Lats1
Large Tumor Suppressor 1 (LATS1) is a serine/threonine kinase and a central tumor suppressor that maintains cellular homeostasis by regulating cell proliferation, apoptosis, genomic stability, and cytoskeletal dynamics[1][2]. Within the Hippo signaling pathway, LATS1 functions together with its paralog LATS2 as a core kinase that negatively regulates the transcriptional co-activators YAP and TAZ, thereby restricting oncogenic transcriptional programs and tumor development[1]. Mechanistically, LATS1-mediated signaling integrates growth-control pathways with additional tumor-suppressive networks, including interactions with p53-associated stress responses and cell-cycle regulatory mechanisms[1]. In cancer-related contexts, reduced expression or functional impairment of LATS1 has been associated with multiple malignancies, and experimental studies demonstrate that loss of LATS pathway activity promotes tumorigenesis and contributes to breast cancer progression[1][3]. Beyond canonical Hippo signaling, LATS1 also functions as an actin-binding protein and negative regulator of actin polymerization, linking tumor suppression to cytoskeletal organization, cell migration, and cell-spreading processes[2]. Compared with the closely related isoform LATS2, accumulating evidence indicates that LATS1 and LATS2 possess both overlapping and nonredundant tumor-suppressive functions, with distinct contributions to mammary tumor phenotypes and cancer-associated biological programs[1][3]. For experimental applications, selective pharmacological inhibitors of LATS1/2 have recently been developed as chemical tools to interrogate Hippo-YAP pathway regulation and kinase-dependent signaling mechanisms in cellular models[4].
References:
- [1]. Furth N, et al. The LATS1 and LATS2 tumor suppressors: beyond the Hippo pathway. Cell Death Differ. 2017 Sep;24(9):1488-1501. [Content Brief]
- [2]. Visser-Grieve S, et al. LATS1 tumor suppressor is a novel actin-binding protein and negative regulator of actin polymerization. Cell Res. 2011 Oct;21(10):1513-6. [Content Brief]
- [3]. Furth N, et al. LATS1 and LATS2 suppress breast cancer progression by maintaining cell identity and metabolic state. Life Sci Alliance. 2018 Oct 30;1(5):e201800171. [Content Brief]
- [4]. Namoto K, et al. Discovery and Optimization of Selective Inhibitors of Large Tumor Suppressor Kinases LATS1 and 2 for In Vivo Investigation of the Hippo-YAP Pathway in Tissue Regeneration. J Med Chem. 2025 Jul 10;68(13):13591-13608. [Content Brief]
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Lats1 Related Products (8)
Related Products (8)
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TRULI
0 ImagesSynonyms: Lats-IN-1TRULI (Lats-IN-1) is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. TRULI promotes Yap-dependent proliferation in postmitotic mammalian tissues.
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GA-017
0 ImagesGA-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.
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VT02956
0 ImagesVT02956 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.
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LATS-IN-2
0 ImagesLATS-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.
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Cardiomyocyte proliferation promoting agent-1
0 ImagesSynonyms: (E/Z)-GA-002Cardiomyocyte 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.
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DDO-4033
0 ImagesCat. No.: HY-175247Purity: 99.11%DDO-4033 is a SPOP inhibitor (IC50 = 16.9 μM, Kd = 15.1 μM). DDO-4033 impairs the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts SPOP recruitment to its substrate LATS1, inhibits its polyubiquitination and subsequent degradation, and upregulates LATS1 expression. DDO-4033 has promising antitumor activity and is promising for renal cell carcinoma research.
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LATS1/2-IN-1
0 ImagesCat. No.: HY-175649CAS No.: 3024011-99-9LATS1/2-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.
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VT02956 hydrochloride
0 ImagesCat. No.: HY-147165AVT02956 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.
