Search Result
Results for "
4-1BB Ligand Inhibitors
" in MedChemExpress (MCE) Product Catalog:
2819
Inhibitors & Agonists
49
Biochemical Assay Reagents
34
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P99572
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BNT-312; DuoBody-CD40x-4-1BB; GEN1042
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TNF Receptor
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Inflammation/Immunology
Cancer
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Tecaginlimab (BNT-312) is a Fc-inert bispecific antibody for dual targeting and conditional stimulation of CD40 and 4-1BB. Tecaginlimab can enhance priming and reactivation of tumor-specific immunity .
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-
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- HY-P99119
-
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TNF Receptor
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Inflammation/Immunology
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Anti-Mouse 4-1BB/CD137 Antibody (3H3) is an IgG2a antibody agonist against mouse 4-1BB, derived from a rat host, capable of stimulating 4-1BB signaling in vivo.
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-
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- HY-P99605
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PRS 343
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EGFR
TNF Receptor
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Cancer
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Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research .
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- HY-P99419
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GEN1046
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PD-1/PD-L1
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Cancer
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Acasunlimab (GEN1046) is a bispecific antibody (bsAb) targeting PD-L1 and 4-1BB. Acasunlimab enhances T-cell and NK-cell function through conditional 4-1BB stimulation while constitutively blocking the PD-1/PD-L1 inhibitory axis. Acasunlimab can be used in research of cancer .
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-
-
- HY-P990067
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ATOR-1017
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TNF Receptor
|
Cancer
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Evunzekibart (ATOR-1017) is an Fc-γ receptor conditional 4-1BB agonist and IgG4-type antibody. Evunzekibart can be used as monotherapy or in combination with anti-PD1 to exert anticancer activity.
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- HY-161575
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-
-
- HY-161537
-
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EGFR
|
Cancer
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EGFR ligand-9 is an EGFR ligand. EGFR ligand-9 can be used for synthesis of PROTAC EGFR degrader 9 (HY-161536) .
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-
-
- HY-P990017
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CD19-4-1BBL; RO7227166; RG6076
|
CD19
|
Cancer
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Englumafusp alfa (CD19-4-1BBL; RO7227166) is a fusion construct comprised of a CD19-specific antibody domain fused to a trimerized extracellular domains of human 41BBL. Englumafusp alfa promotes CD19-specific 4-1BB cross-linking on the surface of T and NK cells .
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-
- HY-P990809
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TNF Receptor
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Others
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Anti-Mouse 4-1BB/CD137 Antibody (LOB12.3) is a kind of rat IgG1 kappa in vivo mouse antibody, targeting to 4-1BB/CD137. The recommend isotype control of Anti-Mouse 4-1BB/CD137 Antibody (LOB12.3): Rat IgG1 kappa, Isotype Control (HY-P99979).
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-
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- HY-P99119A
-
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Transmembrane Glycoprotein
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Others
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Anti-Mouse 4-1BB/CD137 (LALA-PG) Antibody (LOB12.3) is a mouse-derived IgG2a, κ type antibody agonist, targeting to mouse 4-1BB/CD137.
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- HY-161829
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-
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- HY-161598
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-
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- HY-75578
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-
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- HY-W342590
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Ligands for E3 Ligase
|
Cancer
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CRBN ligand-9 (Compound 4d) is a CRBN ligand (Ki: 8.9 μM). CRBN ligand-9 can be used for synthesis of PROTACs .
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- HY-161830
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-
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- HY-168658
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-
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- HY-158771
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-
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- HY-168633
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Bombesin Receptor
PSMA
|
Cancer
|
PSMA/GRPR ligand 1 (compound 3 ) is a bispecific PSMA/GRPR ligand that shows dual targeting for PSMA(+) and GRPR(+) tumors .
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- HY-168314
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-
-
- HY-164925
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-
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- HY-103597
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Cereblon Ligand 3; E3 ligase Ligand 3
|
Ligands for E3 Ligase
Autophagy
Apoptosis
|
Others
|
Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs .
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-
-
- HY-158677
-
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Bcl-2 Family
|
Cancer
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BcI-2/BcI-xI ligand 1 is a BcI-2/BcI-xI ligand, and can be used for synthesis of PROTAC BcI-2/BcI-xI Degrader-1 (HY-158551) .
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-
-
- HY-146441
-
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STAT
|
Cardiovascular Disease
Inflammation/Immunology
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Prohibitin ligand 1 (Compound 22i), a cardioprotectant prohibitin ligand, induces a phosphorylation of the pro-survival factor STAT3. Prohibitin ligand 1 exhibits in vitro cardioprotectant activities at nanomolar concentrations .
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- HY-168302
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-
-
- HY-168691
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-
-
- HY-168283
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-
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- HY-156595
-
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BCL6
|
Neurological Disease
|
BCL6 ligand-1 (compound I-94) is a ligand for TCIP 1 (HY-156531). TCIP 1 is a BCL6 inhibitor that activates apoptosis and is used in cancer research .
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- HY-145484
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-
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- HY-150859
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-
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- HY-168299
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-
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- HY-168683
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-
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- HY-150905
-
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EGFR
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Cancer
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EGFR ligand-2 (compound C4), a covalent EGFR ligand, is a EGFR mutant inhibitor with IC50s of 21 nM and 48 nM for EGFR L858R and EGFR L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .
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-
-
- HY-168671
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-
-
- HY-168296
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-
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- HY-170304
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Ligands for E3 Ligase
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Cancer
|
E3 ligase Ligand 44 is a ligand for E3 ligase, used for the synthesis of PROTAC AR Degrader-7 (HY-160221) .
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- HY-168271
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-
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- HY-133045
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Ligands for E3 Ligase
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Cancer
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VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
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- HY-168685
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-
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- HY-168191
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-
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- HY-168700
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-
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- HY-170303
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-
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- HY-44824
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-
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- HY-169487
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-
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- HY-168230
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-
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- HY-47709
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-
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- HY-169152
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-
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- HY-168226
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Ligands for E3 Ligase
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Others
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E3 ligase Ligand 34 is the E3 ligase ligand part of PROTAC SMARCA2/4-degrader-35 (HY-168225) and can be utilized in the synthesis of PROTACs .
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-
- HY-168638
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-
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- HY-168275
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-
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- HY-168056
-
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Others
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Others
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KRAS ligand 5 is the target protein ligand for PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can specifically degrade KRAS mutated proteins .
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- HY-147366
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Lipocalin Family
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Metabolic Disease
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RBP4 ligand-1 is a non-retinoid ligands for (RBP4) retinol-binding protein 4. The hRBP4SPA IC50 and RBP4–TTR FRET IC50 values are 0.23±0.11 and 0.13±0.12 μM in the radioligand binding assay and FRET assay, respectively .
|
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- HY-150407
-
|
Ligands for Target Protein for PROTAC
Autophagy
|
Others
Neurological Disease
Cancer
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TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration .
|
-
- HY-125905
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VHL Ligand 3; E3 ligase Ligand 19
|
Ligands for E3 Ligase
|
Cancer
|
VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4 .
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- HY-151479
-
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Ligands for Target Protein for PROTAC
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Cancer
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GID4 Ligand 3 (compound 16) is a binder of GID4 with an Kd value of 110 μM in vitro and an IC50 value of 148.5 μM. GID4 Ligand 3 can be used for the research related to cereblon and Von Hippel-Lindau .
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- HY-168702
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- HY-168695
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- HY-168288
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- HY-168562
-
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Sigma Receptor
|
Neurological Disease
Cancer
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σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
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- HY-43869
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PSMA-617 Ligand-Linker Conjugate
|
ADC Linker
|
Cancer
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Vipivotide tetraxetan Ligand-Linker Conjugate (PSMA-617 Ligand-Linker Conjugate) is a complex composed of pharmacophore group Glutamate-urea-Lysine peptide coupling linker, which can be used to synthesize Vipivotide tetraxetan (PSMA-617). Glutamate-urea-Lysine selectively binds to prostate-specific membrane antigen (PSMA) .
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- HY-168611
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- HY-145308
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- HY-150839
-
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand PG is a E3 ligase ligand that can be used in the recruitment of CRBN protein. E3 ligase Ligand PG exhibits potent binding activity with CRBN (IC50 of 2.191 μM). E3 ligase Ligand PG can be connected to the BMS-202 (HY-19745) by a linker to form PROTAC, PROTAC PD-L1 degrader-1 (HY-163757) .
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- HY-162125
-
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Angiotensin Receptor
|
Cardiovascular Disease
|
AT2 receptor ligand-1(compound 14) is a potent angiotensin AT2 receptor ligand with the Ki 4.9 nM. AT2 receptor ligand-1 shows high stability in microsomes of the sulfonamide ligands .
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- HY-133073
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CCR7-Cmp2105
|
CCR
Ligands for Target Protein for PROTAC
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Cancer
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CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM .
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- HY-159492
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5-HT Receptor
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Neurological Disease
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5-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for 5-HT7R (Ki=178 nM). 5-HT7 receptor ligand 2 has good membrane permeability, low hepatotoxicity and cardiotoxicity, and high plasma protein binding. 5-HT7 receptor ligand 2 shows neuroprotective effects in SH-SY5Y cells and can be used for the study of central nervous system related diseases .
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- HY-161483
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Epigenetic Reader Domain
Histone Acetyltransferase
|
Neurological Disease
Cancer
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CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function .
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- HY-101763A
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VH032-NH2 monohydrochloride; VHL Ligand 1 monohydrochloride
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2; VHL ligand 1) hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein .
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- HY-161693
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G-quadruplex
DNA/RNA Synthesis
Apoptosis
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Cancer
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Telomeric G4s ligand 1 is a telomeric G-quadruplex ligand that stabilizes telomeric G4 and induces R-loop formation, leading to DNA damage responses. Telomeric G4s ligand 1 induces apoptosis and evokes immunogenic cell death (ICD) in tumor cells .
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- HY-126456
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VH032-propargyl; VHL Ligand 7
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-propargyl (VH032-propargyl) is a VHL ligand which is used in “click reaction” for PROTACs . (S,R,S)-AHPC-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-P1840A
-
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Neuropeptide Y Receptor
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Neurological Disease
Endocrinology
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Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 TFA exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
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- HY-P1840
-
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Neuropeptide Y Receptor
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Neurological Disease
Endocrinology
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Galanin Receptor Ligand M35 is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
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- HY-133046
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader . VHL Ligand-Linker Conjugates 17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-115953
-
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Dopamine Receptor
|
Neurological Disease
|
Dopamine D3 receptor ligand is a potent, selective and high affinity ligand for Dopamine D3 receptor with 89-fold selective for D3 over D2 (D3 Ki= 8 nM, D2 Ki= 715 nM) .
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- HY-168316
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- HY-128809
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E3 ligase Ligand 11
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Ligands for E3 Ligase
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Cancer
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cIAP1 ligand 2 is the LCL161 derivative based IAP ligand. cIAP1 ligand 2 can be connected to the ABL ligand for protein by a linker to form SNIPER.
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- HY-128808
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E3 ligase Ligand 12
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Ligands for E3 Ligase
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Cancer
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cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER.
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- HY-49421
-
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Ligands for Target Protein for PROTAC
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Cancer
|
BTK ligand 12 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BTK ligand 12 can serve as an active control for the target protein ligand of NRX-0492 (HY-153357) .
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- HY-169969
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- HY-168387
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- HY-161808
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-
- HY-161790
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- HY-158400
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- HY-150885
-
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Ligands for Target Protein for PROTAC
Btk
|
Cancer
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BTK ligand 1 (compound 1) is a ligand targeting Bruton’s tyrosine kinase (Btk). BTK ligand 1 can combine with E3 ligase ligand (Ligand for E3 Ligase) through PROTAC Linker to form PROTAC. PROTACs targeting Btk can be used in the study of chronic lymphocytic leukemia (CLL) and other BK cell malignancies .
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- HY-169049
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-
- HY-161807
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-
- HY-103596
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Cereblon Ligand 2; E3 ligase Ligand 2
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Ligands for E3 Ligase
Autophagy
Apoptosis
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Cancer
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Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs .
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- HY-162841
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-
- HY-128837
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MDM2 Ligand 1; E3 ligase Ligand 16
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Ligands for E3 Ligase
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Cancer
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Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTAC .
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- HY-169361
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- HY-146102
-
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mAChR
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Others
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M1 ligand 1 (compound 3b-b) is a muscarinic acetylcholine receptor M1 ligand. M1 ligand 1 is a N-desmethyl congener of arecoline derivative. M1 ligand 1 can be used as PET (positron emission tomography) radiotracer .
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- HY-158126
-
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DNA/RNA Synthesis
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Cancer
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G-quadruplex ligand 2 (compound A3) is a triphenylamine-based ligand that targets mitochondrial DNA G4s. G-quadruplex ligand 2 activates the cGAS-STING pathway. G-quadruplex ligand 2 inhibits tumor growth and metastasis via regulation of TME .
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- HY-123977
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Ras
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Cancer
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RasGRP3 ligand 1 (compound 96) is a RasGRP3 ligand with a Ki of 1.75 nM. RasGRP3 ligand 1 can induce Ras activation and can be used for cancer research .
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- HY-168542
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- HY-169277
-
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Others
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Others
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PXR Ligand 1 is a PXR Ligand and can be used for synthesis of SJYHJ-026 (HY-169264) PROTACs .
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- HY-41547
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Cereblon Ligand 4; E3 ligase Ligand 4
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Ligands for E3 Ligase
Autophagy
Apoptosis
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Cancer
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Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966) .
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- HY-156994
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LYTACs
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Others
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ASGPR ligand-1 is an asialoglycoprotein receptor (ASGPR) ligand compound. ASGPR ligand-1 can be used for kinds of diseases research .
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- HY-139656
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- HY-141724
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PCSK9
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Cancer
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PCSK9 ligand 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) ligand. PCSK9 ligand 1 does not affect PCSK9 function .
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- HY-128807
-
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-129653
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-128811
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-43961
-
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-128810
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-103602B
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VH032-PEG3-NH2 dihydrochloride; VHL Ligand-Linker Conjugates 1 dihydrochloride; E3 ligase Ligand-Linker Conjugates 5 dihydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG3-NH2 dihydrochloride (VH032-PEG3-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology
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- HY-159465
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- HY-163927
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- HY-169978
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- HY-128806
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-150799
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- HY-W453397
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- HY-168292
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- HY-139906
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- HY-150803
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Ligands for E3 Ligase
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Cancer
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VHL Ligand 14 (Compound 11) is a VHL ligand for design of PROTAC estrogen receptor α (ERα) degraders, with a binding affinity IC50 of 196 nM .
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- HY-168545
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- HY-161959
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- HY-169989
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Ligands for E3 Ligase
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Cancer
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CRBN ligand-11 is the E3 ubiquitin ligase ligand for CFT8634 (HY-145925B). CRBN ligand-11 can be used for the synthesis of PROTACs .
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- HY-162973
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- HY-157417
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DNA/RNA Synthesis
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Others
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G-quadruplex ligand 1, a G-quadruplex ligand, disrupts G-Quadruplex DNA structure and enhances gene expression .
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- HY-146125
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Endonuclease
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Metabolic Disease
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CGCG/CGG ligand 1 (compound 10), an anthracenone derivative, is a CGCG or CGG short spacer-ligand. CGCG/CGG ligand 1 can protect cleavable sites of DNA with the multiple CGCG or continuous CGG sites from the restriction enzyme .
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- HY-161234
-
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Ras
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Cancer
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KRAS ligand 3 (compound 1) is BTX-6654 target-binding ligand that can bind KRAS inhibitor and diaplay synergistic tumor growth inhibiton .
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- HY-169280
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- HY-168727
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Kinesin
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Cancer
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KSP ligand 1 is a protein ligand that targets KSP (Kinesin), and it can be used to synthesize PROTAC KSP-IN-1 (HY-168725) for cancer research .
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- HY-162855
-
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Ligands for E3 Ligase
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Cancer
|
E3 ligase Ligand 33 (56-9B) is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 33 can be used in anti-cancer research .
|
-
- HY-161651A
-
|
Epigenetic Reader Domain
|
Cancer
|
BRD4 ligand 6 TFA is the TFA salt form of BRD4 ligand 6 (HY-161651). BRD4 ligand 6 TFA is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .
|
-
- HY-114399
-
-
- HY-401613
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 43 serves as the E3 ubiquitin ligase ligand for ACBI3 (HY-157228). E3 ligase Ligand 43 can be utilized for the synthesis of PROTACs .
|
-
- HY-168676
-
-
- HY-W733176
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 50 is the ligand for E3 ligase Cereblon. E3 ligase Ligand 50 can be used for synthesis of PROTAC BTK Degrader-10 (HY-160966) .
|
-
- HY-170330
-
-
- HY-170334
-
-
- HY-168176
-
|
PROTACs
HDAC
|
Cancer
|
HDAC8 ligand 1 is a PROTAC target protein-ligand of PROTAC HDAC8 Degrader-2 (HY-168174) .
|
-
- HY-159076
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 7 (Compound 6) is a ligand for E3 ligase. E3 ligase Ligand 7 can be utilized for the synthesis of PROTAC BET Degrader-12 (HY-158764) .
|
-
- HY-159660
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 31 is a ligand for E3 ubiquitinase. E3 ligase Ligand 31 can be used to synthesize PTOTAC HSD17B13 degrader 1 (HY-159651) .
|
-
- HY-W382038
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 32 (First product in Example 52) is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 32 can be connected to the ligand for protein by a linker to form PROTACs and can be used for the synthesis of PROTAC SMARCA2/4-degrader-29 (HY-162743) .
|
-
- HY-W1003189
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 42 is an E3 ubiquitin ligase ligand. E3 ligase Ligand 42 can be connected to the target protein ligand through a linker and can be used to synthesize PROTAC AR Degrader-6 (HY-156751). PROTAC can induce ubiquitination degradation of cancer-promoting proteins .
|
-
- HY-134724
-
-
- HY-170452
-
-
- HY-170339
-
-
- HY-158433
-
-
- HY-161711
-
-
- HY-161990
-
-
- HY-49393
-
-
- HY-48932
-
-
- HY-154844
-
|
Biochemical Assay Reagents
|
Cancer
|
FAP Ligand 1 (FL), a high-affinity FAP small-molecule ligand, is used to target attached drugs to FAP-expressing fibroblasts and can be used in radiation imaging studies of targeted cancers .
|
-
- HY-161791
-
-
- HY-170671
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 49 serves as the E3 ubiquitin ligase ligand for PROTAC XPO1 degrader-1 (HY-170669). E3 ligase Ligand 49 can be utilized for the synthesis of PROTACs .
|
-
- HY-158340
-
-
- HY-170341
-
-
- HY-49537
-
-
- HY-168038
-
-
- HY-159544
-
-
- HY-159542
-
-
- HY-150410
-
|
AUTACs
|
Cancer
|
TSPO ligand-3 is a ligand of AUTAC2. AUTAC2 contains an p-fluorobenzylguanine (FBnG) and an synthetic ligand of FKBP (SLF) moiety, which can cause significant silencing of FKBP12 in HeLa cells .
|
-
- HY-169988
-
|
Ligands for Target Protein for PROTAC
|
Cancer
|
BRD9 ligand-5 (Compound 172-11) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BRD9 ligand-5 can be utilized for the synthesis of CFT8634 (HY-145925B) .
|
-
- HY-169482
-
-
- HY-168697
-
-
- HY-168305
-
-
- HY-169954
-
|
Ligands for E3 Ligase
|
Cancer
|
CRBN ligand-10 (compound 18) is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC .
|
-
- HY-168293
-
-
- HY-161960
-
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
|
Cancer
|
EP300/CBP ligand 2 (compound S19) is a ligand targeting the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). EP300/CBP ligand 2 can be used as a target protein ligand in the PROTAC structure, and can be coupled to the E3 ubiquitin ligase ligand through the PTOTAC Linker to synthesize PROTAC molecules with degradation effects. For example, EP300/CBP ligand 2 can be coupled with the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc (HY-161961) to produce the PROTAC molecule dCE-2 (HY-161958) .
|
-
- HY-170450
-
-
- HY-170373
-
-
- HY-161651
-
|
Epigenetic Reader Domain
|
Cancer
|
BRD4 ligand 6 is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .
|
-
- HY-170371
-
-
- HY-169967
-
-
- HY-168319
-
-
- HY-162411
-
|
Others
|
Cancer
|
E3 ligase Ligand 24 (Compound 24) is a Potent Ligand for the E3 Ligase DCAF15 (IC50= 0.053 μM). Due to E3 ligase Ligand 24’s selectivity and potent binding characteristics, it is pivotal in the study of targeted protein degradation .
|
-
- HY-201580
-
-
- HY-168232
-
-
- HY-168699
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 45 is an E3 ligase ligand that can be used to synthesize the PROTAC degrader Setidegrasib (HY-148273) for Ras .
|
-
- HY-159164
-
-
- HY-161236
-
|
Molecular Glues
Ras
|
Cancer
|
KRAS ligand 4 (compound 2) is a bifunctional molecular glue degrader based on SOS1. KRAS ligand 4 reduces downstream signaling markers pERK and pS6 and displays anti-additional activity in cells with multiple KRAS mutations .
|
-
- HY-149337
-
|
Dopamine Receptor
|
Neurological Disease
|
D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling .
|
-
- HY-158430
-
-
- HY-170349
-
-
- HY-161637
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 25 (part of Compd 1) is a ligand for E3 ligase, used for the synthesis of PROTAC SOS1 degrader (HY-161634) .
|
-
- HY-161639
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 26 (part of Compd 10) is a ligand for E3 ligase, used for the synthesis of PROTAC SOS1 degrader (HY-161636) .
|
-
- HY-168253
-
-
- HY-W245311
-
|
Ligands for E3 Ligase
|
Others
|
E3 ligase Ligand 51 is the ligand for E3 ligase VHL, that can be used for synthesis of PROTAC BTK Degrader-12 (HY-170413) .
|
-
- HY-150409
-
|
AUTACs
|
Cancer
|
TSPO ligand-2 is a ligand of AUTAC1. AUTAC1 contains an p-fluorobenzylguanine (FBnG) and a Fumagillol moiety, which can silence endogenous MetAP2 in HeLa cells .
|
-
- HY-146081
-
|
CD22
|
Cancer
|
CD22 ligand-1 (compound 12) is a potent and selective CD22 ligand with KD of 0.335, 30.7 µM for hCD22 and MAG, respectively. CD22 ligand-1 has the potential for the research of B-cell related disease .
|
-
- HY-168311
-
|
Ligands for Target Protein for PROTAC
|
Cancer
|
PROTAC IRAK4 ligand-5 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PROTAC IRAK4 ligand-5 can be utilized for the synthesis of KT-413 (HY-153368) .
|
-
- HY-145990
-
MF6
|
FABP
|
Inflammation/Immunology
|
FABPs ligand 6 (MF6) is an FABP5 and FABP7 inhibitor with KD values of 874 nM and 20 nM, respectively. FABPs ligand 6 can be used for multiple sclerosis research .
|
-
- HY-128836
-
MDM2 Ligand 2; E3 ligase Ligand 15
|
Ligands for E3 Ligase
|
Cancer
|
(4R,5S)-Nutlin carboxylic acid (MDM2 ligand 2) is the Nutlin 3-based MDM2 ligand. (4R,5S)-Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTACs .
|
-
- HY-151476
-
-
- HY-W733885
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 38 serves as the E3 ligase ligand for PROTAC IRAK4 degrader-12 (HY-168586) and can be used in the synthesis of PROTACs.
|
-
- HY-168252
-
-
- HY-162876
-
|
Ligands for Target Protein for PROTAC
|
Cancer
|
PROTAC BRD4 ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PROTAC BRD4 ligand-3 can be used for synthesis PROTAC BRD4 Degrader-27 (HY-162875) .
|
-
- HY-111823
-
VHL Ligand 6
|
Ligands for E3 Ligase
|
Cancer
|
VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC .
|
-
- HY-161415
-
|
Ligands for E3 Ligase
|
Cancer
|
BCL-xL/BCL-2 ligand 1 (compound 72-1) is a BCL-xL and BCL-2 protein ligand. BCL-xL/BCL-2 ligand 1 can be connected to the E3 ligase by a linker to form PROTACs (HY-161410) .
|
-
- HY-161382
-
|
Others
|
Neurological Disease
|
NPFF2-R ligand 1 (Compound 16a) is a NPFF2-R ligand, with Kis of 228 and 27 nM for NPFF1-R and NPFF2-R respectively. NPFF2-R ligand 1 can be used for research related with central nervous system .
|
-
- HY-169968
-
|
Ligands for E3 Ligase
E1/E2/E3 Enzyme
|
Cancer
|
E3 ligase Ligand 41 (Compound SI-13) is a ligand for E3 ubiquitin ligase DCAF16. E3 ligase Ligand 41 can be connected to SLF (HY-114872) by a linker (HY-W040168) to form KB03-SLF (HY-147196) .
|
-
- HY-161467
-
|
Ligands for E3 Ligase
|
Cancer
|
Aster-A Ligand-3 is a target protein ligand and can be used to synthesize PROTAC Aster-A degrader (HY-D2336) .
|
-
- HY-168243
-
-
- HY-168248
-
-
- HY-168667
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
E3 ligase Ligand 40 is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC molecule CPD-39 (HY-168664) .
|
-
- HY-168237
-
-
- HY-W539427
-
-
- HY-161495
-
-
- HY-159545
-
-
- HY-158678
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 27 (part of 15) is a ligand for E3 ligase, used for the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 (HY-158551)
|
-
- HY-158152
-
|
Ligands for E3 Ligase
|
Cancer
|
PROTAC CRBN ligand-2 (12) is a Biguanide-PROTAC derivative, with an EC50 of 0.15 mM in KP4 cells. PROTAC CRBN ligand-2 (12) demonstrates the ability to alter levels of mitochondrial proteins, notably complexes I and IV .
|
-
- HY-170354
-
|
Ligands for Target Protein for PROTAC
|
Cancer
|
SMARCA2/4-ligand-4 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-ligand-4 can be used for the synthesis of PROTAC SMARCA2/4 degrader-36 (HY-170347) .
|
-
- HY-115729
-
-
- HY-163922
-
-
- HY-162814
-
|
Ligands for Target Protein for PROTAC
|
Cancer
|
SMARCA2/4-ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-ligand-3 can be used for synthesis PROTAC SMARCA2/4-degrader-25 (HY-162813) .
|
-
- HY-156499
-
|
Others
|
Others
|
RNF114 ligand 1 is a E3 Ubiquitin ligase binder .
|
-
- HY-147810
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT7 receptor ligand 1 (Compound 5c) is a 5-HT7 receptor ligand with a Ki of 8 nM. 5-HT7 receptor ligand 1 is not hepatotoxic and exhibit moderate potential interaction with other agents metabolized by CYP3A4 or CYP2D6 .
|
-
- HY-139304
-
-
- HY-138539
-
-
- HY-132942
-
-
- HY-132942A
-
-
- HY-156793
-
|
PKC
|
Others
|
hRIO2 kinase ligand-1 (com 9) is a ligand of hRIO2 kinase, with a Kd value of 520 nM .
|
-
- HY-141486
-
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP .
|
-
- HY-129967
-
|
Ligands for Target Protein for PROTAC
|
Cancer
|
PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4 (IRAK4). PROTAC IRAK4 ligand-1 can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966) .
|
-
- HY-U00388
-
-
- HY-111839
-
CRABP-II Ligand 1
|
Ligands for Target Protein for PROTAC
|
Cancer
|
ATRA-hydroxyimino (CRABP-II ligand 1), the Retinoic acid (ATRA)-based moiety, binds to cIAP1 ligand (Bestatin) via a linker to form SNIPER to degrade CRABP-II in IMR-32 cells .
|
-
- HY-W874018
-
-
- HY-170672
-
-
- HY-139660
-
-
- HY-111845
-
-
- HY-145922
-
-
- HY-U00126
-
-
- HY-126351
-
|
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM) .
|
-
- HY-151475
-
|
Ligands for Target Protein for PROTAC
|
Cancer
|
GID4 Ligand 1 (compound 88) is a cell-permeable and high-selective GID4 binder (IC50=5.4 μM; Kd=5.6 μM), binds to GID4 in cells (EC50=558 nM). GID4 Ligand 1 can be used for the synthesis of PROTACs .
|
-
- HY-162659
-
|
Adrenergic Receptor
|
Others
|
β2AR ligand 1 (Compound 4) is a homobivalent bitopic ligand for β2 adrenergic receptor (β2AR) on the orthosteric binding site (OBS) and the metastable binding sites (MBS) .
|
-
- HY-132970
-
|
Histone Methyltransferase
|
Cancer
|
EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
|
-
- HY-162636
-
|
5-HT Receptor
|
Neurological Disease
|
5HT6-ligand-2 (compound 15) is a potent 5-HT6 inhibitor with Ki values of 3.4, 15 nM for 5-HT6, SERT, respectively. 5HT6-ligand-2 shows neuroprotection. 5HT6-ligand-2 has the potential for the research of dementia .
|
-
- HY-172067
-
-
- HY-129939
-
-
- HY-168287
-
-
- HY-101626
-
|
Sigma Receptor
|
Neurological Disease
|
Sigma-LIGAND-1 is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 has a Ki of 4000 nM at the dopamine D2 receptor .
|
-
- HY-101626A
-
|
Sigma Receptor
|
Neurological Disease
|
Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor .
|
-
- HY-115954
-
|
Dopamine Receptor
|
Neurological Disease
|
Dopamine D3 receptor ligand-2 (compound 8) is a potent D3 receptor ligand with a Ki of 11.4 nM. Dopamine D3 receptor ligand-2 have high selectivity for D3 over D2 (Ki=1228 nM) .
|
-
- HY-115955
-
|
Dopamine Receptor
|
Neurological Disease
|
Dopamine D3 receptor ligand-3 (compound 12C) is a potent D3 receptor ligand with a Ki of 3.6 nM. Dopamine D3 receptor ligand-3 have high selectivity for D3 over D2 (Ki=353 nM).
|
-
- HY-111843
-
-
- HY-115968
-
|
Dopamine Receptor
|
Neurological Disease
|
Dopamine D3 receptor ligand-4 (compound 6) is a potent and selective dopamine D3 receptor ligand, with a Ki of 0.5 nM. Dopamine D3 receptor ligand-4 shows high level of selectivity for D3 over D2 (Ki=7.43 nM) .
|
-
- HY-W035384
-
-
- HY-169488
-
|
Epigenetic Reader Domain
Target Protein Ligand-Linker Conjugates
|
Cancer
|
SMARCA2 ligand-12-3-methylazetidin is a target protein ligand-linker conjugate that incorporates a ligand for SMARCA2 (HY-169487), and a PROTAC linker (HY-W052601), which recruit E3 ligases. SMARCA2 ligand-12-3-methylazetidin can be used to synthesize PROTAC SMARCA2 degrader-25 (HY-169276) .
|
-
- HY-130297
-
|
Bcr-Abl
|
Cancer
|
PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1 .
|
-
- HY-157563
-
|
Dopamine Receptor
|
Neurological Disease
|
Dopamine D4 receptor ligand 2 (compound 17) is a potent and selective dopamine D4 ligand with IC50 values of 0.057, >1000, 220, 270 nM for D4, D2, 5-HT1A, α1, respectively .
|
-
- HY-130270
-
E3 Ligase Ligand-Linker Conjugates 57
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
AhR Ligand-Linker Conjugates 1 (E3 Ligase Ligand-Linker Conjugates 57) incorporates an IAP ligand for the E3 ubiquitin ligase, and a SNIPER linker. AhR Ligand-Linker Conjugates 1 can be used to design SNIPER .
|
-
- HY-161655
-
-
- HY-161709
-
|
Ligands for Target Protein for PROTAC
FLT3
CDK
|
Cancer
|
FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708) .
|
-
- HY-144980
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 21 (compound 2) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
|
-
- HY-144983
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 22 (compound 139) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
|
-
- HY-163583
-
-
- HY-157428
-
|
IKZF Family
|
Others
|
USP3 ZnF-UBD ligand-1 (compound 59) is a ligand that binds to the zinc finger ubiquitin-binding domain (ZnF-UBD) of USP3 with a KD of 14 μM .
|
-
- HY-144985
-
|
Ligands for E3 Ligase
|
Cancer
|
E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
|
-
- HY-125906
-