YAP

YAP製品

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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
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
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
E1598New 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
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
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
E1598New 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.
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.
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
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.
E1598New 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.

YAP阻害剤の選択性比較

Tags: YAP antagonist | YAP inhibitor | YAP agonist | YAP activator