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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
20 Results for "
Hippo/YAP
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "Hippo/YAP" in MCE Product Catalog:
4
4 Cited Publications
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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 .
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MYF-03-69 (TEAD-IN-3) is a covalent and irreversible TEAD inhibitor with IC50s of 385, 143, 558 and 173 nM for TEAD1, TEAD2, TEAD3 and TEAD4. MYF-03-69 disrupts YAP-TEAD association, suppresses TEAD transcriptional activity (IC50 = 56 nM) and up-regulates apoptosis gene BMF. MYF-03-69 selectively inhibits mesothelioma cancer cells with defective Hippo signaling. MYF-03-69 can be used for the study of malignant pleural mesothelioma (MPM) .
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2 Cited Publications
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SBP-3264 is a YAP activator and STK/MST inhibitor with IC50 values of 36 nM against STK3/MST2 and 24 nM against STK4/MST1. SBP-3264 modulates the Hippo signaling pathway. SBP-3264 can be used for the research of acute myeloid leukemia .
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1 Cited Publications
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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.
Cat. No.: HY-400902
CAS No.: 2506273-81-8
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VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors .
Cat. No.: HY-164254
CAS No.: 2351906-71-1
Synonyms: (E/Z)-GA-002
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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 .
Cat. No.: HY-175357
CAS No.: 2957895-40-6
YAP/TEAD-IN-2 (Compound T-1) is a YAP/TEAD inhibitor. YAP/TEAD-IN-2 inhibits the luciferase activity driven by YAP/TEAD in 293T cells. YAP/TEAD-IN-2 exhibits strong anti-proliferative activity against human pleural mesothelioma NCI-H226 cells. YAP/TEAD-IN-2 can be used for the study of diseases associated with Hippo pathway dysregulation, particularly cancers .
Cat. No.: HY-W1005067
CAS No.: 2191110-79-7
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EN171 is a covalent ligand that covalently targets both C38 and C96 on 14-3-3 to enhance 14-3-3 interactions with ERα, YAP and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. EN171 can not only be used as a molecular glue to enhance native protein interactions but can also be used as a covalent 14-3-3 recruiter in heterobifunctional molecules to sequester nuclear neo-substrates such as BRD4 and BLC6 into the cytosol .
Cat. No.: HY-159912
CAS No.: 3027484-09-6
pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
Cat. No.: HY-174505
Human YAP1 mRNA encodes the human Yes1 associated transcriptional regulator (YAP1) protein, a downstream nuclear effector of the Hippo signaling pathway which is involved in development, growth, repair, and homeostasis. YAP1 is known to play a role in the development and progression of multiple cancers as a transcriptional regulator of this signaling pathway and may function as a potential target for cancer treatment.
Cat. No.: HY-170936
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MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
Cat. No.: HY-173150
CAS No.: 106928-29-4
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Cat. No.: HY-176171
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Tubulin polymerization-IN-79 (Compound C20) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-79 shows potent antiproliferative activity against esophageal cancer cells (e.g., KYSE450, IC50=0.36 μM; EC-109, IC50=0.63 μM). Tubulin polymerization-IN-79 occupies the colchicine binding site to disrupt microtubule network integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP expression, and inducing G2/M phase arrest and apoptosis in esophageal cancer cells. Tubulin polymerization-IN-79 is promising for research of esophageal cancers .
Cat. No.: HY-186148
CAS No.: 3081701-84-7
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YL-602 is an orally active Hippo pathway activator. YL-602 activates the Hippo pathway via MST1/2, with downstream pathway activation. YL-602 inhibits YAP and CTGF expression in cells irrespective of cell density and serum presence. YL-602 induces tumor cell apoptosis and inhibits colony formation. YL-602 suppresses tumor growth in mice. YL-602 can be used for the research of cancer, such as breast cancer .
Cat. No.: HY-182743
CAS No.: 2803349-61-1
OICR19451 is an orally active dual NUAK1/NUAK2 and MARK2/MARK3 kinase inhibitor, with IC50 values of 12 nM and 10 nM against NUAK1 and NUAK2, and 101 nM and 124 nM against MARK2 and MARK3, respectively. OICR19451 modulates the Hippo signaling pathway, increases the phosphorylation level of YAP, enhances the cytoplasmic localization of YAP/TAZ, and inhibits the expression of oncogenes. OICR19451 inhibits cancer cell growth, reduces metastasis, promotes tumor capsule formation, and improves mouse survival in an orthotopic breast cancer model. OICR19451 can be used for research related to triple-negative breast cancer .
Cat. No.: HY-187181
CAS No.: 2933893-78-6
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GNE-2181 is an orally active, blood-brain barrier-penetrant pan-TEAD transcription factor inhibitor, with IC50 values of 13, 26, 61 and 17 nM against TEAD1, TEAD2, TEAD3 and TEAD4, respectively. GNE-8021 allosterically disrupts the TEAD-YAP/TAZ interaction and inhibits TEAD-mediated oncogenic transcriptional programs via the Hippo signaling pathway. GNE-8021 suppresses YAP-driven tumor cell growth. GNE-2181 inhibits the growth of intracranial tumor models in vivo. GNE-2181 can be used for research on brain metastasis of lung cancer .
Cat. No.: HY-187180
CAS No.: 2933893-27-5
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GNE-8025 is an orally active pan-TEAD transcription factor inhibitor, with IC50 values of 45, 38, 1035 and 24 nM against TEAD1, TEAD2, TEAD3 and TEAD4, respectively. GNE-8025 allosterically disrupts the TEAD-YAP/TAZ interaction and inhibits TEAD-mediated oncogenic transcriptional programs via the Hippo signaling pathway. GNE-8025 suppresses YAP-driven tumor cell growth. GNE-8025 enhances the activity of MAPK and KRAS G12C inhibitors. GNE-8025 can be used for the research of pleural mesothelioma and KRAS G12C-mutant cancers .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
