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Results for "

von Hippel-Lindau

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (2) Apoptosis (4) Autophagy (3) Bcl-2 Family (2) Bcr-Abl (3) CDK (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (36) EGFR (1) Epigenetic Reader Domain (22) ERK (1) Estrogen Receptor/ERR (3) FKBP (3) Fluorescent Dye (1) GLP Receptor (1) Glutaminase (1) HDAC (6) HIF/HIF Prolyl-Hydroxylase (2) Histone Methyltransferase (4) IRAK (1) JAK (1) Ligands for E3 Ligase (19) Ligands for Target Protein for PROTAC (1) MEK (2) Molecular Glues (3) p38 MAPK (2) PROTAC-Linker Conjugates for PAC (1) PROTACs (61) Ras (2) RIP kinase (1) SGK (1) STAT (4)
By Research Areas:	Cancer (120) Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (1)
Click Chemistry:	PROTAC Synthesis (1) Azide (1)

127

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Recombinant Proteins

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156106

VHL-IN-1	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-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-114229

PROTAC BET degrader-3 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET Degrader-3 is a PROTAC connected by ligands for **von Hippel-Lindau and BET**.

HY-111519

dTRIM24 5 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for **von Hippel-Lindau and TRIM24**.

HY-135382A

PROTAC IRAK4 degrader-3	IRAK PROTACs	Inflammation/Immunology
PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on **von Hippel-Lindau** .

HY-112376

MZP-54 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
MZP-54 is a PROTAC connected by ligands for **von Hippel-Lindau and BRD3/4, with a K_d** of 4 nM for Brd4 ^BD2.

HY-112377

MZP-55 1 Publications Verification	Epigenetic Reader Domain PROTACs	Cancer
MZP-55 is a PROTAC connected by ligands for **von Hippel-Lindau and BRD3/4, with a K_d** of 8 nM for Brd4 ^BD2.

HY-101028

ZINC13466751	HIF/HIF Prolyl-Hydroxylase	Cardiovascular Disease Cancer
ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC₅₀ of 2.0 µM .

HY-160555

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

HY-151479

GID4 Ligand 3	Others	Cancer
GID4 Ligand 3 (compound 16) is a binder of GID4 with an K_d value of 110 μM in vitro and an IC₅₀ value of 148.5 μM. GID4 Ligand 3 can be used for the research related to cereblon and Von Hippel-Lindau .

HY-135558

PROTAC BRD4 Degrader-3	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for **von Hippel-Lindau and BRD4** .

HY-111593

Homo-PROTAC pVHL30 degrader 1 1 Publications Verification	PROTACs	Cancer
Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC , consists of two ligands of **von Hippel-Lindau**.

HY-112375

AT6	PROTACs	Cancer
AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for **von Hippel-Lindau and BRD4** with highly selectivity to bromodomain (Brd4).

HY-139309

PROTAC Bcl-xL degrader-2	Bcl-2 Family PROTACs	Cancer
PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on **von Hippel-Lindau ligand, with an IC₅₀** of 0.6 nM.

HY-162553

GNE7599	Ligands for E3 Ligase	Cancer
GNE7599 is a high-affinity and orally active von Hippel-Lindau (VHL) ligand with a K_d of 540 pM. GNE7599 can be connected to the ligand for protein by a linker to form PROTACs .

HY-111433

BRD4 degrader AT1 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
BRD4 degrader AT1 is a PROTAC connected by ligands for **von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a K_d** of 44 nM for Brd4 ^BD2 in cells.

HY-129180

XY028-133	PROTACs CDK	Cancer
XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for **von Hippel-Lindau and CDK** .

HY-130708

UNC6852 2 Publications Verification	Histone Methyltransferase PROTACs	Cancer
UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a **von Hippel-Lindau ligand, with an IC₅₀** of 247 nM for EED .

HY-135345

PROTAC FKBP Degrader-3 1 Publications Verification	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-123109

(S,R,S)-AHPC-Boc VH032-Boc	Ligands for E3 Ligase	Cancer
(S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology .

HY-136257

CMP98	PROTACs	Others
CMP98, a PROTAC, is unable to induce degradation of VHL. CMP98 can be used as a negative control compound for CM11 . CMP98 consists of two **von Hippel-Lindau** ligands on their active domain.

HY-160555A

(S,R,S)-AHPC-CO-C9-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	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-101763A

(S,R,S)-AHPC monohydrochloride 1 Publications Verification VH032-NH2 monohydrochloride; VHL ligand 1 monohydrochloride	Ligands for E3 Ligase	Others
(S,R,S)-AHPC (VH032-NH2; VHL ligand 1) hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein .

HY-114405

SJFδ	PROTACs p38 MAPK Autophagy	Cancer
SJFδ is a 10-atom linker PROTAC based on **von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC₅₀** of 46.17 nM, but does not degrade p38α, p38β, or p38γ .

HY-133737

PROTAC BRD4 Degrader-5	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for **von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-5 can potent degrade BRD4** in HER2 positive and negative breast cancer cell lines .

HY-157512

SJF-0661	Ligands for E3 Ligase	Cancer
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 .

HY-130297

PROTAC BCR-ABL1 ligand 1	Bcr-Abl	Cancer
PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1 .

HY-130257

CP5V	PROTACs	Cancer
CP5V is a PROTAC connected by ligands for **von Hippel-Lindau and CDK, which specifically degrades Cdc20** by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation. CP5V induces mitotic inhibition and suppresses cancer cell proliferation .

HY-120217

VH032 3 Publications Verification	Ligands for E3 Ligase	Cancer
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 K_d

HY-141438

SIM1 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
SIM1 is a potent **von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC₅₀**=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer 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-155643

PROTAC TG2 degrader-1	PROTACs Glutaminase	Cancer
PROTAC TG2 degrader-1 (compound 11) is a von Hippel-Lindau (VHL)-based PROTAC targeting tissue transglutaminase (TG2) with a K_D of 68.9 μM. PROTAC TG2 degrader-1 reduces TG2 in ovarian cancer cells in a proteasome-dependent manner .

HY-123921

Gefitinib-based PROTAC 3 2 Publications Verification	PROTACs EGFR	Cancer
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a **von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC₅₀**s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively .

HY-114322

VZ185 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
VZ185 is a potent, fast, and selective **von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC₅₀**s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC₅₀s of 3 nM and 40 nM, respectively .

HY-125845A

(S,S,S)-AHPC hydrochloride 2 Publications Verification (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-44630

VH 032 amide-alkylC6-acid (S,R,S)-AHPC-CO-C6-COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
VH 032 amide-alkylC6-acid ((S,R,S)-AHPC-CO-C6-COOH) is a VH032 analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH 032 amide-alkylC6-acid can be used in the synthesis of PROTACs .

HY-130492

ARCC-4 1 Publications Verification	PROTACs Androgen Receptor	Cancer
ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC₅₀ of 5?nM. ARCC-4 is an enzalutamide-based **von Hippel-Lindau** (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy .

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-139185

PROTAC ERRα Degrader-3	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on **von Hippel-Lindau** ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins .

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-123109A

(S,S,S)-AHPC-Boc (S,S,S)-VH032-Boc	Others	Cancer
(S,S,S)-AHPC-Boc is the isomer of (S,R,S)-AHPC-Boc (HY-123109), and can be used as an experimental control. (S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology .

HY-114404

SJFα	PROTACs p38 MAPK Autophagy	Cancer
SJFα is a 13-atom linker PROTAC based on **von Hippel-Lindau ligand. SJFα degrades p38α with a DC₅₀** of 7.16 nM, but is far less effective at degrading p38δ (DC₅₀=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM .

HY-138633

PROTAC BRD4 Degrader-10	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-10 (compound 8b) is a PROTAC connected by ligands for **von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀** of 1.3 nM and 18 nM, respectively .

HY-138632

PROTAC BRD4 Degrader-9	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for **von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀** of 0.86 nM and 7.6 nM, respectively .

HY-138555

PROTAC BRD4 Degrader-8	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for **von Hippel-Lindau and BRD4, with IC₅₀s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2**, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .

HY-138634

PROTAC BRD4 Degrader-11	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-11 (compound 9a) is a PROTAC connected by ligands for **von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-11 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀** of 0.23 nM and 0.38 nM, respectively .

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library

54 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 54 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.

HY-L045

Oxygen Sensing Compound Library

2,691 compounds

Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

MCE offers a unique collection of 2,691 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Cat. No.	Product Name	Type

HY-D2413

BODIPY FL VH032

BODIPY FL PEG4-VH032

Fluorescent Dyes/Probes

BODIPY FL VH032 is a high-affinity VHL fluorescent probe with aK_d value of 3.01 nM. BODIPY FL VH032 consists of von Hippel-Lindau (VHL) ligand VH032 (HY-120217) and BODIPY FL (HY-43520). BODIPY FL VH032 can be used for time-resolved fluorescence resonance energy transfer (TR-FRET) detection for high-throughput identification and characterization of VHL ligands with maximum excitation emission wavelength: 504/520 nm .

Cat. No.	Compare	Product Name	Species	Source

HY-P76124

	VHL Protein, Human (His) von Hippel-Lindau disease tumor suppressor; Protein G7; pVHL; VHL	Human	E. coli
	VHL protein is an important component of the von Hippel-Lindau ubiquitination complex and plays a key role in ubiquitination and proteasomal degradation. As a target recruitment subunit in the E3 ubiquitin ligase complex, VHL specifically recruits hydroxylated hypoxia-inducible factor (HIF) under normoxic conditions and regulates cellular responses to oxygen levels. VHL Protein, Human (His) is the recombinant human-derived VHL protein, expressed by E. coli , with N-6*His labeled tag. The total length of VHL Protein, Human (His) is 213 a.a., with molecular weight of ~34 kDa.

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HY-133020

ARD-266		PROTAC Synthesis
ARD-266 is a highly potent and **von Hippel-Lindau 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 . ARD-266 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-163167

VH 032 amide-alkylC5-azide		Azide
VH 032 amide-alkylC5-amine is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand .

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