S1786 |
Verteporfin
|
ベルテポルフィン (Verteporfin (CL 318952)) は、TEAD-YAP 相互作用 と YAP による肝肥大を阻害します。 また、ポルフィリンに由来する強力な第 2 世代の光増感剤でもあります。ベルテポルフィンはオートファジー (autophagy) 阻害剤です。 ベルテポルフィンは細胞増殖を阻害し、アポトーシス (apoptosis) を誘導します。 |
-
Acta Pharm Sin B, 2024, 14(3):1222-1240
-
Bone Res, 2024, 12(1):12
-
Cancer Lett, 2024, 587:216692
|
|
S8661 |
CA3 (CIL56)
|
CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS). |
-
Cell Rep, 2024, 43(4):114003
-
BMC Cancer, 2024, 24(1):587
-
FEBS Open Bio, 2024, 10.1002/2211-5463.13901
|
|
S8164 |
YAP-TEAD Inhibitor 1 (Peptide 17)
|
YAP-TEAD Inhibitor 1 (Peptide 17) is a YAP-TEAD protein-protein interaction inhibitor which has potential usage in treatment of YAP-involved cancers with IC50 of 25 nM. |
-
Development, 2024, 151(6)dev201621
-
J Cell Mol Med, 2023, 27(21):3217-3234
-
J Cancer, 2023, 14(13):2562-2573
|
|
S8554 |
Super-TDU
|
Super-TDU is an inhibitory peptide targeting YAP-TEADs interaction.
|
-
Matrix Biol, 2024, S0945-053X(24)00107-0
-
Gut Microbes, 2023, 15(1):2192501
-
Cell Death Discov, 2023, 9(1):424
|
|
S8184 |
Cytochalasin D
|
Cytochalasin D (Zygosporin A, NSC 209835) is a potent actin polymerization inhibitor derived from fungus. Cytochalasin D inhibits actin filament dynamics in cells. It induces phosphorylation and cytoplasmic retention of Yap. |
-
Cell Prolif, 2024, e13728.
-
Nat Commun, 2023, 14(1):7576
-
Adv Sci (Weinh), 2023, 10(7):e2205566
|
|
S8951 |
TED-347
|
TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD⋅Yap protein-protein interaction. TED-347 inhibits TEAD4⋅Yap1 protein-protein interaction with an apparent EC50 of 5.9 μM. |
-
Aging Cell, 2023, e13913.
-
Sci Adv, 2023, 9(28):eadf9460
-
Sci Adv, 2023, 9(28):eadf9460
|
|
S0881 |
Mitochonic acid 5 (MA-5)
|
Mitochonic acid 5 (MA-5) reduces mitochondrial apoptosis via upregulation of mitophagy. Mitochonic acid 5 regulates mitophagy via Bnip3 through the MAPK-ERK-Yap signaling pathway. Mitochonic acid 5 modulates mitochondrial ATP synthesis. |
-
Animals (Basel), 2024, 14(3):368.
-
Animals (Basel), 2024, 14(3)368
-
J Ovarian Res, 2022, 15(1):103
|
|
E1314 |
TDI-011536
|
TDI-011536 is a potent Lats kinase inhibitor that interrupts Hippo-Yap signaling and promotes proliferation of lesioned cardiac muscle cells. |
-
Nat Commun, 2024, 15(1):6953
-
Int J Mol Sci, 2024, 25(20)11234
-
bioRxiv, 2024, 2024.10.11.617852
|
|
S9861New |
PY-60
|
PY-60 is a small-molecule activator of the transcriptional coactivator Yes-associated protein (YAP) with EC50 of 1.6 µM, which acts by inhibiting a central scaffolding protein in the Hippo pathway, Annexin A2. It promotes the regenerative repair of cutaneous wounds in pig and human models. |
|
|
E1061 |
TRULI
|
TRULI inhibits both Lats1 and Lats2 with a IC50 of 0.2 nM, suppresses Yap phosphorylation, induces cell proliferation in several cell lines and tissues, and promotes the initial stages of proliferative regeneration of the sensory receptors in the inner ear. |
-
Nat Commun, 2024, 15(1):5449
-
Cell Rep, 2024, 43(4):114032
-
EMBO Rep, 2024, 25(9):4033-4061
|
|
E1563New |
GNE-7883
|
GNE-7883 is a potent and allosteric small-molecule inhibitor of pan-TEAD, that allosterically blocks the interactions between YAP/TAZ and all human TEAD paralogs through binding to the TEAD lipid pocket. It effectively reduces chromatin accessibility at TEAD motifs, suppresses cell proliferation in a variety of cell line models and achieves strong antitumor efficacy in vivo. Furthermore, it effectively overcomes KRAS G12C inhibitor resistance. |
|
|
E1490 |
IAG933
|
IAG933 (YAP-TEAD-IN-3) is a small molecule and acts as a YAP/TAZ-TEAD inhibitor. It also inhibits NCI-H2052 and can be used in research of tumor invasion and metastatic spread of solid tumors. |
-
FEBS Open Bio, 2024, 10.1002/2211-5463.13901
-
bioRxiv, 2024, 2024.09.18.613629
|
|
E1598 |
VT103
|
VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation with anti-proliferative and anti-tumor activity. It also inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation and disrupts interaction between YAP/TAZ and TEAD. |
|
|
S1786 |
Verteporfin
|
ベルテポルフィン (Verteporfin (CL 318952)) は、TEAD-YAP 相互作用 と YAP による肝肥大を阻害します。 また、ポルフィリンに由来する強力な第 2 世代の光増感剤でもあります。ベルテポルフィンはオートファジー (autophagy) 阻害剤です。 ベルテポルフィンは細胞増殖を阻害し、アポトーシス (apoptosis) を誘導します。 |
- Acta Pharm Sin B, 2024, 14(3):1222-1240
- Bone Res, 2024, 12(1):12
- Cancer Lett, 2024, 587:216692
|
|
S8661 |
CA3 (CIL56)
|
CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS). |
- Cell Rep, 2024, 43(4):114003
- BMC Cancer, 2024, 24(1):587
- FEBS Open Bio, 2024, 10.1002/2211-5463.13901
|
|
S8164 |
YAP-TEAD Inhibitor 1 (Peptide 17)
|
YAP-TEAD Inhibitor 1 (Peptide 17) is a YAP-TEAD protein-protein interaction inhibitor which has potential usage in treatment of YAP-involved cancers with IC50 of 25 nM. |
- Development, 2024, 151(6)dev201621
- J Cell Mol Med, 2023, 27(21):3217-3234
- J Cancer, 2023, 14(13):2562-2573
|
|
S8554 |
Super-TDU
|
Super-TDU is an inhibitory peptide targeting YAP-TEADs interaction.
|
- Matrix Biol, 2024, S0945-053X(24)00107-0
- Gut Microbes, 2023, 15(1):2192501
- Cell Death Discov, 2023, 9(1):424
|
|
S8184 |
Cytochalasin D
|
Cytochalasin D (Zygosporin A, NSC 209835) is a potent actin polymerization inhibitor derived from fungus. Cytochalasin D inhibits actin filament dynamics in cells. It induces phosphorylation and cytoplasmic retention of Yap. |
- Cell Prolif, 2024, e13728.
- Nat Commun, 2023, 14(1):7576
- Adv Sci (Weinh), 2023, 10(7):e2205566
|
|
S8951 |
TED-347
|
TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD⋅Yap protein-protein interaction. TED-347 inhibits TEAD4⋅Yap1 protein-protein interaction with an apparent EC50 of 5.9 μM. |
- Aging Cell, 2023, e13913.
- Sci Adv, 2023, 9(28):eadf9460
- Sci Adv, 2023, 9(28):eadf9460
|
|
E1314 |
TDI-011536
|
TDI-011536 is a potent Lats kinase inhibitor that interrupts Hippo-Yap signaling and promotes proliferation of lesioned cardiac muscle cells. |
- Nat Commun, 2024, 15(1):6953
- Int J Mol Sci, 2024, 25(20)11234
- bioRxiv, 2024, 2024.10.11.617852
|
|
E1061 |
TRULI
|
TRULI inhibits both Lats1 and Lats2 with a IC50 of 0.2 nM, suppresses Yap phosphorylation, induces cell proliferation in several cell lines and tissues, and promotes the initial stages of proliferative regeneration of the sensory receptors in the inner ear. |
- Nat Commun, 2024, 15(1):5449
- Cell Rep, 2024, 43(4):114032
- EMBO Rep, 2024, 25(9):4033-4061
|
|
E1563New |
GNE-7883
|
GNE-7883 is a potent and allosteric small-molecule inhibitor of pan-TEAD, that allosterically blocks the interactions between YAP/TAZ and all human TEAD paralogs through binding to the TEAD lipid pocket. It effectively reduces chromatin accessibility at TEAD motifs, suppresses cell proliferation in a variety of cell line models and achieves strong antitumor efficacy in vivo. Furthermore, it effectively overcomes KRAS G12C inhibitor resistance. |
|
|
E1490 |
IAG933
|
IAG933 (YAP-TEAD-IN-3) is a small molecule and acts as a YAP/TAZ-TEAD inhibitor. It also inhibits NCI-H2052 and can be used in research of tumor invasion and metastatic spread of solid tumors. |
- FEBS Open Bio, 2024, 10.1002/2211-5463.13901
- bioRxiv, 2024, 2024.09.18.613629
|
|
E1598 |
VT103
|
VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation with anti-proliferative and anti-tumor activity. It also inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation and disrupts interaction between YAP/TAZ and TEAD. |
|
|