Search Result
Results for "
VHL-ligand
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-112078
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VHL ligand 2; E3 ligase ligand 1A
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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- HY-120217
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VH032
Maximum Cited Publications
9 Publications Verification
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Ligands for E3 Ligase
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Cancer
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VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kdligand for protein by a linker to form PROTACs .
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- HY-125905
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VHL ligand 3; E3 ligase ligand 19
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Ligands for E3 Ligase
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Cancer
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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-103602
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VH032-PEG3-NH2 hydrochloride; VHL ligand-Linker Conjugates 1 hydrochloride; E3 ligase ligand-Linker Conjugates 5
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG3-NH2 (VH032-PEG3-NH2) hydrochloride 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-42424
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VHL ligand 2 hydrochloride; E3 ligase ligand 1
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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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-103604
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VH032-PEG4-NH2 hydrochloride; VHL ligand-Linker Conjugates 4 hydrochloride; E3 ligase ligand-Linker Conjugates 7
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
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- HY-103603
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VH032-PEG2-NH2 hydrochloride; VHL ligand-Linker Conjugates 3 hydrochloride; E3 ligase ligand-Linker Conjugates 6
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG2-NH2 hydrochloride (VH032-PEG2-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs .
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- HY-103601
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VH032-PEG4-N3; VHL ligand-Linker Conjugates 5; E3 ligase ligand-Linker Conjugates 4
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E3 Ligase Ligand-Linker Conjugates
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Others
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(S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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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-103598
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VH032-PEG3-N3; VHL ligand-Linker Conjugates 8; E3 ligase ligand-Linker Conjugates 12
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG3-N3 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. (S,R,S)-AHPC-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-103600
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VH032-PEG1-N3; VHL ligand-Linker Conjugates 9; E3 ligase ligand-Linker Conjugates 3
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG1-N3 (VH032-PEG1-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-111663
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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-125845
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VH032-NH2; VHL ligand 1
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
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- HY-103604A
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VH032-PEG4-NH2; VHL ligand-Linker Conjugates 4 ; E3 ligase ligand-Linker Conjugates 7 Free Base
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
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- HY-42419
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me-NHBoc is an E3 ubiquitin ligase VHL ligand used to recruit the VHL protein. (S,R,S)-AHPC-Me-NHBoc can be linked to a target protein ligand via a linker to form a PROTAC.
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- HY-148671
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-amido-C7-acid incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design PROTACs .
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- HY-111905
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Epigenetic Reader Domain
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Cancer
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BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively) .
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- HY-130271
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VH032-PEG5-COOH; VHL ligand-Linker Conjugates 16; E3 Ligase ligand-Linker Conjugates 58
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 5-unit PEG linker used in PROTAC technology .
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- HY-103603A
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VH032-PEG2-NH2 ; VHL ligand-Linker Conjugates 3 ; E3 ligase ligand-Linker Conjugates 6 Free Base
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG2-NH2 (VH032-PEG2-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs .
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- HY-103608
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VHL ligand-Linker Conjugates 11; E3 ligase ligand-Linker Conjugates 11
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-(C3-PEG)2-C6-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-PEG)2-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
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- HY-47851
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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-174873
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PROTACs
METTL3
Apoptosis
Bcl-2 Family
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Cancer
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AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875)) .
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- HY-135345
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PROTACs
FKBP
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Cancer
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PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader .
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- HY-172946
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PROTACs
STAT
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Cancer
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SD-2301 is a selective STAT3 PROTAC degrader. SD-2301 induces STAT3 degradation without affecting the protein levels of other STAT family members (STAT1, STAT2, STAT4, STAT5, STAT6). SD-2301 exerts anti-tumor effects in B16F10-bearing mice. SD-2301 can be used for the study of cancer. (Pink: STAT3 ligand (HY-172947), Blue: VHL Ligand (HY-172948), Black: Linker (HY-W577012), VHL ligand-linker conjugate (HY-172949)) .
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- HY-42424A
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VHL ligand 2 dihydrochloride; E3 ligase ligand 1 dihydrochloride
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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- HY-103599
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VH032-PEG2-N3; VHL ligand-Linker Conjugates 6; E3 ligase ligand-Linker Conjugates 13
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-N3 can be used for the synthesis of PROTACs .
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- HY-103606
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VH032-PEG6-C4-Cl; VHL ligand-Linker Conjugates 10; E3 ligase ligand-Linker Conjugates 9
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG6-C4-Cl is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG6-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
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- HY-103605
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VH032-C6-PEG3-C4-Cl; VHL ligand-Linker Conjugates 12; E3 ligase ligand-Linker Conjugates 8
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
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- HY-D2413
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BODIPY FL PEG4-VH032
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Fluorescent Dye
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Others
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BODIPY FL VH032 is a high-affinity VHL fluorescent probe with a Kd value of 3.01 nM. BODIPY FL VH032 consists of von Hippel-Lindau (VHL) ligand VH032 (HY-120217) and BODIPY FL (HY-43520). BODIPY FL VH032 can be used for time-resolved fluorescence resonance energy transfer (TR-FRET) detection for high-throughput identification and characterization of VHL ligands with maximum excitation emission wavelength: 504/520 nm .
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- HY-162553
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Ligands for E3 Ligase
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Cancer
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GNE7599 is a high-affinity and orally active von Hippel-Lindau (VHL) ligand with a Kd of 540 pM. GNE7599 can be connected to the ligand for protein by a linker to form PROTACs .
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- HY-136164
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Ligands for E3 Ligase
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Cancer
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VH032-OH is the VH032-based VHL ligand. VH032-OH can be connected to the ligand for protein by a linker to form PROTACs .
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- HY-138861A
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C1-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology .
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- HY-151227
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Ligands for E3 Ligase
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Cancer
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VL285 Phenol is a phenol-based VL285 analog. VL285 is an E3 ubiquitin ligase VHL ligand and can be used in the synthesis of HaloPROTAC3, degrading HaloTag7 fusion protein (IC50=0.34 μM).
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- HY-111823
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VHL ligand 6
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Ligands for E3 Ligase
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Cancer
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VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC .
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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-110402
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VH032-NH2 TFA; VHL ligand 1 TFA
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2) TFA is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
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- HY-103607
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VH032-PEG2-C4-Cl; VHL ligand-Linker Conjugates 7; E3 ligase ligand-Linker Conjugates 10
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
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- HY-176198
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PROTACs
FAK
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Cancer
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BI-0319 is a selective PTK2/FAK PROTAC degrader. BI-0319 can reduce cancer cells viability inhibit proliferation and invasion. BI-0319 can be used for the research of cancer, such as liver cancer . (Structure Note: Pink: PTK2/FAK ligand (HY-43760); Blue: VHL ligand (HY-125845); Black: linker (HY-140189); VHL ligand-Linker: (HY-103602A))
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- HY-148896
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- HY-173422
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PROTACs
Histone Methyltransferase
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Cancer
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MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC50: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424)) .
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- HY-136163
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C2-NH2 dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-OH can be used in the synthesis of a series of PROTACs .
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- HY-114176B
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VH032-C4-NH2 dihydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C4-NH2 dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC .
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- HY-157512
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Ligands for E3 Ligase
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Cancer
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SJF-0661 is a variant of the von Hippel-Lindau (VHL) protein ligand with no targeted degradation ability and can be used as a control reagent for the VHL ubiquitin ligase ligand. SJF-0661 is a variant obtained by inverting the stereocenter of the key hydroxyproline group in the VHL ligand .
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- HY-125906
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E3 Ligase ligand-Linker Conjugates 56
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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VHL Ligand-Linker Conjugates 15 incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs .
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- HY-W998246
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(R,R,S)-VH032-NH2; (R,R,S)-VHL ligand 1
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Ligands for E3 Ligase
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Cancer
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(R,R,S)-AHPC ((R,R,S)-VH032-NH2) is a VHL ligand based on (S,R,S)-AHPC that recruits von Hippel-Lindau (VHL) protein. (R,R,S)-AHPC can be linked to a target protein ligand via a linker to form a PROTACs.
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- HY-114176
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VH032-C4-NH2 hydrochloride; VHL ligand-Linker Conjugates 13; E3 ligase ligand-Linker Conjugates 28
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC .
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- HY-103602A
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VH032-PEG3-NH2; VHL ligand-Linker Conjugates 1; E3 ligase ligand-Linker Conjugates 5 Free Base
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG3-NH2 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-172948
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Ligands for E3 Ligase
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Cancer
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VHL Ligand 36 is a von Hippel-Lindau (VHL) ligand. VHL Ligand 36 can be used to synthesize SD-2301 (HY-172946) .
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- HY-W998339
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Ligands for E3 Ligase
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Cancer
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(R,S,R)-AHPC-NHBoc is an E3 ubiquitin ligase VHL ligand used to recruit the VHL protein. (R,S,R)-AHPC-NHBoc can be linked to a target protein ligand via a linker to form a PROTAC.
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- HY-158047
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PROTACs
STING
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Infection
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UNC8900 is a VHL recruiting STING PROTAC degrader (DC50: 0.0.924 μM). UNC8900 can be used for research of viral or bacterial infection. (Blue: VHL ligand, black: linker; Pink: STING inhibitor) .
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- HY-158046
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PROTACs
STING
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Infection
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UNC8899 is a VHL-recruiting STING PROTAC degrader (DC50: 0.0.924 μM). UNC8899 can be used for viral or bacterial infection research (Blue: VHL ligand, Black: linker; Pink: STING inhibitor) .
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- HY-136183
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VH032 phenol-alkylC6-amine dihydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-phenol-alkylC6-amine dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and an alkyl linker used for PROTAC degrader .
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- HY-114176A
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VH032-C4-NH2
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC .
|
-
- HY-W998247
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,R)-VH032 hydrochloride is a VHL ligand based on VH032 that recruits von Hippel-Lindau (VHL) protein. (S,R,R)-VH032 hydrochloride can be linked to a target protein ligand via a linker to form a PROTACs.
|
-
- HY-168453
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
dBAZ2B is a BAZ2B PROTAC degrader, with a DC50 of 19 nM . (Pink: BAZ2A/B ligand (HY-168449); Black: linker (HY-168450); Blue: VHL Ligand (HY-125905))
|
-
- HY-136165
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG3-propionic acid 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 .
|
-
- HY-49514
-
|
|
Ligands for E3 Ligase
SOS1
|
Cancer
|
|
VHL Ligand intermediate-1 (intermediate 18a) is an intermediate in the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs .
|
-
- HY-49515
-
|
|
Ligands for E3 Ligase
SOS1
|
Cancer
|
|
VHL Ligand intermediate-2 (compound 18c) is an intermediate for the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs .
|
-
- HY-163219
-
-
- HY-111824
-
|
VHL ligand-Linker Conjugates 14; E3 ligase ligand-Linker Conjugates 29
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-thiol-C6-NH2 (VHL Ligand-Linker Conjugates 14) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-101763B
-
|
VH032-NH2 dihydrochloride; VHL ligand 1 dihydrochloride
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC (VH032-NH2) dihydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC dihydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
|
-
- HY-125846
-
|
VH032-PEG1-OTs; VHL ligand-Linker Conjugates 2; E3 ligase ligand-Linker Conjugates 51
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG1-OTs is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.
|
-
- HY-103602B
-
|
VH032-PEG3-NH2 dihydrochloride; VHL ligand-Linker Conjugates 1 dihydrochloride; E3 ligase ligand-Linker Conjugates 5 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(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
|
-
- HY-161367
-
-
- HY-168454
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
trans-VH032-Cyclopropane-F-C-cyclohexane-p-C-OTs incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs, such as dBAZ2B (HY-168453) .
|
-
- HY-112078A
-
-
- HY-173433
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)) .
|
-
- HY-161368
-
-
- HY-138678B
-
-
- HY-162450
-
|
|
PROTACs
MDM-2/p53
Apoptosis
|
Cancer
|
Antitumor agent-150 (V10), an anti-breast cancer agent, is a PROTAC-based MDM2 protein degrader (Red: Ganoderic acid A; Black: 4O-PEG linker; Blue: VHL ligand) .
|
-
- HY-138862
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology .
|
-
- HY-136163A
-
-
- HY-131959
-
-
- HY-138861
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology .
|
-
- HY-148406
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C10-NHBoc is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC (HY-125845) based VHL ligand and a linker used for BET-Targeted PROTAC .
|
-
- HY-130798
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180) .
|
-
- HY-122570
-
|
|
E1/E2/E3 Enzyme
|
Others
|
|
VHL Ligand 38 (Compound 1) is a competitive E3 ubiquitin-protein ligase VHL inhibitor with IC50s of 4.1 and 7.0 μM in 1% and 10% DMSO, respectively. VHL Ligand 38 contains a hydroxyproline residue and an isoxazolylacetamide fragment. VHL Ligand 38 significantly inhibits the binding of a fluorescent peptide derived from HIF1α (FAM-DEALA-Hyp-YIPD) (HY-P5908F) to VHL .
|
-
- HY-117844
-
|
|
Ligands for E3 Ligase
|
Others
|
|
VHL Ligand 35 (Compound 14) is a von Hippel-Lindau protein (pVHL) E3 ubiquitin ligase ligand with a Kd of 0.291 μM. VHL Ligand 35 disrupts protein-protein interaction between pVHL and hypoxia inducible factor 1α (HIF-1α) .
|
-
- HY-181791
-
|
|
Ligands for E3 Ligase
|
Others
|
|
VHL Ligand 39 is a conjugate of an E3 ligase ligand, serving as a key intermediate in the synthesis of complete PROTAC molecules .
|
-
- HY-181748
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VHL Ligand-Linker Conjugates 18 is an E3 ligase ligand-linker conjugate containing an E3 ligase ligand (HY-181791) and a linker. VHL Ligand-Linker Conjugates 18 can be used for the synthesis of PROTACs, such as DOT1L808 (HY-181789) .
|
-
- HY-101763AR
-
|
VH032-NH2 monohydrochloride (Standard); VHL ligand 1 monohydrochloride (Standard)
|
Reference Standards
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC monohydrochloride (Standard) (VH032-NH2 monohydrochloride (Standard)) is the analytical standard of (S,R,S)-AHPC monohydrochloride (HY-101763A). This product is intended for research and analytical applications. (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 .
|
-
- HY-103604AR
-
|
VH032-PEG4-NH2 (Standard); VHL ligand-Linker Conjugates 4 (Standard); E3 ligase ligand-Linker Conjugates 7 Free Base (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG4-NH2 (Standard) is the analytical standard of (S,R,S)-AHPC-PEG4-NH2 (HY-103604A). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
|
-
- HY-103603R
-
|
VH032-PEG2-NH2 hydrochloride (Standard); VHL ligand-Linker Conjugates 3 hydrochloride (Standard); E3 ligase ligand-Linker Conjugates 6 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-NH2 hydrochloride (Standard) is the analytical standard of (S,R,S)-AHPC-PEG2-NH2 hydrochloride (HY-103603). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG2-NH2 hydrochloride (VH032-PEG2-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs .
|
-
- HY-103602R
-
|
VH032-PEG3-NH2 hydrochloride (Standard); VHL ligand-Linker Conjugates 1 hydrochloride (Standard); E3 ligase ligand-Linker Conjugates 5 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG3-NH2 hydrochloride (Standard) is the analytical standard of (S,R,S)-AHPC-PEG3-NH2 hydrochloride (HY-103602). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG3-NH2 (VH032-PEG3-NH2) hydrochloride 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.
|
-
- HY-103599R
-
|
VH032-PEG2-N3 (Standard); VHL ligand-Linker Conjugates 6 (Standard); E3 ligase ligand-Linker Conjugates 13 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-N3 (Standard) is the analytical standard of (S,R,S)-AHPC-PEG2-N3 (HY-103599). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-N3 can be used for the synthesis of PROTACs .
|
-
- HY-103603AR
-
|
VH032-PEG2-NH2 (Standard); VHL ligand-Linker Conjugates 3 (Standard); E3 ligase ligand-Linker Conjugates 6 Free Base (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-NH2 (Standard) is the analytical standard of (S,R,S)-AHPC-PEG2-NH2 (HY-103603A). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG2-NH2 (VH032-PEG2-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs .
|
-
- HY-103608R
-
|
VHL ligand-Linker Conjugates 11 (Standard); E3 ligase ligand-Linker Conjugates 11 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-(C3-PEG)2-C6-Cl (Standard) is the analytical standard of (S,R,S)-AHPC-(C3-PEG)2-C6-Cl (HY-103608). This product is intended for research and analytical applications. (S,R,S)-AHPC-(C3-PEG)2-C6-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-PEG)2-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
|
-
- HY-103601R
-
|
VH032-PEG4-N3 (Standard); VHL ligand-Linker Conjugates 5 (Standard); E3 ligase ligand-Linker Conjugates 4 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
(S,R,S)-AHPC-PEG4-N3 (Standard) is the analytical standard of (S,R,S)-AHPC-PEG4-N3 (HY-103601). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-103600R
-
|
VH032-PEG1-N3 (Standard); VHL ligand-Linker Conjugates 9 (Standard); E3 ligase ligand-Linker Conjugates 3 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG1-N3 (Standard) is the analytical standard of (S,R,S)-AHPC-PEG1-N3 (HY-103600). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG1-N3 (VH032-PEG1-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-103606R
-
|
VH032-PEG6-C4-Cl (Standard); VHL ligand-Linker Conjugates 10 (Standard); E3 ligase ligand-Linker Conjugates 9 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG6-C4-Cl (Standard) is the analytical standard of (S,R,S)-AHPC-PEG6-C4-Cl (HY-103606). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG6-C4-Cl is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG6-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
|
-
- HY-103607R
-
|
VH032-PEG2-C4-Cl (Standard); VHL ligand-Linker Conjugates 7 (Standard); E3 ligase ligand-Linker Conjugates 10 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-C4-Cl (Standard) is the analytical standard of (S,R,S)-AHPC-PEG2-C4-Cl (HY-103607). This product is intended for research and analytical applications. (S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
|
-
- HY-103605R
-
|
VH032-C6-PEG3-C4-Cl (Standard); VHL ligand-Linker Conjugates 12 (Standard); E3 ligase ligand-Linker Conjugates 8 (Standard)
|
Reference Standards
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C6-PEG3-C4-Cl (Standard) is the analytical standard of (S,R,S)-AHPC-C6-PEG3-C4-Cl (HY-103605). This product is intended for research and analytical applications. (S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
|
-
- HY-W998245
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(R,R,R)-AHPC hydrochloride is an E3 ubiquitin ligase VHL ligand used to recruit the VHL protein. (R,R,R)-AHPC hydrochloride can be linked to a target protein ligand via a linker to form a PROTAC.
|
-
- HY-169395
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-CO-PEG-C2-iodine is an E3 ligase (VHL) ligand-linker conjugate, and can be used for synthesis of PROTACs, such as PROTAC FAK degrader 1 (HY-119932)
|
-
- HY-W800964
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC 2-OH hydrochloride is an E3 ubiquitin ligase VHL ligand used to recruit the VHL protein. (S,R,S)-AHPC 2-OH hydrochloride can be linked to a target protein ligand via a linker to form a PROTAC.
|
-
- HY-48682
-
-
- HY-103603C
-
|
|
E3 Ligase Ligand-Linker Conjugates
Drug Isomer
|
Cancer
|
|
(S,S,S)-AHPC-PEG2-NH2 is an isomer of Compound 15b. Compound 15b is a conjugate of a VHL ligand and linker. Compound 15b can be used to synthesize PROTAC. Compound 15b can be used in leukemia research .
|
-
- HY-185142
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
The (S,R,S)-AHPC-Me-C8-NHS ester is an E3 ubiquitin ligase VHL ligand, used to recruit the VHL protein. The (S,R,S)-AHPC-Me-C8-NHS ester can be linked to the target protein ligand through a linker to form a PROTAC.
|
-
- HY-158048
-
|
|
PROTACs
STING
|
Inflammation/Immunology
|
|
UNC9036 is a PROTAC-based STING degrader, with a DC50 of 227 nM. UNC9036-mediated STING degradation is proteasome and VHL dependent (Structure Note: Red, STING agonist diABZI (HY-112921A); Blue, VHL ligand VH032 (HY-120217); Black, linker) .
|
-
- HY-W1130374
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-amide-C10-azide is an E3 ubiquitin ligase VHL ligand used to recruit the VHL protein. (S,R,S)-AHPC-amide-C10-azide can be linked to a target protein ligand via a linker to form a PROTAC.
|
-
- HY-136006B
-
|
VH032-C6-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C6-NH2 (VH032-C6-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in?PROTAC?technology .
|
-
- HY-W998314
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-CO-C2-COOH is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-Me-CO-C2-COOH can be used to synthesize PROTAC.
|
-
- HY-W688682
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-NH2 hydrochloride is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-C5-NH2 hydrochloride can be used to synthesize PROTAC.
|
-
- HY-W1130395
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-SH is a VHL ligand based on (S,R,S)-AHPC that recruits von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-PEG2-SH can be linked to a target protein ligand via a linker to form a PROTACs.
|
-
- HY-130711B
-
|
VH032-C3-NH2 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology .
|
-
- HY-111905A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively) .
|
-
- HY-W998311
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-CO-C6-COOH is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-Me-CO-C6-COOH can be used to synthesize PROTAC.
|
-
- HY-136008
-
|
VH032-PEG1-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG1-NH2 (VH032-PEG1-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology .
|
-
- HY-W598206
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG8-NH2 hydrochloride is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-C5-NH2 hydrochloride can be used to synthesize PROTAC.
|
-
- HY-W1130361
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-PEG5-Azide is a VHL ligand based on (S,R,S)-AHPC that recruits von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-PEG5-Azide can be linked to a target protein ligand via a linker to form a PROTACs.
|
-
- HY-W998297
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-CO-C-PEG5-amine hydrochloride is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-CO-C-PEG5-amine hydrochloride can be used to synthesize PROTAC.
|
-
- HY-W590558
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG8-NH2 is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-PEG8-NH2 can be used to synthesize PROTAC.
|
-
- HY-130849
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-C5-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-C5-COOH can be used in PROTAC DT2216 (HY-130604) .
|
-
- HY-135045
-
|
VH032-C4-COOH
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C4-COOH (VH032-C4-COOH) (linker 45) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-targeted PROTAC .
|
-
- HY-133487A
-
|
VH032-C8-NH2 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology .
|
-
- HY-W998315
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-CO-C3-COOH is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-Me-CO-C3-COOH can be used to synthesize PROTAC.
|
-
- HY-174453
-
|
|
PROTACs
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)) .
|
-
- HY-175885
-
|
|
PROTACs
Fat Mass and Obesity-associated Protein (FTO)
Apoptosis
Caspase
PARP
YTHDF
|
Cancer
|
|
PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m6A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML) . (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))
|
-
- HY-129941
-
|
VH032-C10-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC .
|
-
- HY-W926049
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-C4-NH2 hydrochloride is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-Me-C4-NH2 hydrochloride can be used to synthesize PROTAC.
|
-
- HY-136186
-
|
VH032-C7-amine
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-129941A
-
|
VH032-C10-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-C10-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC .
|
-
- HY-136186B
-
|
VH032-C7-amine hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-W1130360
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-Me-PEG3-azide is a VHL ligand based on (S,R,S)-AHPC that recruits von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me-PEG3-azide can be linked to a target protein ligand via a linker to form a PROTACs.
|
-
- HY-155815
-
|
|
Histone Methyltransferase
PROTACs
|
Cancer
|
|
MS9715 is a potent and seletive NSD3-targeting PROTAC. MS9715 is designed by BI-9321, which binds NSD3’s PWWP1 domain, with an E3 ligase VHL ligand. MS9715 has the potental for NSD3-dependent cancer research .
|
-
- HY-168229
-
|
|
PROTACs
SWI/SNF Complex
|
Cancer
|
|
PROTAC SMARCA2 degrader-27 (compound 4) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-27 has the potential to be used in cancer research (Pink: SMARCA2 ligand (HY-168230); Blue: VHL ligand (HY-168232); Black: linker (HY-168231)) .
|
-
- HY-131865
-
|
|
PROTACs
EGFR
|
Cancer
|
|
SJF-1521 is a selective EGFR PROTAC degrader. SJF-1521 is capable of inducing EGFR degradation in OVCAR8 cells. SJF-1521 can be used for tumor research. (Pink: EGFR ligand (HY-177379); Black: Linker (HY-128804); Blue: VHL Ligand (HY-125845)) .
|
-
- HY-161445
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-piperazine-acetyl-PIP-AcOH is a conjugate of the VHL ligand and linker of the E3 ubiquitinase VH032. The Linker of (S,R,S)-AHPC-Me-piperazine-acetyl-PIP-AcOH can further be linked to target protein ligands (such as BCR-ABL1) to form PROTAC molecules .
|
-
- HY-130641
-
|
|
PROTAC Linkers
|
Cancer
|
|
Br-C10-methyl ester is a PROTAC linker, which refers to the alkyl/ether composition. Br-C10-methyl ester is used in the synthesis of a series of PROTACs (MS432). PROTACs contain two different ligands connected by a linker; one is the VHL ligand portion and the other is for the target protein .
|
-
- HY-44432
-
|
ABT-263-piperazine
|
Ligands for Target Protein for PROTAC
Bcl-2 Family
|
Cancer
|
|
Navitoclax-piperazine (ABT-263-piperazine) is a Navitoclax (HY-10087) analog and BCL-XL inhibitor. Navitoclax-piperazine is the ligand for target protein of PROTAC DT2216 (HY-130604). Navitodax-pperaie and E3 ubiquitin ligase VHL ligand can be used to synthesize PROTAC DT2216 (HY-130604) .
|
-
- HY-136184
-
|
VH032-phenol-C4-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-phenol-C4-NH2 (VH032-phenol-C4-NH2) dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology .
|
-
- HY-W998310
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-CO-C4-COOH is a conjugate of the E3 ligase VHL ligand and a linker, which can be used to synthesize PROTAC ERα Degrader-12 (HY-174453). PROTAC ERα Degrader-12 is a potent and highly selective ERα PROTAC degrader .
|
-
- HY-176530
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-amide-C4-Br incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-Me-amide-C4-Br can be used to design PROTAC, such as PROTAC ERK5 degrader-1 (HY-176528) .
|
-
- HY-179230
-
|
|
PROTAC-Linker Conjugates for PAC
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 214 is an E3 ligase ligand-linker conjugate containing a Von Hippel-Lindau (VHL) ligand and a linker. E3 Ligase Ligand-linker Conjugate 214 can bind to a target protein ligand to form a PROTAC molecule, PROTAC LSD1 Degrader 1 (HY-179229) .
|
-
- HY-130847
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-C10-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-C10-NH2 can be used in PROTAC MS432 (HY-130602) .
|
-
- HY-176366
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
AHPC-PEG6-CH2COOH is an E3 ligase ligand-linker conjugate that incorporates a VHL ligand and 6-unit PEG linker (HY-122702). AHPC-PEG6-CH2COOH can be used for synthesis of PROTAC CMP98 (HY-136257) .
|
-
- HY-136187
-
|
VH032-C5-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-172645
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-amide-C-O-C5-Br incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-Me-amide-C-O-C5-Br can be used to design PROTACs, such as ERD-308 (HY-128600) .
|
-
- HY-139218
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
(S,R,S)-AHPC-Me-C6-NH2 is a VHL E3 ubiquitin ligase ligand-linker conjugate structurally modified based on VHL ligand 2 (HY-112078). (S,R,S)-AHPC-Me-C6-NH2 can be used for the synthesis of PROTACs .
|
-
- HY-147174
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker .
|
-
- HY-136008A
-
|
VH032-PEG1-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG1-NH2 (VH032-PEG1-NH2) dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-PEG1-NH2 dihydrochloride can be used to design PROTACs .
|
-
- HY-400685
-
|
|
Drug Intermediate
|
Cancer
|
|
SMD-3040 intermediate-2 is an intermediate in the synthesis of SMD-3040 (HY-156568). SMD-3040 contains SMARCA2/4 ligands, linker and VHL ligands and is a selective SMARCA2 degrader. MD-3040 can be used for ADC drug synthesis and has strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-103603B
-
|
VH032-PEG2-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-PEG2-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs .
|
-
- HY-136187A
-
|
VH032-C5-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-W584528
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032 analogue-2 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-2 will remove the protective group under acidic conditions, and can be directly used for the synthesis of PROTAC molecules. VH032 analogue-2 is a key intermediate for the synthesis of PROTACs based on VHL ligands.
|
-
- HY-W584527
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032 analogue-1 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-1 will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032 analogue-1 is a key intermediate in the synthesis of PROTACs based on VHL ligands.
|
-
- HY-W998298
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-PEG3-C3 is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-C5-PEG3-C3 can be used to synthesize PROTAC.
|
-
- HY-162835
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-28 (PROTAC 1) is a PROTAC-based partial degrader of SMARCA2 and SMARCA4(Bliue: CRL2 VHL ligand (S,R,S)-AHPC (HY-125845); Black: linker (HY-159680); Pink: a SMARCA-BD ligand (+)-JQ-1 (HY-13030)) .
|
-
- HY-162834
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-27 (PROTAC 2) is a PROTAC-based degrader of SMARCA2 and SMARCA4. (Blue: CRL2 VHL ligand VH032-cyclopropane-F (HY-125905); Black: linker (HY-159678);Pink: a SMARCA-BD ligand 1 for PROTAC (HY-44012)) .
|
-
- HY-174875
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
(S,R,S)-AHPC-CO-C2-phenylboronic acid is an E3 ligase ligand-linker conjugate that incorporates the VH032-based VHL ligand (HY-125845) and linker. (S,R,S)-AHPC-CO-C2-phenylboronic acid can be used for synthesis of PROTAC AF151 (HY-174873) .
|
-
- HY-163440
-
|
|
PROTACs
NAMPT
|
Cancer
|
|
PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells.
(Structure Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .
|
-
- HY-W998296
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG6-C4-NH2 hydrochloride is an E3 ligase ligand-linker conjugate containing a VHL ligand and linker based on (S,R,S)-AHPC. (S,R,S)-AHPC-PEG6-C4-NH2 hydrochloride can be used to synthesize PROTAC.
|
-
- HY-137346
-
|
(S,R,S)-AHPC-Me-PEG2-dabrafenib
|
PROTACs
LIM Kinase (LIMK)
CDK
|
Cancer
|
|
DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17 (Blue: VHL ligand (HY-112078), Black: linker HY-124380 (HY-124380);Pink: BRAF inhibitor (HY-14660)) .
|
-
- HY-162362
-
|
|
PROTACs
GLP Receptor
|
Cancer
|
|
MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker) .
|
-
- HY-138678
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669) .
|
-
- HY-114404
-
|
|
PROTACs
p38 MAPK
|
Cancer
|
|
SJFα is a selective p38α PROTAC degrader with a DC50 of 7.16 nM and Dmax of 97.4%. SJFα is far less effective at degrading p38δ (DC50 = 299 nM). SJFαcan be used for the research of cancer, such as breast cancer . (Structure Note: Pink: p38α ligand (HY-45124); Blue: VHL ligand (HY-125845))
|
-
- HY-W937057
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-10-bromodecanoic acid is an E3 ligase ligand-linker conjugate that incorporates a VHL ligand 2 (HY-112078) and linker 10-bromoheptanoic acid. (S,R,S)-AHPC-Me-10-bromodecanoic acid can be used for synthesis of PROTAC PI3Kδ degrader-1 (HY-176239) .
|
-
- HY-156568
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 can be used in the study of tumors such as melanoma . (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
|
-
- HY-159457
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-6 (compound I-438) is a SMARCA2/4 degrader. PROTAC SMARCA2/4-degrader-6 has the potential for the research of cancer. (Pink: SMARCA2/4 ligand, (HY-159545); Black: linker (HY-W006635); Blue: VHL ligand (HY-112078)) .
|
-
- HY-171830
-
|
YX39-105
|
PROTACs
Tyrosinase
Apoptosis
|
Cancer
|
|
MS105 (YX39-105) is an orally active and selective protein tyrosine kinase 6 (PTK6) (BRK) PROTAC degrader. MS105 recruits VHL E3 ligase via a VHL ligand moiety, promotes PTK6 ubiquitination and proteasomal degradation, inhibits the proliferation and migration of breast cancer cells, and induces apoptosis. MS105 shows potential for use in breast cancer research .
|
-
- HY-159147
-
|
|
PROTACs
ROS Kinase
Apoptosis
|
Cancer
|
|
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
|
-
- HY-168290
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide can be used in the synthesis of PROTACs, such as MS934 (HY-153863). MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader .
|
-
- HY-157596
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 ligase Ligand-Linker Conjugate 40 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 ligase Ligand-Linker Conjugate 40 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-157598
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 ligase Ligand-Linker Conjugate 46 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 ligase Ligand-Linker Conjugate 46 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-157590
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 ligase Ligand-Linker Conjugate 32 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 ligase Ligand-Linker Conjugate 32 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-173010
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Infection
|
|
Me-(S,R,S)-AHPC-CO-C5-N3 is an E3 ligase ligand-linker conjugate composed of a VHL ligand (HY-112078) and a linker (HY-W123015). Me-(S,R,S)-AHPC-CO-C5-N3 can be used for synthesis of PROTACs, such as PROTAC CG167 (HY-173009) .
|
-
- HY-157752
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 101 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 Ligase Ligand-linker Conjugate 101 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-157754
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 103 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 Ligase Ligand-linker Conjugate 103 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-156568A
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 TFA is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 TFA can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 TFA can be used in the study of tumors such as melanoma . (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
|
-
- HY-156568B
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 formate is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 formate can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 formate can be used in the study of tumors such as melanoma . (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
|
-
- HY-157597
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 ligase Ligand-Linker Conjugate 42 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 ligase Ligand-Linker Conjugate 42 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-125845A
-
|
(S,S,S)-VH032-NH2 hydrochloride
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,S,S)-AHPC ((S,S,S)-VH032-NH2) hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC (Compound 27) is a ligand used as a negative control for (S,R,S)-AHPC (HY-125845). (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein .
|
-
- HY-125845B
-
|
(S,S,S)-VH032-NH2
|
Ligands for E3 Ligase
|
Others
|
|
(S,S,S)-AHPC ((S,S,S)-VH032-NH2) is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC (Compound 27) is a ligand used as a negative control for (S,R,S)-AHPC (HY-125845). (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein .
|
-
- HY-157753
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 102 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 Ligase Ligand-linker Conjugate 102 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-157593
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 ligase Ligand-Linker Conjugate 35 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 ligase Ligand-Linker Conjugate 35 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-119932
-
|
|
PROTACs
FAK
Akt
|
Cancer
|
|
PROTAC FAK degrader 1 (Compound PROTAC-3) is a selective and effective degrader of Fak PROTAC with a DC50 of 3.0 nM. PROTAC FAK degrader 1 reduces the ability of cancer cells to migrate and invade. PROTAC FAK degrader 1 can be used in the study of tumor. (Pink: Fak ligand (HY-44146); Black: Linker (HY-44141); Blue: VHL ligand 1 (HY-125845)) .
|
-
- HY-128767
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-PEG3-acetylene is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology . VH032-PEG3-acetylene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-162193
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 27 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 Ligase Ligand-linker Conjugate 27 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-157634
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 91 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 Ligase Ligand-linker Conjugate 91 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-162202
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 50 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 Ligase Ligand-linker Conjugate 50 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-163872
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-10 (compound I-399) is a potent SMARCA2 degrader with an DC50 value of <100 nM. PROTAC SMARCA2/4-degrader-10 has the potential for the research of cancer (Blue:SMARCA2/4 ligand, (HY-159542); Black: linker (HY-W088435); Pink:VHL ligand (HY-125845)) .
|
-
- HY-161194
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-acetyl-azetidine-PIP-boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S,R,S)-AHPC-acetyl-azetidine-PIP-boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-145514D
-
dTAGV-1
5 Publications Verification
|
PROTACs
FKBP
|
Cancer
|
|
dTAGV-1 is a potent and selective degrader of FKBP12 F36V-tagged proteins PROTAC degrader. dTAGV-1 can induce degradation of FKBP12 F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A)) .
|
-
- HY-136262
-
|
|
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. (Pink: VHL ligand (HY-125845); Blue: E3 Ligase ligand (HY-10984); Black: linker (HY-403544)) .
|
-
- HY-130815A
-
-
- HY-130815
-
-
- HY-128845
-
|
|
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other . (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))
|
-
- HY-161207
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-acetyl-Pip-O-azetidine-boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S,R,S)-AHPC-acetyl-Pip-O-azetidine-boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-144323
-
|
|
PROTACs
PERK
|
Cancer
|
|
YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
|
-
- HY-162538
-
|
|
NF-κB
IRAK
PROTACs
|
Inflammation/Immunology
|
|
LC-MI-3 is an orally active and potent interleukin-1 receptor-associated kinase 4 (IRAK4) PROTAC degrader, with a DC50 of 47.3 nM. LC-MI-3 effectively inhibits the activation of downstream NF-κB signaling. LC-MI-3 can be used for the research of acute and chronic inflammatory skin. (Blue: VHL ligand, Black: linker, Pink: CRBN ligand (HY-14658)) .
|
-
- HY-145514C
-
|
|
FKBP
PROTACs
|
Cancer
|
|
dTAGV-1 hydrochloride is a potent and selective degrader of FKBP12 F36V-tagged proteins PROTAC degrader. dTAGV-1 hydrochloride can induce degradation of FKBP12 F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A)) .
|
-
- HY-160415
-
WD6305
2 Publications Verification
|
PROTACs
Apoptosis
METTL3
|
Cancer
|
|
WD6305 is a potent and selective METTL3-METTL14 PROTAC degrader. WD6305 has DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. WD6305 inhibits m 6A modification and proliferation of AML cells, and induces apoptosis. WD6305 has antitumor activity .(Pink: UZH2 (HY-115717); Black: Linker; Blue: VHL ligand (HY-150803))
|
-
- HY-176904
-
|
|
PROTACs
HDAC
Apoptosis
|
Cancer
|
|
JPS004 is a HDAC1-3 PROTAC degrader. JPS004 can induce degradation of HDAC1-3 and induce histone acetylation. JPS004 can induce cancer cells apoptosis. JPS004 can be used for the research of cancer . (Structure Note: Pink: HDAC1-3 ligand (HY-50934); Blue: VHL ligand (HY-125845); HDAC1-3 ligand-Linker: (HY-176905))
|
-
- HY-145514
-
|
|
PROTACs
FKBP
|
Cancer
|
|
dTAGV-1 TFA is a potent and selective degrader of FKBP12 F36V-tagged proteins PROTAC degrader. dTAGV-1 TFA can induce degradation of FKBP12 F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A))
|
-
- HY-W584534
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032-CH2-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-CH2-Boc will remove the protecting group under acidic conditions and be directly used in PROTAC molecule synthesis. VH032-CH2-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.
|
-
- HY-168234
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2-degrader-36 (compound 38) is a SMARCA2 degrader and can reach the the degradation rate of 99 % at the 100 nM in H929 cells. PROTAC SMARCA2-degrader-36 shows anti-proliferative activity and can be used for study of cancer(Structure Note: PINK SMARCA2 ligand HY-44012; Blue, VHL ligand (HY-112078); Black, linker HY-W014125) .
|
-
- HY-131168
-
|
VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH (VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH) is a E3 ligase ligand-linker conjugate that contains on one end a VHL ligand. (S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH is used in PROTAC technology .
|
-
- HY-170859A
-
|
|
PROTACs
Casein Kinase
|
Cancer
|
|
AH081 (Compound 38) is a CK1δ/ε PROTAC degrader. AH081 is the negative control compound of AH078 (HY-170859). AH081 has inhibitory but no degradation activity for CK1δ/ε by using an inactive stereoisomer of the VHL ligand . Pink: CK1δ/ε ligand (HY-148251); Blue: VHL ligase ligand (HY-125845B); Black: linker
|
-
- HY-W584525
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032-NH-CO-CH2-NHBoc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL to recruit von Hippel-Lindau (VHL) proteins. VH032-NH-CO-CH2-NHBoc will remove the Boc protection under acidic conditions, and connect with the target protein ligand through a linker to form a PROTAC molecule, which is a key intermediate for the synthesis of PROTAC based on VHL ligand.
|
-
- HY-W584535
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-C3-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-C3-Boc will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032-C3-Boc is a key intermediate for the synthesis of PROTACs based on VHL ligands.
|
-
- HY-163216
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
PROTAC PTK6 ligand-O-4,4-dimethylpiperidine-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. PROTAC PTK6 ligand-O-4,4-dimethylpiperidine-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-136001
-
|
|
PROTACs
α-synuclein
|
Neurological Disease
|
|
PROTAC α-synuclein degrader 3 (Compound 5) is a selective α-synuclein PROTAC degrader. PROTAC α-synuclein degrader 3 can promote the ubiquitination and degradation of α-synuclein. PROTAC α-synuclein degrader 3 can be used for Parkinson's disease research (Pink: target protein ligand (HY-W278021); Black: linker; HY-133302; Blue: E3 ligase VHL ligand (HY-112078)) .
|
-
- HY-143275
-
|
|
PROTACs
PI3K
Akt
|
Cancer
|
|
HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042)) .
|
-
- HY-160415A
-
|
|
PROTACs
Apoptosis
METTL3
|
Cancer
|
|
WD6305 TFA is a potent and selective METTL3-METTL14 PROTAC degrader. WD6305 TFA has DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. WD6305 TFA inhibits m 6A modification and proliferation of AML cells, and induces apoptosis. WD6305 TFA has antitumor activity .(Pink: UZH2 (HY-115717); Black: Linker; Blue: VHL ligand (HY-150803))
|
-
- HY-163215
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S)-PROTAC PTK6 ligand-O-4,4-dimethylpiperidine-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S)-PROTAC PTK6 ligand-O-4,4-dimethylpiperidine-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-W584531
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-C6-NH-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-C6-NH-Boc will remove the protecting group under acidic conditions and be directly used in PROTAC molecule synthesis. VH032-C6-NH-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.
|
-
- HY-163228
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
PROTAC PTK6 ligand-O-C2-O-piperidine-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. PROTAC PTK6 ligand-O-C2-O-piperidine-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-136006A
-
|
VH032-C6-NH2 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Inflammation/Immunology
Cancer
|
|
(S,R,S)-AHPC-C6-NH2 hydrochloride (VH032-C6-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1 .
|
-
- HY-153119
-
|
|
PROTACs
PIKfyve
|
Inflammation/Immunology
|
|
TMX-4153 is a selective PIP4K2C PROTAC degrader. TMX-4153 induces PIP4K2C degradation in MOLT4 cells (DC50 = 24 nM) and HAP1 cells (DC50 = 361 nM). TMX-4153 can be used for the study of biological functions of PIP4K2C (immune modulation)-related diseases. (Pink: BTK ligand (HY-177432), Blue: VHL Ligand (HY-112078), Black: Linker) .
|
-
- HY-169264
-
|
|
PROTACs
Pregnane X Receptor (PXR)
|
Cancer
|
|
SJYHJ-026 (compound 37) is a pregnane X receptor (PXR) PROTAC degrader with the DC50 of 86.6 nM and maximal degradation of 66.4%. SJYHJ-026 shows cell cytotoxic aganist SNU-C4 HiBiT-PXR KI cells with the IC50 values of 97.4 μM (24 h) and 99.5 μM (72 h) (Blue: VHL ligand HY-125845,Black: linker HY-43048;Pink: PXR inhibitor HY-169277) .
|
-
- HY-133487
-
|
VH032-C8-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Inflammation/Immunology
Cancer
|
|
(S,R,S)-AHPC-C8-NH2 dihydrochloride (VH032-C8-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1 .
|
-
- HY-W584529
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-C2-NH-Boc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-C2-NH-Boc will remove the protecting group under acidic conditions, and can be directly used for the synthesis of PROTAC molecules. VH032-C2-NH-Boc is a key intermediate for the synthesis of PROTACs based on VHL ligands.
|
-
- HY-164995
-
|
|
PROTACs
Epigenetic Reader Domain
Drug-Linker Conjugates for ADC
|
Cancer
|
|
L1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments. (Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-171663)) .
|
-
- HY-163224
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S)-PROTAC PTK6 ligand-O-C2-O-piperidine-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S)-PROTAC PTK6 ligand-O-C2-O-piperidine-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-148030
-
|
|
PROTACs
LRRK2
|
Neurological Disease
|
|
XL01126 is a potent LRRK2 PROTAC (DC50: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)) composed of the VHL ligand VH 101, thiol (HY-47851, blue part) and the LRRK2 inhibitor HG-10-102-01 (HY-13488, red part). XL01126 crosses the blood-brain barrier and is used as a degradation probe in Parkinson's disease research. XL01126 can be used to study the non-catalytic and framework functions of LRRK2 .
|
-
- HY-181356
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
(S,R,S,R)-AHPC-Me-CO-C7-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S,R)-AHPC-Me based VHL ligand and a linker used in PROTAC technology. (S,R,S,R)-AHPC-Me-CO-C7-N3 can be connected to the ligand for protein by a linker to form PROTAC EZH2 Degrader-28 (HY-181355) .
|
-
- HY-W584530
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-C4-NH-Boc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL to recruit von Hippel-Lindau (VHL) proteins. VH032-C4-NH-Boc will remove the protecting group under acidic conditions and be directly used in PROTAC molecule synthesis. VH032-C4-NH-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.
|
-
- HY-136006
-
|
VH032-C6-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Inflammation/Immunology
Cancer
|
|
(S,R,S)-AHPC-C6-NH2 dihydrochloride (VH032-C6-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 dihydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1 .
|
-
- HY-128600
-
ERD-308
1 Publications Verification
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity. (Pink: Target Protein Ligand (HY-48027); Black: Linker (HY-172643); Blue: VHL Ligand (HY-112078); VHL Ligand+Linker:(HY-172645))
|
-
- HY-136186A
-
|
VH032-C7-amine dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine dihydrochloride is the dihydrochloride form of (S,R,S)-AHPC-C7-amine (HY-136186). (S,R,S)-AHPC-C7-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker. (S,R,S)-AHPC-C7-amine can be used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-133487B
-
|
VH032-C8-NH2
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E3 Ligase Ligand-Linker Conjugates
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Inflammation/Immunology
Cancer
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(S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized?E3 ligase ligand-linker conjugate?that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1 .
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- HY-W584533
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
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VH032-PEG2-NH-BOC is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-PEG2-NH-BOC will remove the protecting group under acidic conditions and be directly used for PROTAC molecule synthesis. VH032-PEG2-NH-BOC is a key intermediate in the synthesis of PROTAC based on VHL ligand.
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-
- HY-174920
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-34 (Compound MZ2) is a selective BRD4 PROTAC degrader (pDC50 = 8.4). PROTAC BRD4 Degrader-34 can induce BD2 degradation mediated by VHL. PROTAC BRD4 Degrader-34 can be used for research on cancer. (Pink: BRD4-BD2 Ligand (HY-78695); Blue: VHL Ligand (HY-125845); Black: Linker (HY-130524)) .
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- HY-163217
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
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PROTAC PTK6 ligand-2,7-diazaspiro[3.5]nonane-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. PROTAC PTK6 ligand-2,7-diazaspiro[3.5]nonane-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
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-
- HY-130711A
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VH032-C3-NH2 TFA
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
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- HY-130711
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VH032-C3-NH2
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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|
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
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-
- HY-186146A
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SGI-1776-cis-VHL-02
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Drug Isomer
Pim
c-Myc
Apoptosis
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Cancer
|
|
SGI-1776-VHL-02-epimer (SGI-1776-cis-VHL-02) is an epimer control compound of with SGI-1776-VHL-02 (HY-186146). SGI-1776-VHL-02-epimer has an inverted stereocenter in the critical hydroxyl-proline group in the VHL ligand. SGI-1776-VHL-02-epimer cannot trigger the VHL E3 ligase complex and does not degrade PIM1 .
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-
- HY-145703
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PROTACs
SHP2
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Cancer
|
|
SHP2-D26 isomer-1 is an isoform of SHP2-D26 (HY-145162). SHP2-D26 isomer-1 cannot degrade SHP2 at 3-1000 nM. SHP2-D26 is a PROTAC SHP2 degrader. (Pink: SHP2 ligand (HY-176797); Blue: Isomer control of VHL Ligand 14 (HY-150803); Black: linker) .
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- HY-114323
-
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PROTACs
FLT3
Apoptosis
STAT
MEK
ERK
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Cancer
|
|
PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845)) .
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-
- HY-178467
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FAK
PROTACs
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Cancer
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|
PROTAC FAK degrader 4 (Compound 9C) is an efficient and selective FAK PROTAC degrader. PROTAC FAK degrader 4 has a DC50 of 3.6 nM in MDA-MB-231 cells. PROTAC FAK degrader 4 significantly inhibits tumor cell proliferation, migration, and invasion, and enhances chemotherapy sensitivity to cisplatin (HY-17394). PROTAC FAK degrader 4 can be used for research on cancer. (Pink: FAK Ligand (HY-43760); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W208616))
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-
- HY-168487
-
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DNA/RNA Synthesis
PROTACs
WDR5
|
Others
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|
PROTAC WDR5 degrader 1 (compound 8g) is a PROTAC degrader targeting WDR5. PROTAC WDR5 degrader 1 is composed of a target protein ligand (red part) WDR5 ligand 2 (HY-168488), a VHL-type E3 ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and a PROTAC linker (balck part) 5-Aminovaleric acid (HY-W015878), in which the VHL ligand and the PROTAC linker form a conjugate (HY-114176A) .
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-
- HY-W584532
-
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-O-C2-NH-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-O-C2-NH-Boc will remove the protecting group under acidic conditions and can be directly used in PROTAC molecule synthesis. VH032-O-C2-NH-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.
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-
- HY-138632
-
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PROTACs
Epigenetic Reader Domain
PROTAC-Linker Conjugates for PAC
|
Cancer
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PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC50 values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)) .\n
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-
- HY-125834
-
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PROTACs
Bcr-Abl
Apoptosis
STAT
JAK
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Cancer
|
|
GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .
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-
- HY-145162
-
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|
PROTACs
SHP2
Phosphatase
|
Cancer
|
|
SHP2-D26 is a first, potent and effective SHP2 PROTAC degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent. SHP2-D26 can be used for the study of esophageal cancer and acute myeloid leukemia (Pink: SHP2 ligand (HY-176797); Blue: VHL ligand (HY-150803); Black: linker) .
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- HY-131387
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 can be used in PROTAC BRD4 Degrader-5 (HY-133737) and PROTAC BRD4 Degrader-5-CO-PEG3-N3 (HY-133736) .
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-
- HY-130816
-
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VH032-O-Ph-PEG1-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02 .
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-
- HY-174856
-
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PROTACs
HBV
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Infection
|
|
PROTAC HBeAg degrader-1 is a PROTAC targeting degradation agent for HBeAg. PROTAC HBeAg degrader-1 recruits the VHL E3 ligase but degrades HBV protein HBeAg through VHL-independent mechanism. PROTAC HBeAg degrader-1 decreases levels of secreted and intracellular HBeAg. PROTAC HBeAg degrader-1 can be used for the research of hepatitis B virus (HBV) . (Structure Note: Pink: HBeAg ligand (HY-174857); Blue: VHL Ligand (HY-125845); Black: linker; E3-linker (HY-135045))
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-
- HY-163231
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-CO-CH2-azetidine-piperazine-CH2-COOH is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S,R,S)-AHPC-CO-CH2-azetidine-piperazine-CH2-COOH can be used as a key intermediate for the synthesis of complete PROTAC molecules.
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-
- HY-130604
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DT2216
2 Publications Verification
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Bcl-2 Family
PROTACs
Apoptosis
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Cancer
|
|
DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax-piperazine (HY-44432), a linker, and a VHL E3 ubiquitin ligase (Pink: Navitoclax-piperazine; Blue: VHL ligand; Black: linker) .
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-
- HY-163220
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-CO-CH2-O-CH2-piperidine-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S,R,S)-AHPC-CO-CH2-O-CH2-piperidine-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
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-
- HY-164977
-
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PROTACs
Phosphatase
|
Cancer
|
|
JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3
ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC50 in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230)) .
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-
- HY-163223
-
|
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-CO-CH2-piperazine-C3-piperazine-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S,R,S)-AHPC-CO-CH2-piperazine-C3-piperazine-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
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-
- HY-145479
-
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|
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR-V7 degrader-1 is an orally active and selective AR-V7 PROTAC degrader with a DC50 of 0.32 μM (in 22Rv1 cells). PROTAC AR-V7 degrader-1 can inhibit the proliferation of tumor cells and exhibit anti-tumor activity. PROTAC AR-V7 degrader-1 can be used for the research of cancers such as prostate cancer .(Pink: VPC-14228 (HY-117669); Black: linker (HY-W041652); Blue: VHL Ligand (HY-112078))
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-
- HY-149760
-
|
|
PROTACs
Phosphatase
IFNAR
STAT
|
Cancer
|
|
PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). PVD-06 induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. PVD-06 can be used to further investigate PTPN2 in diseases such as leukemia and melanoma . (Pink: PTPN2 ligand (HY-168691), Black: linker (HY-B0236), Blue: VHL ligand (HY-112078)).
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-
- HY-W999557
-
|
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(R,S,S)-VH032-PEG5-N3 is an E3 ligase ligand-linker conjugate comprising a VHL ligand based on VH032 and a 5-unit PEG linker. (R,S,S)-VH032-PEG5-N3 is a click chemistry reagent. It contains an azide group and can undergo copper-catalyzed azido-azynylene cycloaddition (CuAAc) with molecules containing an alkyne group. It can also undergo ring-strain-driven alkyne-azido cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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-
- HY-112495
-
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HaloPROTAC 2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. VH032-PEG5-C6-Cl incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
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-
- HY-158429
-
|
|
PROTACs
Cytochrome P450
|
Cancer
|
|
PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC50 of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006) .
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-
- HY-169093
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078) .
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-
- HY-170620
-
|
|
PROTACs
PARP
|
Cancer
|
|
PARP1 PROTAC 180055 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)) .
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-
- HY-134303
-
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PROTAC CDK4/6 degrader 34
|
PROTACs
CDK
|
Cancer
|
|
CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin dependent kinase CDK4/6 PROTAC degrader. CST651 can degrade CDK4 and CDK6 in MM.1S cells with DC50 values of 20 and 5.1 nM. CST651 can inhibit cancer cells proliferation and migration. CST651 can be used for the research of cancer, such as acute lymphoblastic leukemia . (Structure Note: Pink: CDK4/6 ligand (HY-50767); Blue: VHL ligand (HY-125905); Black: linker (HY-W017440))
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-
- HY-125878
-
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SGK3-PROTAC1
|
PROTACs
SGK
|
Cancer
|
|
PROTAC SGK3 degrader-1 (SGK3-PROTAC1), a chemical probe, is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate) .
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- HY-136420
-
|
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PROTACs
Raf
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
SJF-0628 is a RAF PROTAC degrader. SJF-0628 induces targeted degradation of BRAF in various cancer cell lines (colorectal cancer cell lines (Colo-205, LS-411N, HT-29, RKO) and triple-negative breast cancer cell line DU-4475). SJF-0628 decreases pMEK and pErk levels in DU-4475 cells. SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of colorectal cancer and triple-negative breast cancer. (Pink: RAF ligand (HY-12057), Blue: VHL Ligand ( HY-125845), Black: Linker (HY-B0912)) .
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-
- HY-163897
-
|
|
PROTACs
Ferroptosis
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
|
PROTAC NCOA4 degrader-1 is a VHL-based PROTAC NCOA4 degrader. PROTAC NCOA4 degrader-1 is a ferroptosis inhibitor. PROTAC NCOA4 degrader-1 reduces Fe 2+ elevation, ROS production, MDA content and PTGS2 mRNA expression. PROTAC NCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model. PROTAC NCOA4 degrader-1 can be used for the researches of inflammation and immunology. (Pink: NCOA4 ligand (HY-149457). Black: linker (HY-163903). Blue: VHL ligand (HY-138678B)) .
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- HY-130711C
-
|
VH032-C3-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 (dihydrochloride) is the dihydrochloride form of (S,R,S)-AHPC-C3-NH2 (HY-130711). (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
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-
- HY-161176
-
|
|
PROTACs
Ras
ERK
|
Cancer
|
|
PROTAC KRAS G12D degrader 1 is a selective PROTAC KRAS G12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRAS G12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRAS G12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893)) .
|
-
- HY-173333
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343)) .
|
-
- HY-159175
-
|
|
PROTACs
Deubiquitinase
Apoptosis
MDM-2/p53
|
Cancer
|
|
XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)) .
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- HY-178065
-
|
|
PROTACs
Histone Methyltransferase
GLP Receptor
|
Cancer
|
|
PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468)) .
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-
- HY-155994
-
|
|
PROTACs
PIKfyve
Autophagy
|
Cancer
|
|
PIK5-12d is a PROTAC PIKfyve degrader (DC50 = 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d significantly suppresses tumor proliferation in mice bearing LTL-331R human prostate cancer PDX tumors. PIK5-12d can be used for the study of prostate cancer. (Pink: PIKfyve ligand (HY-175631), Blue: VHL Ligand (HY-125845), Black: Linker, PIKfyve ligand-linker conjugate (HY-175632)) .
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- HY-160924
-
|
|
PROTACs
BMI1
E1/E2/E3 Enzyme
Histone Methyltransferase
|
Cancer
|
|
MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H2A Lys119 mono-ubiquitination without altering histone H3 Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma . (Pink: BMI1/RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker)
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- HY-165298
-
|
|
PROTACs
FGFR
ERK
|
Cancer
|
|
DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers. (Pink: FGFR1/2 ligand (HY-160013), Blue: VHL Ligand (HY-112078), Black: Linker (HY-W020017)) .
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- HY-175767
-
|
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PROTACs
Epigenetic Reader Domain
|
Cancer
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PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC50 value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))
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- HY-111997
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HaloPROTAC 3
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E3 Ligase Ligand-Linker Conjugates
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Others
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VH285-PEG4-C4-Cl (HaloPROTAC 3) is a conjugate of ligands for E3 and 16-atom-length linker. The connector of linker is Halogen group. VH285-PEG4-C4-Cl incorporates the VH285 based VHL ligand and an alkyl/ether-based linker. VH285-PEG4-C4-Cl is a highly potent and efficacious degrader of GFP-HaloTag7 with a DC50 of 19 nM. VH285-PEG4-C4-Cl is able to induce 90 % degradation of GFP-Halotag at 625 nM. VH285-PEG4-C4-Cl binds to VHL with an IC50 of 0.54 μM .
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- HY-176823
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PROTACs
SGK
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Cancer
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PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation. (Pink: SGK3 ligand (HY-167701), Blue: VHL Ligand (HY-120217A), Black: Linker (HY-130618), SGK3 ligand-linker conjugate (HY-176824)) .
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- HY-181906
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PROTACs
Reactive Oxygen Species (ROS)
CDK
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Cancer
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ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC) .
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- HY-114402
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PROTACs
Androgen Receptor
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Cancer
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ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
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- HY-130654
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VH032-C2-PEG4-N3
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM . (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-174469
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PROTACs
P-glycoprotein
Apoptosis
Reactive Oxygen Species (ROS)
Akt
Bcl-2 Family
Na+/K+ ATPase
PI3K
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Cancer
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PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer. (Pink: PI3K/110β Ligand (HY-75124); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W002042)) .
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| Cat. No. |
Product Name |
Type |
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- HY-D2413
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BODIPY FL PEG4-VH032
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Fluorescent Dyes
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BODIPY FL VH032 is a high-affinity VHL fluorescent probe with a Kd value of 3.01 nM. BODIPY FL VH032 consists of von Hippel-Lindau (VHL) ligand VH032 (HY-120217) and BODIPY FL (HY-43520). BODIPY FL VH032 can be used for time-resolved fluorescence resonance energy transfer (TR-FRET) detection for high-throughput identification and characterization of VHL ligands with maximum excitation emission wavelength: 504/520 nm .
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| Cat. No. |
Product Name |
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Classification |
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- HY-103601
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VH032-PEG4-N3; VHL ligand-Linker Conjugates 5; E3 ligase ligand-Linker Conjugates 4
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Azide
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(S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-126456
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VH032-propargyl; VHL ligand 7
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PROTAC Synthesis
Alkynes
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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-103598
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VH032-PEG3-N3; VHL ligand-Linker Conjugates 8; E3 ligase ligand-Linker Conjugates 12
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Azide
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(S,R,S)-AHPC-PEG3-N3 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. (S,R,S)-AHPC-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-103600
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VH032-PEG1-N3; VHL ligand-Linker Conjugates 9; E3 ligase ligand-Linker Conjugates 3
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Azide
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(S,R,S)-AHPC-PEG1-N3 (VH032-PEG1-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-114402
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PROTAC Synthesis
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ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
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- HY-128767
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Alkynes
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VH032-PEG3-acetylene is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology . VH032-PEG3-acetylene 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-103599
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VH032-PEG2-N3; VHL ligand-Linker Conjugates 6; E3 ligase ligand-Linker Conjugates 13
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Azide
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(S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-N3 can be used for the synthesis of PROTACs .
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- HY-159147
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Azide
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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- HY-130654
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VH032-C2-PEG4-N3
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Azide
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(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM . (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-W1130361
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Azide
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(S,R,S)-AHPC-PEG5-Azide is a VHL ligand based on (S,R,S)-AHPC that recruits von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-PEG5-Azide can be linked to a target protein ligand via a linker to form a PROTACs.
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- HY-159457
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Azide
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PROTAC SMARCA2/4-degrader-6 (compound I-438) is a SMARCA2/4 degrader. PROTAC SMARCA2/4-degrader-6 has the potential for the research of cancer. (Pink: SMARCA2/4 ligand, (HY-159545); Black: linker (HY-W006635); Blue: VHL ligand (HY-112078)) .
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- HY-181356
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Azide
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(S,R,S,R)-AHPC-Me-CO-C7-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S,R)-AHPC-Me based VHL ligand and a linker used in PROTAC technology. (S,R,S,R)-AHPC-Me-CO-C7-N3 can be connected to the ligand for protein by a linker to form PROTAC EZH2 Degrader-28 (HY-181355) .
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