Search Result
Results for "
TEAD inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-155309
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YAP
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Cancer
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LM-41 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2. LM-41 inhibits migration of human MDA-MB-231 breast cancer cells .
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- HY-147088
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YAP
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Cancer
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TEAD-IN-2 is a novel, orally active inhibitor of transcriptional enhancer associate domain (TEAD) and modulates TEAD by ubiquitination and/or degradation by compounds. TEAD-IN-2 can be used for the research of a variety of diseases, disorders or conditions associated with TEAD .
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- HY-147135
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TEAD-IN-3
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YAP
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Cancer
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MYF-03-69 (TEAD-IN-3) is a potent and irreversible TEAD inhibitor. MYF-03-69 disrupts YAP-TEAD association, suppresses TEAD transcriptional activity and inhibits cell growth of Hippo signaling defective malignant pleural mesothelioma (MPM) .
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- HY-153811
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YAP-TEAD-IN-3
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YAP
Apoptosis
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Cancer
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IAG933 (YAP-TEAD-IN-3) is an orally available YAP/TAZ-TEAD inhibitor that has anti-tumor effects and promotes apoptosis. IAG933 YAP-TEAD-IN-3 inhibits Avi-human TEAD 4217-434, with an IC50 value of 9 nM .
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- HY-163173
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YAP
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Cancer
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TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
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- HY-161569
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YAP
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Cancer
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TEAD-IN-11 (compound 38) has a good inhibitory effect on TEAD1 (IC50=8.7 nM), TEAD2 (IC50=3.4 nM), TEAD3 (IC50=5.6 nnM). TEAD-IN-11 has good selective activity against TEAD1-3 as a covalent inhibitor. TEAD-IN-11 can be used for cancer research .
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- HY-161568
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YAP
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Cancer
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TEAD-IN-10 (compound 15) has good selective activity and inhibitory effect on TEAD1 (IC50=14 nM), TEAD2 (IC50=179 nM) and TEAD3 (IC50=4 nnM) as a covalent inhibitor. TEAD-IN-10 can be used for cancer research .
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- HY-155310
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YAP
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Cancer
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AF-2112 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2.
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- HY-161443
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YAP
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Cancer
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TEAD-IN-9 (compound 17) is a TEAD1 inhibitor with an IC50 of 0.29 μM. TEAD-IN-9 targets the palmitoyl pocket of TEAD, thereby effectively inhibiting the binding of YAP-TEAD and blocking the transcriptional function of YAP-TEAD .
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- HY-163732
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YAP
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Cancer
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TEAD-IN-16 (compound BC-011) is a potent inhibitor of TEAD, with the IC50 of 72.43 μM. TEAD-IN-16 plays an important role in cancer research .
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- HY-134955
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VT103
2 Publications Verification
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YAP
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Cancer
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VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer .
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- HY-147208
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YAP
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Cancer
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MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
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- HY-P2244
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YAP
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Cancer
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YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
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- HY-P2244A
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YAP
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Cancer
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YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of?YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
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- HY-158395
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YAP
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Cancer
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TEAD-IN-13 (64) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 3.2 h in mouse .
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- HY-158396
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YAP
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Cancer
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TEAD-IN-14 (75a) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 2.3 h in mouse .
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- HY-169316
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YAP
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Cancer
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YAP/TAZ inhibitor-4 (Compound 45) is an inhibitor of YAP/TAZ, exhibiting TEAD transcriptional activation inhibitory activity by suppressing the binding of YAP or TAZ to TEAD .
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- HY-125269
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YAP
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Cancer
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TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity .
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- HY-151525
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YAP
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Cancer
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YAP-TEAD-IN-2 (compound 6) is a potent YAP-TEAD PPI (protein-protein interaction) inhibitor with IC50 is 2.7 nM .
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- HY-158394
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YAP
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Cancer
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TEAD-IN-12 (58B) is an orally active TEAD inhibitor, with an IC50 of <100 nM and a half-life of 3.6 h in mouse .
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- HY-155338
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YAP
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Cancer
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SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .
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- HY-139603
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YAP
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Cancer
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MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction .
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- HY-168505
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YAP
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Cancer
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MSC-5046 is a selective TEAD1 inhibitor .
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- HY-B1221
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COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
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Inflammation/Immunology
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Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
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- HY-134956
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YAP
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Cancer
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VT104 is a potent and orally active YAP/TAZ inhibitor. VT104 prevents palmitoylation of endogenous TEAD1 and TEAD3 proteins. VT104 can be used in research of cancer .
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- HY-158342
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PROTACs
YAP
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Cancer
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PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
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- HY-147214
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YAP
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Cancer
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GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
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- HY-138565
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YAP
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Cancer
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K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma .
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- HY-126621
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YAP
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Cancer
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DC-TEADin02 is a potent TEAD autopalmitoylation inhibitor. DC-TEADin02 has TEAD autopalmitoylation inhibitory with the IC50 value of 197 nM. DC-TEADin02 can be used for the research of development, regeneration and tissue homeostasis .
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- HY-139330
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Apoptosis
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Cancer
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MGH-CP1 is a potent and orally active TEAD2 and TEAD4 auto-palmitoylation inhibitor with IC50s of 710 nM and 672 nM, respectively. MGH-CP1 can decrease the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion .
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- HY-B1221S
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Isotope-Labeled Compounds
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
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Inflammation/Immunology
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Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
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- HY-B1221S1
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Isotope-Labeled Compounds
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
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Inflammation/Immunology
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Flufenamic acid- 13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
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- HY-B1221R
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COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
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Inflammation/Immunology
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Flufenamic acid (Standard) is the analytical standard of Flufenamic acid. This product is intended for research and analytical applications. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
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- HY-B0990
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Bacterial
Antibiotic
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Infection
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Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation .
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- HY-162012
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YAP
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Cancer
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HC-258 (compound 26) binds with the cysteine in TEAD’s PA pocket. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells .
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- HY-163644
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Others
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Cancer
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VT-105 is a potent and selective TEAD autopalmitoylation inhibitor that inhibits proliferation and tumor growth in NF2-deficient mesothelioma.
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- HY-168506
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YAP
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Cancer
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MSC-1254 is a reversible, selective and covalent TEAD1 inhibitor. MSC-1254 can be used for the study of cancer .
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- HY-153585
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IK-930
1 Publications Verification
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YAP
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Cancer
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IK-930 (compound I-32) is a potent and orally active TEAD inhibitor with an EC50 value of <0.1 µM .
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- HY-168085
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YAP
Apoptosis
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Cancer
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CV-4-26 (Compound 22) is a covalent inhibitor of TEAD. CV-4-26 inhibits YAP/TEAD-based transcription, leading to the reduction of CTGF and CYR61 expression. CV-4-26 inhibits Huh7 and HepG2 cell colony formation, induces cell cycle arrest, and apoptosis. CV-4-26 shows antitumor activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB) .
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- HY-160657
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Others
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Others
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DC-TEADin04 has weak inhibitory activity against TEAD4 palmitoylation .
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- HY-150256
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YAP
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Cancer
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YTP-17 is an orally active YAP-TEAD protein-protein interaction inhibitor with an IC50 of 4 nM. YTP-17 shows anti-tumor efficacy .
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- HY-134957
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VT107
3 Publications Verification
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YAP
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Cancer
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VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer .
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- HY-147322
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YAP
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Cancer
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YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity .
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- HY-157083
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YAP
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Cancer
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mCMY020 is a covalent inhibitor of TEAD. mCMY020 effectively reduces YAP (Yes-associated protein)-driven transcription and selectively slows the proliferation of Hippo-deficient cancer cells. mCMY020 can be used in cancer research .
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- HY-134956B
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YAP
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Cancer
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(R)-VT104 is the R-enantiomer of VT104. (R)-VT104 shows an IC50 value of 0.1-1 μΜ for firefly luciferase. VT104 is an orally active and pan-TEAD auto-palmitoylation inhibitor .
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- HY-P1728
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YAP
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Cancer
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Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
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- HY-B0146
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Verteporfin
Maximum Cited Publications
172 Publications Verification
CL 318952
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YAP
Apoptosis
Autophagy
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Cancer
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Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis . Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation .
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- HY-P1728A
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YAP
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Cancer
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Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
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- HY-B0146R
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CL 318952 (Standard)
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YAP
Apoptosis
Autophagy
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Cancer
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Verteporfin (Standard) is the analytical standard of Verteporfin. This product is intended for research and analytical applications. Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis . Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2244
-
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YAP
|
Cancer
|
YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
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- HY-P2244A
-
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YAP
|
Cancer
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YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of?YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
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- HY-B0990
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Thiostrepton
Maximum Cited Publications
17 Publications Verification
|
Bacterial
Antibiotic
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Infection
|
Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation .
|
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- HY-P1728
-
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YAP
|
Cancer
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Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
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- HY-P1728A
-
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YAP
|
Cancer
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Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B1221S1
-
|
Flufenamic acid- 13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
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- HY-B1221S
-
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Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
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