicine-related conditions, such as wound healing.

LATS1/2-IN-1 (Compound 27) exhibits significant inhibitory activity on LATS1 and LATS2, with IC₅₀ values of 4.4 nM and 5.5 nM, respectively, as determined by the r 33 P functional assay. At the cellular level, the IC₅₀ values for LATS1 and LATS2 are 136 nM and 36.0 nM, respectively, as measured by NanoBRET assay. The compound demonstrates high binding affinity to LATS1 and LATS2, with Kd values of 2.5 nM and 1.7 nM, respectively, according to TR-FRET assay results. Additionally, LATS1/2-IN-1, at a concentration of 1 μM for 4 hours, induces a 24.8-fold increase in CYR61 mRNA expression in HepG2 cells. Furthermore, treatment with LATS1/2-IN-1, ranging from 4 to 500 nM for 16 hours, enhances wound healing in HepG2 cells.

LATS1/2-IN-1 (Compound 27), when administered as a single intraperitoneal injection at a dose of 30 mg/kg, significantly reduces the phosphorylation level of YAP1 at serine 397 (p-YAP1 S397) in mouse liver homogenate. Additionally, LATS1/2-IN-1 applied topically in concentrations of 0.01–1.0 mg/mL, dissolved in 0.1 mL PF-127 hydrogel, and administered every other day for up to three weeks, promotes accelerated wound healing in the skin of hairless SKH1 mice.