TEAD

亜型選択性的な製品

TEAD製品

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  • TEAD阻害剤 (12)
  • 新製品
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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
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
S9735 MGH-CP1 MGH-CP1 is a potent and selective inhibitor of transcriptional enhanced associate domain (TEAD) palmitoylation. MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively.
EMBO Rep, 2024, 25(9):4033-4061
Sci Adv, 2023, 9(1):eadd0960
Sci Adv, 2023, 9(28):eadf9460
S8950 MYF-01-37 MYF-01-37 is a novel covalent inhibitor of TEAD targeting Cys380 when incubated with the TEAD2 protein.
Exp Dermatol, 2022, 31(10):1477-1499
E1483 IK-930 IK-930 is a selective, small-molecule inhibitor of TEAD that prevents palmitate binding and thereby disrupts aberrant TEAD-dependent transcription. IK-930 demonstrates antitumor activity in mouse xenograft models with Hippo pathway genetic alterations.
E1329 K-975 K-975 is a potent, selective and orally active TEAD inhibitor that directly inhibits YAP/TAZ-TEAD protein-protein interaction and shows a potent anti-tumor effect in malignant pleural mesothelioma.
Nat Commun, 2024, 15(1):8159
E4655New VT104 VT104 is an inhibitor of TEAD auto-palmitoylation that effectively blocks the palmitoylation of TEAD1 and TEAD3 proteins. It selectively inhibits YAP/TAZ-TEAD-promoted gene transcription and exhibits strong antitumor and anti-proliferative effects.
E1599 VT107 VT107 is an enantiomer analogous to VT10 and is a potent inhibitor of pan-TEAD auto-palmitoylation with IC50 of 4.93 nM that blocks TEAD-mediated gene transcription by preventing its association with YAP/TAZ.
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
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
S9735 MGH-CP1 MGH-CP1 is a potent and selective inhibitor of transcriptional enhanced associate domain (TEAD) palmitoylation. MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively.
EMBO Rep, 2024, 25(9):4033-4061
Sci Adv, 2023, 9(1):eadd0960
Sci Adv, 2023, 9(28):eadf9460
S8950 MYF-01-37 MYF-01-37 is a novel covalent inhibitor of TEAD targeting Cys380 when incubated with the TEAD2 protein.
Exp Dermatol, 2022, 31(10):1477-1499
E1483 IK-930 IK-930 is a selective, small-molecule inhibitor of TEAD that prevents palmitate binding and thereby disrupts aberrant TEAD-dependent transcription. IK-930 demonstrates antitumor activity in mouse xenograft models with Hippo pathway genetic alterations.
E1329 K-975 K-975 is a potent, selective and orally active TEAD inhibitor that directly inhibits YAP/TAZ-TEAD protein-protein interaction and shows a potent anti-tumor effect in malignant pleural mesothelioma.
Nat Commun, 2024, 15(1):8159
E4655New VT104 VT104 is an inhibitor of TEAD auto-palmitoylation that effectively blocks the palmitoylation of TEAD1 and TEAD3 proteins. It selectively inhibits YAP/TAZ-TEAD-promoted gene transcription and exhibits strong antitumor and anti-proliferative effects.
E1599 VT107 VT107 is an enantiomer analogous to VT10 and is a potent inhibitor of pan-TEAD auto-palmitoylation with IC50 of 4.93 nM that blocks TEAD-mediated gene transcription by preventing its association with YAP/TAZ.
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.
E4655New VT104 VT104 is an inhibitor of TEAD auto-palmitoylation that effectively blocks the palmitoylation of TEAD1 and TEAD3 proteins. It selectively inhibits YAP/TAZ-TEAD-promoted gene transcription and exhibits strong antitumor and anti-proliferative effects.
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.

TEAD阻害剤の選択性比較

Tags: TEAD inhibitor|TEAD agonist|TEAD activator|TEAD inducer|TEAD antagonist|TEAD signaling pathway|TEAD assay kit