LATS1 Inhibitor

TRULI (Lats-IN-1) is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. TRULI promotes Yap-dependent proliferation in postmitotic mammalian tissues.

GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC₅₀ values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids.

VT02956 is a LATS inhibitor (IC₅₀: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids. VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

LATS-IN-2 is an efficiently acting LATS (large tumor suppressor kinase) inhibitor. LATS-IN-2 shows potent inhibitory activity against LATS1 with an IC₅₀ value of 1.3 nM. LATS-IN-2 suppresses the phosphorylation of YAP by inhibiting LATS kinase activity. LATS-IN-2 increases the thickness of the epidermis in mice. LATS-IN-2 can be used for the study of ocular diseases such as limbal stem cell deficiency and corneal endothelial dysfunction.

Cardiomyocyte proliferation promoting agent-1 ((E/Z)-GA-002), which is an E/Z mixture, is a cardiomyocyte proliferation promoter. GA-002 (single E configuration) is a kinase inhibitor for LATS1 and LATS2, with its IC₅₀ values being 3.93 nM and 3.87 nM respectively. GA-002 can induce the expression of genes regulated by the Hippo pathway, inhibit the phosphorylation of YAP/TAZ, and induce the nuclear translocation of YAP.

NCGC-023 is a LATS1/2 inhibitor. NCGC-023 selectively inhibits LATS1/2, an upstream regulator of Yap in the Hippo signaling pathway, increases the expression of active Yap protein, activates Yap-dependent signaling pathways, triggers non-Yap-dependent metallothionein-mediated heavy metal responses, and upregulates IL-33-related regenerative responses. NCGC-023 can be used in studies related to gastrointestinal acute radiation syndrome (GI-ARS).

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.

VT02956 is a LATS inhibitor (IC₅₀: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids. VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.