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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
13 Results for "
TEAD4 inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "TEAD4 inhibitors" in MCE Product Catalog:
12
12 Publications Verification
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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2 Cited Publications
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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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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1 Cited Publications
MYF-03-176 is an orally active inhibitor of TEAD, and suppresses TEAD transcriptional activity with an IC50 of 11 nM. The IC50 values of MYF-03-176 for TEAD1, TEAD3, and TEAD4 are 47, 32, and 71 nM, respectively. MYF-03-176 inhibits hippo signaling defective malignant pleural mesothelioma (MPM) cells. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model .
Cat. No.: HY-172932
CAS No.: 3007592-85-7
TEAD-IN-20 is a TEAD inhibitor. The IC50 values of TEAD-IN-20 in TEAD4 FRET and TEAD4 MCF7-Tead cell lines are 0.021 and 0.044 μM, respectively. TEAD-IN-20 can be used in cancer research .
Cat. No.: HY-173139
TEAD-IN-19 (Compound 1l) is a transcriptional inhibitor of TEAD, exhibiting inhibition rates of 38.5%, 36.2%, 57.8%, and 71.3% against TEAD1, TEAD2, TEAD3, and TEAD4, respectively, at a concentration of 10 μM. TEAD-IN-19 shows potent anti-proliferative and anti-migratory activities in prostate cancer cell lines and significantly reduces the expression of TEAD-regulated downstream genes. TEAD-IN-19 holds promise for research in the field of cancer therapy .
Cat. No.: HY-179706
CAS No.: 2576427-49-9
VS3 is a YAP-TEAD interaction inhibitor. VS3 directly disrupts the interaction between YAP-TEAD by binding to TEAD4 Interface 3 (Kd = 6 μM) on the surface. VS3 exhibits anti-proliferative activity against HT29, HCT116, and A2780. VS3 can be used for research on colorectal adenocarcinoma and ovarian cancer .
Cat. No.: HY-183753
LC-TD-05 is a non-covalent inhibitor of TEAD1, TEAD2 and TEAD4, with IC50 values of 116.6 nM, 168.7 nM and 68.3 nM, respectively; it shows weak activity against TEAD3, with a human IC50 of 1261.0 nM. LC-TD-05 induces apoptosis in hepatocellular carcinoma cells. LC-TD-05 can be used for the research of hepatocellular carcinoma .
Cat. No.: HY-181594
PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma .
Cat. No.: HY-187181
CAS No.: 2933893-78-6
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Research Areas:
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-147209
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Research Areas:
DC-TEAD3in03 is a subtype-selective and covalent TEAD3 inhibitor with an IC50 of 0.16 μM. DC-TEAD3in03 exhibits the inhibitory activity on TEAD1/2/4 reduced by more than 100 times. DC-TEAD3in03 has the IC50 for TEAD3 of 1.15 μM in the GAL4-TEAD reporter gene experiment in cells, and it does not interfere with the β-catenin pathway. DC-TEAD3in03 reduces the growth rate of the zebrafish tail fin. DC-TEAD3in03 can be used to study the proportional growth of appendages in vertebrates .
Cat. No.: HY-187180
CAS No.: 2933893-27-5
Research Areas:
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 .
Cat. No.: HY-189200
CAS No.: 3006101-94-3
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Research Areas:
AZ'4331 is an orally active pan-TEAD family inhibitor, with an IC50 of 0.381 μM against TEAD1, 0.020 μM against TEAD2, 0.014 μM against TEAD3, and 0.031 μM against TEAD4. AZ'4331 slows cell cycle progression. AZ'4331 exerts effects in cancer xenograft models with dysregulated Hippo pathway. AZ'4331 can be used to study cancers with altered Hippo pathways, including mesothelioma, head and neck squamous cell carcinoma, and EGFR-mutant non-small cell lung cancer .
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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
