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-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-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-101763A
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VH032-NH2 monohydrochloride; VHL ligand 1 monohydrochloride
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Ligands for E3 Ligase
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Others
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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-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-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-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-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-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-163219
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- HY-111824
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VHL ligand-Linker Conjugates 14; E3 ligase ligand-Linker Conjugates 29
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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.
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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-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-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-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-101763B
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VH032-NH2 dihydrochloride; VHL ligand 1 dihydrochloride
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Ligands for E3 Ligase
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Cancer
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(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 .
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- HY-125846
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VH032-PEG1-OTs; VHL ligand-Linker Conjugates 2; E3 ligase ligand-Linker Conjugates 51
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(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.
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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-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-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 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-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-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-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-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-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-103602B
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VH032-PEG3-NH2 dihydrochloride; VHL ligand-Linker Conjugates 1 dihydrochloride; E3 ligase ligand-Linker Conjugates 5 dihydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG3-NH2 dihydrochloride (VH032-PEG3-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology
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- HY-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-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-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 used in PROTAC technology. (S,R,S)-AHPC-PEG2-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 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-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-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-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-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-111663
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- HY-47851
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- HY-161367
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- HY-112078A
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Others
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Others
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(S,R,S,R)-AHPC-Me serves as a VHL ligand that facilitates the recruitment of the VHL protein.
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- HY-49514
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Ligands for E3 Ligase
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Cancer
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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 .
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- HY-49515
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Ligands for E3 Ligase
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Cancer
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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 .
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- HY-148896
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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-400254
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Ligands for E3 Ligase
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Others
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cis VH032 amine dihydrochloride is a VHL ligand with a Ki of 5.7 μM. cis VH032 amine dihydrochloride can be used to regulate hypoxia signaling pathways and to study chronic anemia or ischemia .
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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-161368
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- HY-138678B
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- HY-162450
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PROTACs
MDM-2/p53
Apoptosis
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Cancer
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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) .
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- HY-136163A
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- HY-138862
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(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 .
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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-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-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-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-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-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 .
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- HY-131959
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- HY-138861
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(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 .
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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-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-136165
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(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 .
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- HY-148406
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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-158142
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PROTACs
JAK
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Cancer
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PROTAC TYK2 degrader-1 (CPD-155) is a PROTAC targeting degrader to TYK2 with Dmax >60%. (Srtucture Note: PINK, TYK2 ligand 1 (HY-158340); Blue, VHL ligand Thalidomide (HY-14658); Black, linker)
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- HY-151227
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Others
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Cancer
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VL285 Phenol is a VL285 analogue with Phenol group. VL285, a small molecule VHL ligand, can be served as a degrader for HaloPROTAC3 synthesis.VL285 degrades HaloTag7 fusion proteins (IC50=0.34 μM) .
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- HY-44432
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ABT-263-piperazine
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Bcl-2 Family
Ligands for Target Protein for PROTAC
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Cancer
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Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor. Navitoclax-piperazine and a VHL ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC DT2216 (HY-130604) with anti-tumor activity .
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- HY-120217
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VH032
3 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-130798
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E3 Ligase Ligand-Linker Conjugates
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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-111905
-
|
Epigenetic Reader Domain
|
Cancer
|
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) .
|
-
- HY-156568A
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
SMD-3040 TFA is a selective degrader of SMARCA2. SMD-3040 TFA contains SMARCA2/4 ligands, linker and VHL ligands and can be used for PROTAC drug synthesis. SMD-3040 TFA exhibits strong tumor growth inhibition in tumor xenograft models .
|
-
- 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 (Srtucture Note: Red, STING agonist diABZI (HY-112921A); Blue, VHL ligand VH032 (HY-120217); Black, linker) .
|
-
- HY-125845A
-
(S,S,S)-VH032-NH2 hydrochloride
|
Ligands for E3 Ligase
|
Cancer
|
(S,S,S)-AHPC 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. (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein .
|
-
- 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-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-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-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-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-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-139218
-
-
- 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-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-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-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-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-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-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-168229
-
|
PROTACs
|
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 (blue: VHL ligand (HY-168232); black: linker, (HY-168231); pink: SMARCA2 ligand, (HY-168230)) .
|
-
- 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-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-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 treatment research .
|
-
- 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-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-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-400685
-
|
Others
|
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-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-162608
-
|
PROTACs
|
Cancer
|
PROTAC JAK1 degrader 1 degrader 1 (compound 10c) is an effective and selective PROTAC JAK1 degrader with a DC50 of 214 nM. PROTAC JAK1 degrader 1 has antitumor activity. (Structure Note: PINK, JAK1 ligand 1 (HY-10961); Blue, VHL ligand Thalidomide (HY-14658); Black, linker) .
|
-
- 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.
(Srtucture Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .
|
-
- HY-156568
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models .
|
-
- 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-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-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-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-135345
-
|
PROTACs
FKBP
|
Cancer
|
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 .
|
-
- 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-130815
-
-
- 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-130815A
-
-
- 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-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-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-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-13001
-
Quizartinib
Maximum Cited Publications
31 Publications Verification
AC220; AC708
|
FLT3
Ligands for Target Protein for PROTAC
Apoptosis
|
Cancer
|
Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
|
-
- 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-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-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-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-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(Srtucture Note: PINK SMARCA2 ligand HY-44012; Blue, VHL ligand (HY-112078); Black, linker HY-W014125) .
|
-
- 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-133487B
-
VH032-C8-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Inflammation/Immunology
Cancer
|
(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 .
|
-
- 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-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-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-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-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-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-W584533
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
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.
|
-
- 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-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-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-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-158036
-
|
PROTACs
STING
|
Others
Inflammation/Immunology
|
PROTAC STING degrader-2 is a protein Degrader that targets Stimulator of interferon genes (STING) (DC50=0.53 μM). PROTAC STING Degrader-2 is combined with STING protein and E3 ubiquitin ligase in a covalent manner to induce the degradation of STING protein. PROTAC STING Degrader-2 can be used to investigate the role of STING in autoinflammation and autoimmune diseases (PINK: STING binder (HY-145009); Blue: VHL ligand (HY-164043); Black: linker) .
|
-
- HY-162930
-
|
PROTACs
METTL3
|
|
PROTAC METTL3 degrader 1 (Compound KH12) is a VHL-based PROTAC METTL3 degrader (DC50: 220 nM in MOLM-13 cells). PROTAC METTL3 degrader 1 inhibits METTL3/14 complex with an IC50 value of 341 nM. PROTAC METTL3 degrader 1 has anti-proliferative activities against AML cells. Black: Linker (HY-ER002); Red: METTL3 ligand (HY-115717); Blue: VHL ligand (HY-120217) .
|
-
- HY-169264
-
|
PROTACs
|
Cancer
|
SJYHJ-026 (compound 37) is a pregnane X receptor (PXR) 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-130711
-
VH032-C3-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
(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 .
|
-
- HY-130711A
-
VH032-C3-NH2 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
(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 .
|
-
- HY-W584532
-
|
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.
|
-
- HY-163217
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
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.
|
-
- HY-13001R
-
|
FLT3
Ligands for Target Protein for PROTAC
Apoptosis
Autophagy
|
Cancer
|
Quizartinib (Standard) is the analytical standard of Quizartinib. This product is intended for research and analytical applications. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
|
-
- HY-14217
-
AC220 dihydrochloride
|
FLT3
Apoptosis
Ligands for Target Protein for PROTAC
|
Cancer
|
Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001). Quizartinib dihydrochloride is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis .
|
-
- HY-130816
-
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 .
|
-
- HY-125834
-
|
PROTACs
Bcr-Abl
Apoptosis
STAT
JAK
|
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)) .
|
-
- HY-131387
-
|
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) .
|
-
- 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.
|
-
- HY-163223
-
|
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.
|
-
- HY-163231
-
|
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.
|
-
- HY-130604
-
DT2216
1 Publications Verification
|
Bcl-2 Family
PROTACs
Apoptosis
|
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 (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker) .
|
-
- HY-112495
-
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 .
|
-
- 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) .
|
-
- HY-125878
-
SGK3-PROTAC1
|
PROTACs
SGK
|
Cancer
|
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 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) .
|
-
- HY-158684
-
|
PROTACs
MDM-2/p53
|
Cancer
|
YX-02-030M is a PROTAC MDM2 degrader. YX-02-030M inhibits MDM2-p53 binding and VHL-HIF1α binding with IC50s of 63 nM and 1.35 μM respectively. YX-02-030M binds MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, and effectively kills p53 mutant or deleted Triple-negative breast cancers (TNBC) cells. (Blue: VHL ligand; Black: linker; Pink: MDM2 inhibitor) .
|
-
- HY-163897
-
|
PROTACs
Ferroptosis
|
Inflammation/Immunology
|
PROTAC NCOA4 degrader-1 (Compound V3) is a PROTAC NCOA4 degrader (DC50: 3 nM in HeLa cells). PROTAC NCOA4 degrader-1 is a ferroptosis inhibitor. PROTAC NCOA4 degrader-1 reduces NCOA4 levels and downregulates intracellular ferrous iron (Fe 2+) levels. PROTAC NCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model. (Red: NCOA4 ligand (HY-149457). Black: linker (HY-163903). Blue: VHL ligand (HY-138678B)) .
|
-
- 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) .
|
-
- 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 .
|
-
- 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)) .
|
-
- HY-111997
-
HaloPROTAC 3
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
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 .
|
-
- HY-160924
-
|
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
MS147 is a VHL-based PROTAC degrader of PRC1 (Polycomb Repressive Complex 1). The dissociation constants (Kd) of MS147 for EED (Embryonic Ectoderm Development) and VHL (Von Hippel-Lindau) are 3.0 μM and 450 nM, respectively. MS147 specifically binds to the EED protein through its EED-binding moiety; EED is a core component of PRC2 (Polycomb Repressive Complex 2) and interacts with the core components of PRC1, BMI1 (B-lymphoma Mo-MLV insertion region 1 homolog) and RING1B (Ring Finger Protein 1B). By this binding, MS147 is able to recruit BMI1 and RING1B near to VHL. Through the degradation of BMI1 and RING1B, MS147 reduces the level of H2AK119ub (histone H2A lysine 119 ubiquitination), affecting the proliferation of cancer cells. (Blue: VHL ligand (HY-125845), Black: linker ; Pink: PRC1 ligand (HY-158771)) .
|
-
- HY-130654
-
VH032-C2-PEG4-N3
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
(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.
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-126456
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VH032-propargyl; VHL ligand 7
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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-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 used in PROTAC technology. (S,R,S)-AHPC-PEG2-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 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-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-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-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-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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