YAP1 Inhibitor

2-Methylbutanal (2-Methylbutyraldehyde) is a short-chain aliphatic aldehyde and a characteristic volatile biomarker that can be used to detect the urinary tract pathogen Proteus. 2-Methylbutanal is an orally active CaSR activator and ENO1 inhibitor (K_d = 4.92 μM). 2-Methylbutanal activates oral CaSR to enhance the umami and salty taste of food. 2-Methylbutanal downregulates YAP1 by inhibiting the RNA-binding function of ENO1, thereby upregulating HPGD and reducing PGE2 production, ultimately relieving immunosuppression to promote the infiltration and activation of intratumoral CD8⁺ T cells. 2-Methylbutanal can be used in research on bacterial infections, colorectal cancer, and food flavor modulation.

TD034 is a selective, reversible and noncovalent HDAC11 inhibitor with an IC₅₀ of 5.1 nM and a K_i of 1.5 nM. TD034 does not inhibit other HDACs or sirtuins. TD034 inhibits the defatty acylation of SHMT2 (HDAC11 substrate). TD034 decreases the YAP1 level via HDAC11 inhibition. TD034 can be used for the study of lung cancer.

LATS1/2-IN-1 is a potent and selective LATS1 and LATS2 inhibitor. LATS1/2-IN-1 exhibits potent inhibitory activity against LATS1 and LATS2 with IC₅₀ values of 4.4 nM and 5.5 nM as determined via r³³P functional assay. LATS1/2-IN-1 displays cellular IC₅₀ values of 136 nM for LATS1 and 36.0 nM for LATS2 as determined via NanoBRET assay. LATS1/2-IN-1 reduces phosphorylation of YAP1 in mouse liver. LATS1/2-IN-1 demonstrates wound healing activity in HT-1080 scratch assay and in vivo SKH1 mouse punch biopsy model. LATS1/2-IN-1 can be used for the study of regenerative medicine indications such as wound healing.