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von Hippel-Lindau (VHL) E3 ligase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E3 Ligase Ligand-Linker Conjugates (2) Ligands for E3 Ligase (29) Apoptosis (3) Bcl-2 Family (1) Bcr-Abl (2) FKBP (1) GLP Receptor (1) HDAC (6) HIF/HIF Prolyl-Hydroxylase (1) Histone Methyltransferase (1) Ligands for Target Protein for PROTAC (1) PROTACs (14) Ras (1)
By Research Areas:	Cancer (41)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Screening Libraries

Click Chemistry

Targets Recommended: Ligands for E3 Ligase E3 Ligase Ligand-Linker Conjugates E1/E2/E3 Enzyme

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-160555A

(S,R,S)-AHPC-CO-C9-NH2 hydrochloride	Ligands for E3 Ligase	Cancer
(S,R,S)-AHPC-CO-C9-NH2 (hydrochloride) is a von Hippel-Lindau (VHL) amino building block that can be used to synthesize E3 ligase ligands required for PROTACs..

HY-157590

E3 ligase Ligand-Linker Conjugate 32	Ligands for E3 Ligase	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 Conjugate 35	Ligands for E3 Ligase	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 Conjugate 40	Ligands for E3 Ligase	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 Conjugate 42	Ligands for E3 Ligase	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 Conjugate 46	Ligands for E3 Ligase	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 Conjugate 91	Ligands for E3 Ligase	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 Conjugate 101	Ligands for E3 Ligase 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 Conjugate 102	Ligands for E3 Ligase	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 Conjugate 103	Ligands for E3 Ligase	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 Conjugate 27	Ligands for E3 Ligase	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 Conjugate 50	Ligands for E3 Ligase	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-128756

SIAIS178	PROTACs Bcr-Abl	Cancer
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC₅₀ of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting **Von Hippel-Lindau** (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity .

HY-153119

TMX-4153	Ligands for Target Protein for PROTAC	Others
TMX-4153 is a bivalent degrader. TMX-4153 rapidly and selectively degrades endogenous PIP4K2C by recruiting the von Hippel-Lindau (VHL) E3 ligase complex, with a K_D value of 42 nM. TMX-4153 can be used to synthesize PROTAC .

HY-145815

JPS014	HDAC PROTACs	Cancer
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-145816

JPS016	HDAC PROTACs	Cancer
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-145818

JPS035	HDAC PROTACs	Cancer
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-145819

JPS036	HDAC PROTACs	Cancer
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-145816A

JPS016 TFA	HDAC PROTACs	Cancer
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-156106

VHL-IN-1	PROTACs Ligands for E3 Ligase HIF/HIF Prolyl-Hydroxylase	Cancer
VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) .

HY-145815A

JPS014 TFA	PROTACs HDAC Apoptosis	Cancer
JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-162250

MS8847	PROTACs Histone Methyltransferase	Cancer
MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase **von Hippel-Lindau (VHL)**. MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells .

HY-138678

(R,S,S)-VH032	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-47070

VH 101, acid	Ligands for E3 Ligase	Others
VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. VH 101, acid contains an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand .

HY-42424

(S,R,S)-AHPC-Me hydrochloride VHL ligand 2 hydrochloride; E3 ligase Ligand 1	Ligands for E3 Ligase	Cancer
(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 .

HY-112078

(S,R,S)-AHPC-Me VHL ligand 2; E3 ligase Ligand 1A	Ligands for E3 Ligase	Cancer
(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 .

HY-42424A

(S,R,S)-AHPC-Me dihydrochloride VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride	Ligands for E3 Ligase	Cancer
(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 .

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-161194

(S,R,S)-AHPC-acetyl-azetidine-PIP-boc	Ligands for E3 Ligase	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

(S,R,S)-AHPC-acetyl-Pip-O-azetidine-boc	Ligands for E3 Ligase	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-163216

PROTAC PTK6 ligand-O-4,4-dimethylpiperidine-Boc	Ligands for E3 Ligase	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-139335

VH 101 phenol-alkylC4-amine dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
VH 101 phenol-alkylC4-amine dihydrochloride is a von-Hippel-Lindau protein ligand (VHL), and incorporates an E3 ligase ligand plus an alkylC4 linker. VH 101 phenol-alkylC4-amine dihydrochloride can be used for PROTAC research extracted from patent WO2022051326A1.

HY-136005

VH032-C7-COOH	Ligands for E3 Ligase	Others
VH032-C7-COOH is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. VH032-C7-COOH contains an E3 ligase ligand and an alkyl linker with a terminal amine for conjugation of target protein ligands .

HY-163215

(S)-PROTAC PTK6 ligand-O-4,4-dimethylpiperidine-Boc	Ligands for E3 Ligase	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

(S)-PROTAC PTK6 ligand-O-C2-O-piperidine-Boc	Ligands for E3 Ligase	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

PROTAC PTK6 ligand-O-C2-O-piperidine-Boc	Ligands for E3 Ligase	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-162362

MS8709	PROTACs GLP Receptor	Cancer
MS8709 (10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 (10) 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-125834

GMB-475	PROTACs Bcr-Abl Apoptosis	Cancer
GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent agent resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase **Von Hippel Lindau** (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein .

HY-163217

PROTAC PTK6 ligand-2,7-diazaspiro[3.5]nonane-Boc	Ligands for E3 Ligase	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-163220

(S,R,S)-AHPC-CO-CH2-O-CH2-piperidine-Boc	Ligands for E3 Ligase	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

(S,R,S)-AHPC-CO-CH2-piperazine-C3-piperazine-Boc	Ligands for E3 Ligase	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

(S,R,S)-AHPC-CO-CH2-azetidine-piperazine-CH2-COOH	Ligands for E3 Ligase	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-137516

LC-2 1 Publications Verification	PROTACs Ras	Cancer
LC-2 is a potent and first-in-class **von Hippel-Lindau**-based PROTAC capable of degrading endogenous KRAS G12C, with DC₅₀s between 0.25 and 0.76 μM . LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines .

HY-145514A

dTAGV-1-NEG

PROTACs FKBP Cancer

dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12 ^F36V-selective degrader .

dTAGV-1-NEG	PROTACs FKBP	Cancer
dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12 ^F36V-selective degrader .

E3 Ligase Ligand Library	88 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2). MCE carefully prepared a unique collection of 88 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

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