Scientific Reviews
Product Guides
Blogs
Topics
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
26 Results for "
TEAD targets
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "TEAD targets" in MCE Product Catalog:
6
1
Cat. No.: HY-172113
H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM. H122 exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6 and 1.6 nM, respectively. H122 relies on binding to TEAD1 and CRBN, functional E3 ligase activity, and a functional proteasome for degradation.H122 induces degradation of TEAD3 and forms a ternary complex with TEAD4 and CRBN/DDB1 to mediate degradation.H122 downregulates expression of Myc target genes. H122 exhibits antitumor efficacy in MSTO-211H mouse xenograft models.H122 can be used for the research of malignant mesothelioma .
Cat. No.: HY-168016
CAS No.: 3058483-58-9
PROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC50=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma .
PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on CRBN and the proteasome system for TEAD2 degradation; disruption of CRBN binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer .
Cat. No.: HY-179505
CAS No.: 2866423-35-8
OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research .
Cat. No.: HY-158400
CAS No.: 2971850-47-0
Research Areas:
TEAD ligand 1 is the ligand for target protein TEAD. TEAD ligand 1 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) .
Cat. No.: HY-168704
Target:
Research Areas:
YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that inhibits the interaction between YAP/TAZ and TEAD. YAP/TAZ-TEAD-IN-2 suppresses the transcriptional activity of TEAD, with an IC50 of 1.2 nM. YAP/TAZ-TEAD-IN-2 inhibits YAP/TAZ-TEAD target genes expression (Cyr61, CTGF, AXL and Survivin) and breast cancer cell proliferation .
Cat. No.: HY-159912
CAS No.: 3027484-09-6
pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
Cat. No.: HY-179440
EA-C15 is a potent and selective TEAD inhibitor with an IC50 of 0.34 μM. EA-C15 covalently binds to the TEAD palmitoylation site, blocks palmitoylation and transcriptional activity, and inhibits YAP-dependent cancer cell proliferation and YAP-TEAD target gene (CTGF and CYR61) transcription. EA-C15 can be used for cancer research .
Cat. No.: HY-186118
Research Areas:
TEAD ligand 6 is a TEAD ligand. TEAD ligand 6 serves as a ligand for target protein for PROTAC (Ligands for Target Protein for PROTAC) and is used to develop and design PROTAC-based TEAD degraders, such as KG-FP-003 (HY-186117). TEAD ligand 6 applies to glioblastoma research .
Cat. No.: HY-181538
Research Areas:
TEAD ligand 3 (compound S20) is a TEAD ligand. As a target protein ligand, TEAD ligand 3 can be used in the synthesis of PROTAC TEAD1/IAP degrader-2 (HY-181537) .
Cat. No.: HY-181536
Research Areas:
TEAD ligand 2 is a target protein ligand that can be used for the synthesis of PROTACs, such as PROTAC TEAD1/IAP degrader-1 (HY-181534). PROTAC TEAD1/IAP degrader-1 is a potent TEAD1/IAP PROTAC degrader with anti-cancer activity .
Cat. No.: HY-181539
Research Areas:
TEAD ligand-Linker Conjugate 2 (compound S24) is a conjugate of TEAD‑targeted ligand and linker, which can be used for the synthesis of PROTAC TEAD1/IAP degrader-2 (HY-181537) .
Cat. No.: HY-179559
CAS No.: 2866423-06-3
OPN-9643 is a covalent inhibitor targeting the central palmitate binding pocket of TEADs with an IC50 of 15 nM, preventing autopalmitoylation and reducing TEAD-driven luciferase activity and canonical TEAD targets, CTGF and CYR61. OPN-9643 can be used for the research of cancer, such as melanoma .
Cat. No.: HY-186023
CAS No.: 2918762-34-0
Research Areas:
TEAD ligand-Linker Conjugate 1 is a synthetic target protein ligand-linker conjugate that can be used for the synthesis of PROTACs, such as PROTAC TEAD degrader-2 (HY-186021). PROTAC TEAD degrader-2 is a potent TEAD1 PROTAC degrader with anti-cancer activity .
Cat. No.: HY-181593
Research Areas:
IAP ligand-Linker Conjugate 2 is a synthetic target E3 ligase ligand-linker conjugate that can be used for the synthesis of PROTACs, such as PROTAC TEAD1/IAP degrader-3 (HY-181590). PROTAC TEAD degrader-2 is a potent TEAD1/IAP PROTAC degrader with anti-cancer activity .
Cat. No.: HY-190510
CAS No.: 3137325-81-3
Target:
Research Areas:
DF-CIV-2 is a TEAD2 inhibitor. DF-CIV-2 covalently modifies the TEAD2 palmitoylation pocket, inhibiting TEAD2 palmitoylation and YAP-TEAD binding. DF-CIV-2 inhibits YAP/TAZ-TEAD transcriptional output and downregulates Hippo target genes. DF-CIV-2 can be used for research on malignant mesothelioma .
- 1
- 2
-
-
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
