2. Search Result
Search Result
Results for "

TEAD degradation

" in MedChemExpress (MCE) Product Catalog:

31

Inhibitors & Agonists

3

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-172113
    H122

    		PROTACs YAP c-Myc Apoptosis Cancer
    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 .
    H122
  • HY-168016
    PROTAC YAP degrader-1

    		PROTACs YAP Cancer
    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 YAP degrader-1
  • HY-158342
    PROTAC TEAD degrader-1

    		PROTACs YAP Cancer
    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 .
    PROTAC TEAD degrader-1
  • HY-147088
    TEAD-IN-2

    		YAP Cancer
    TEAD-IN-2 is a novel, orally active inhibitor of transcriptional enhancer associate domain (TEAD) and modulates TEAD by ubiquitination and/or degradation by compounds. TEAD-IN-2 can be used for the research of a variety of diseases, disorders or conditions associated with TEAD .
    TEAD-IN-2
  • HY-158400
    TEAD ligand 1

    		Ligands for Target Protein for PROTAC YAP Cancer
    TEAD ligand 1 is the ligand for target protein TEAD. TEAD ligand 1 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) .
    TEAD ligand 1
  • HY-158343
    Thalidomide-NH-PEG2-C2-CH2

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-NH-PEG2-C2-CH2 is a conjugate of E3 ligase ligand and linker. Thalidomide-NH-PEG2-C2-CH2 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) .
    Thalidomide-NH-PEG2-C2-CH2
  • HY-186021
    PROTAC TEAD degrader-2

    		PROTACs YAP Cancer
    PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma .
    PROTAC TEAD degrader-2
  • HY-181590
    PROTAC TEAD1/IAP degrader-3

    		PROTACs SNIPERs YAP IAP Cancer
    PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma .
    PROTAC TEAD1/IAP degrader-3
  • HY-181534
    PROTAC TEAD1/IAP degrader-1

    		PROTACs YAP IAP SNIPERs Cancer
    PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma .
    PROTAC TEAD1/IAP degrader-1
  • HY-181594
    PROTAC TEAD/IAP degrader-1

    		PROTACs SNIPERs YAP Cancer
    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 .
    PROTAC TEAD/IAP degrader-1
  • HY-181536
    TEAD ligand 2

    		Ligands for Target Protein for PROTAC YAP Cancer
    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 .
    TEAD ligand 2
  • HY-181537
    PROTAC TEAD1/IAP degrader-2

    		PROTACs SNIPERs YAP IAP Cancer
    PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research .
    PROTAC TEAD1/IAP degrader-2
  • HY-186023
    TEAD ligand-Linker Conjugate 1

    		Target Protein Ligand-Linker Conjugates Cancer
    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 .
    TEAD ligand-Linker Conjugate 1
  • HY-181593
    IAP ligand-Linker Conjugate 2

    		E3 Ligase Ligand-Linker Conjugates Cancer
    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 .
    IAP ligand-Linker Conjugate 2
  • HY-181538
    TEAD ligand 3

    		Ligands for Target Protein for PROTAC YAP Others
    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) .
    TEAD ligand 3
  • HY-181530
    IAP ligand 6

    		IAP Cancer
    IAP ligand 6 (A250) is an IAP ligand with a Ka value of 0.1 μM for the human XIAP BIR3 domain. IAP ligand 6 binds to the XIAP BIR3 domain and serves as an alkynylpyridine scaffold for the preparation of TEAD degraders that recruit IAP. IAP ligand 6 is applicable to research related to mesothelioma .
    IAP ligand 6
  • HY-186022
    YAP/TAZ-TEAD-IN-3

    		Ligands for Target Protein for PROTAC YAP Cancer
    YAP/TAZ-TEAD-IN-3 is a YAP/TAZ-TEAD interaction inhibitor with an IC50 of 1.8 nM. YAP/TAZ-TEAD-IN-3 can be used as a TEAD1 ligand to construct PROTACs, such as PROTAC TEAD degrader-2 (HY-186021) .
    YAP/TAZ-TEAD-IN-3
  • HY-181539
    TEAD ligand-Linker Conjugate 2

    		Target Protein Ligand-Linker Conjugates YAP Others
    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) .
    TEAD ligand-Linker Conjugate 2
  • HY-185230
    HC278

    		PROTACs YAP Cancer
    HC278 is a selective TEAD1/TEAD3 PROTAC degrader. HC278 induces proteasome-dependent degradation by forming a stable ternary complex with CRBN/DDB1. HC278 is applicable to the research of mesothelioma .
    HC278
  • HY-181595
    TEAD ligand 5

    		Ligands for Target Protein for PROTAC YAP Cancer
    TEAD ligand 5 (Compound S19) is a TEAD PROTAC ligand. TEAD ligand 5 can be conjugated with E3 ligase Ligand (HY-181531) and linker (HY-181608) to synthesize PROTAC TEAD/IAP degrader-1 (HY-181594) .
    TEAD ligand 5
  • HY-186117
    KG-FP-003

    		YAP PROTACs Cancer
    KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer .
    KG-FP-003
  • HY-181592
    TEAD ligand 4

    		Ligands for Target Protein for PROTAC YAP Cancer
    TEAD ligand 4 is a TEAD PROTAC ligand. TEAD ligand 4 can be conjugated with E3 ligase Ligand (HY-181591) and linker to synthesize PROTAC TEAD1/IAP degrader (HY-181590) .
    TEAD ligand 4
  • HY-186118
    TEAD ligand 6

    		Ligands for Target Protein for PROTAC YAP Neurological Disease Cancer
    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 .
    TEAD ligand 6
  • HY-181535
    IAP ligand-Linker Conjugate 1

    		E3 Ligase Ligand-Linker Conjugates IAP Others
    IAP ligand-Linker Conjugate 1 is a ligand-linker conjugate targeting IAP, which can be used in the synthesis of PROTAC TEAD1/IAP degrader-1 (HY-181534) .
    IAP ligand-Linker Conjugate 1
  • HY-181607
    TEAD ligand-Linker Conjugate 3

    		YAP Others
    TEAD ligand-Linker Conjugate 3 (the blue structure + black structure of A536 in the literature) is a conjugate of a TEAD1-targeting ligand and a linker. TEAD ligand-Linker Conjugate 3 can be coupled with an IAP ligand (HY-181531) to form an IAP-recruiting bifunctional protein degrader (IPD) (HY-181594), also known as a SNIPER degrader. This TEAD SNIPER simultaneously binds to the TEAD1 palmitoylation pocket and the BIR3 domain of cIAP1 to form a ternary complex, efficiently inducing the ubiquitination and degradation of both TEAD1 and cIAP1 (DC50=110 nM, Dmax=51%; IC50=122 nM for cIAP1). TEAD ligand-Linker Conjugate 3 and its synthesized SENIPER molecule can be utilized in research on Hippo pathway dysregulation-related diseases, such as NF2-mutant tumors .
    TEAD ligand-Linker Conjugate 3
  • HY-W803227
    1-(2-Chloro-acetyl)-piperazine

    		PROTAC Linkers Cancer
    1-(2-Chloro-acetyl)-piperazine is a PROTAC linker. 1-(2-Chloro-acetyl)-piperazine can be used to synthesize PROTAC TEAD1/IAP degrader-2 (HY-181537) .
    1-(2-Chloro-acetyl)-piperazine
  • HY-181531
    IAP ligand 7

    		Ligands for E3 Ligase IAP Cancer
    IAP ligand 7 is an E3 ligase ligand. IAP ligand 7 can be conjugated with TEAD ligand (HY-181595) and linker (HY-181608) to synthesize PROTAC TEAD/IAP degrader-1 (HY-181594) .
    IAP ligand 7
  • HY-181591
    IAP ligand 10

    		Ligands for E3 Ligase Cancer
    IAP ligand 10 is an E3 ligase ligand (E3 ligase ligand). E3 ligase Ligand 58 can be used for the synthesis of PROTAC TEAD1/IAP degrader-3 (HY-181590) .
    IAP ligand 10
  • HY-181532
    IAP ligand 8

    		Ligands for E3 Ligase IAP Cancer
    IAP ligand 8 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 8 selectively targets cIAP1-BIR3, XIAP-BIR2 (with a KD of 15.8 nM for both). IAP ligand 8 serves as an IAP ligand moiety to synthesize IAP-recruiting protein degrader (IPD) (HY-181590). This IPD simultaneously forms two ternary complexes, cIAP1-A538-TEAD1 and XIAP-A538-TEAD1, and efficiently degrades TEAD1 via a dual E3 recruitment mechanism, while inducing the autodegradation of cIAP1. IAP ligand 8 and its series of degraders are applicable to targeted research on Hippo pathway-dysregulated cancers such as NF2-mutant mesothelioma .
    IAP ligand 8
  • HY-181533
    IAP ligand 9

    		Ligands for E3 Ligase IAP Cancer
    IAP ligand 9 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 9 selectively targets cIAP1-BIR3, XIAP-BIR3, exhibits extremely weak binding affinity for XIAP-BIR2, with a KD of 100 nM for cIAP1-BIR3 and 10 nM for XIAP-BIR2. IAP ligand 9 can be used to synthesize IAP-recruiting protein degraders (IPD), and can calibrate the cell permeability and cellular-level target binding assays of the IPD molecule SNIPER (TEAD)-1 (HY-181607). IAP ligand 9 and its series of degraders can be used in the research of solid tumors such as malignant pleural mesothelioma associated with abnormal activation of the Hippo pathway .
    IAP ligand 9
  • HY-186119
    E3 Ligase Ligand-linker Conjugate 228

    		E3 Ligase Ligand-Linker Conjugates Neurological Disease Cancer
    E3 Ligase Ligand-linker Conjugate 228 is an E3 ligase CRBN ligand-linker conjugate composed of 2-(4-(2,4-Dioxotetrahydropyrimidin-1 (2H)-yl)-3-methylphenoxy) acetic acid (HY-W733199) and a linker. E3 ligase ligand-linker conjugates can be used to synthesize degraders of PROTAC TEAD, such as KG-FP-003 (HY-186117). E3 Ligase Ligand-linker Conjugate 228 can be applied to glioblastoma research .
    E3 Ligase Ligand-linker Conjugate 228

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: