Large Tumor Suppressor (LATS)

Large Tumor Suppressor

LATS is a type of highly conserved serine/threonine protein kinase, belonging to the AGC kinase family. It mainly consists of two homologous members, LATS1 and LATS2. The two have a high degree of functional overlap and are widely involved in processes such as tumor suppression, cell cycle checkpoints, apoptosis, migration, and organ size regulation.
LATS is an enzyme in the Hippo pathway that directly acts on YAP. It achieves two coordinated mechanisms, namely "cytoplasmic retention" and "primer-mediated protein degradation", by phosphorylating the Ser127 and Ser381 sites of YAP. As a result, it precisely and powerfully inhibits the oncogenic activity of YAP.

References:

[1]. Zhao B, et al. A coordinated phosphorylation by Lats and CK1 regulates YAP stability through SCF(beta-TRCP). Genes Dev. 2010 Jan 1;24(1):72-85. [Content Brief]

Large Tumor Suppressor (LATS) Related Products (11):

By Effects:	Inhibitors (9) Activators (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-138489

TRULI	Inhibitor	99.98%
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.

HY-150042

TDI-011536	Inhibitor	99.91%
TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration.

HY-160769

NIBR-LTSi	Inhibitor	99.97%
NIBR-LTSi is an orally active and selective LATS kinase inhibitor. NIBR-LTSi can activate YAP signaling. NIBR-LTSi promotes stem cell proliferation, maintains stemness and blocks differentiation. NIBR-LTSi accelerates liver regeneration following extended hepatectomy in mice.

HY-147082

GA-017	Inhibitor	98.95%
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.

HY-147165

VT02956	Inhibitor	99.58%
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.

HY-N8847

α-Ionone	Activator
α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro.

HY-164254

Cardiomyocyte proliferation promoting agent-1	Inhibitor	99.87%
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.

HY-176886

LATS-IN-2	Inhibitor	99.45%
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.

HY-175247

DDO-4033	Activator	99.11%
DDO-4033 is a SPOP inhibitor (IC₅₀ = 16.9 μM, K_d = 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.

HY-175649

LATS1/2-IN-1	Inhibitor
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.

HY-147165A

VT02956 hydrochloride	Inhibitor
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.

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