vhl

Azido-PEG2-VHL is a multikinase degrader utilized in PROTACs (PROteolysis TArgeting Chimeras) synthesis [1].

VHL Ligand-Linker Conjugates 17 are chemical compounds that consist of a VHL ligand specialized for the E3 ubiquitin ligase, as well as a PROTAC linker. These conjugates are utilized in the synthesis of various PROTACs, including the notable ARD-266. ARD-266 is an exceptionally effective androgen receptor (AR) PROTAC degrader[1].

Potent and selective cereblon degrader (DC50 = 1.5 nM). Induces complete degradation of cereblon in MM1S cells. Comprises a cereblon E3 ligase ligand joined by a linker to a ligand for the E3 ligase VHL. Cell-permeable. Steinebach et al (2019) PROTAC-mediated crosstalk between E3 ligases. Chem.Commun.(Camb) 55 1821 PMID:30672516

VHL Ligand 8, a VHL ligand essential for synthesizing ARD-266, acts as a highly potent VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. It efficiently facilitates the degradation of AR protein in AR-positive prostate cancer cell lines LNCaP, VCaP, and 22Rv1, exhibiting DC50 values ranging from 0.2-1 nM [1].

VHL-IN-1 (compound 30), a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor with a dissociation constant (Kd) of 37 nM, potently stabilizes HIF-1α and enhances its transcriptional activity. It shows promise for applications as a HIF-1α stabilizer and for the degradation of proteolytically targeted chimeras (PROTACs) [1].

VHL Ligand-Linker Conjugates 15 is a chemical compound that combines a VHL ligand, which targets the E3 ubiquitin ligase, with a PROTAC linker. It is specifically designed for the creation of PROTACs[1].

(S,R,S)-AHPC TFA (VHL ligand 1 TFA) (VH032-NH2 TFA) is a VH032-based ligand designed for von Hippel-Lindau (VHL) protein recruitment. This compound can be linked to protein ligands (e.g., BCR-ABL1) using a linker to create PROTACs (e.g., GMB-475), which effectively induce the degradation of BCR-ABL1, demonstrated by an IC50 of 1.11 μM in Ba/F3 cells.

(S,R,S)-AHPC-C4-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 28) is a synthesized E3 ligase ligand-linker conjugate incorporating the (S,R,S)-AHPC based VHL ligand and a linker.

(S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthetic E3 ligase ligand-linker conjugate developed for use in PROTAC technology. It consists of the (S,R,S)-AHPC based VHL ligand and a 5-unit PEG linker [1].

(S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that 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[1].

(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[1].

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is a chemical compound utilized in the synthesis of ARV-771, an exceptionally potent BET protein degrader. This compound selectively degrades BET protein in cells resistant to castration, exhibiting a remarkable DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, (S,R,S)-AHPC-Me hydrochloride serves as the VHL ligand derived from (S,R,S)-AHPC for the recruitment of von Hippel-Lindau (VHL) protein.

(S, R, S)-AHPC-PEG4-NH2 hydrochloride is a chemically synthesized conjugate consisting of an E3 ligase ligand-linker, incorporating the VHL ligand based on (S, R, S)-AHPC, and a 4-unit PEG linker, which are specifically designed for use in PROTAC technology.

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound utilized in the synthesis of ARV-771. ARV-771, a BET PROTAC degrader relying on von Hippel-Landau (VHL) E3 ligase, demonstrates potent degradation of BET protein in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound serves as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, that facilitates the recruitment of von Hippel-Lindau (VHL) protein.

(S,R,S)-AHPC-PEG2-C4-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-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

(S,R,S)-AHPC-Me is a VHL ligand based on (S,R,S)-AHPC that can be used to recruit von Hippel-Lindau (VHL) proteins. It efficiently degrades BET proteins in desmoplasia-resistant prostate cancer cells with a DC50 < 1 nM, and it can be used to synthesize ARV-771.

(S,R,S)-AHPC-C6-PEG3-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

VH032-cyclopropane-F is a VHL ligand based on VH032. It is able to utilize linkers to ligands of target proteins to yield PROTAC molecules such as PROTAC 1. PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.

VH032 thiol (VHL ligand 6) is a VHL ligand that interacts with pan-BET inhibitor JQ1 through a linker to create a PROTAC[1] compound.

(S, R, S)-AHPC-PEG3-N3 (VHL Ligand-Linker Conjugates 8) is a synthesized E3 ligase ligand-linker conjugate. (S, R, S)-AHPC-PEG3-N3 incorporates the (S, R, S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.

(S,R,S)-AHPC-propargyl is a VHL ligand which is used in click reaction for PROTACs.

(S,R,S)-AHPC-PEG3-NH2 is a synthetic conjugate of an E3 ligase ligand-linker, incorporating the (S,R,S)-AHPC VHL ligand and a 3-unit PEG linker, which are utilized in PROTAC technology.

(S,R,S)-AHPC-PEG2-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 6) is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-PEG2-NH2 hydrochloride incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTAC.

(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 is potential useful for the targeted degradation of the androgen receptor.

(S,R,S)-AHPC-PEG1-N3 (E3 ligase Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-PEG1-N3 incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.

(S,R,S)-AHPC-PEG4-N3 (VHL Ligand-Linker Conjugates 5) is a synthesized conjugate that functions as a ligand-linker in E3 ligase-based systems. It is composed of the (S,R,S)-AHPC VHL ligand and a 4-unit PEG linker, both commonly employed in PROTAC technology.

(S,R,S)-AHPC-PEG1-OTs is a chemically synthesized conjugate, functioning as an ligase ligand-linker for E3 ligase. It incorporates the VHL ligand derived from (S,R,S)-AHPC and a 1-unit PEG linker. This synthesized compound is commonly employed in PROTAC technology.

(S,R,S)-AHPC-PEG2-NH2 (VHL Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-PEG2-NH2 incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.

(S,R,S)-AHPC-PEG4-NH2 (VHL Ligand-Linker Conjugates 4) is a synthetic E3 ligase ligand-linker conjugate comprising a VHL ligand based on (S,R,S)-AHPC and a 4-unit PEG linker.

(S,R,S)-AHPC-PEG2-N3 (VHL Ligand-Linker Conjugates 6) is a synthesized E3 ligase ligand-linker conjugate containing a (S,R,S)-AHPC based VHL ligand and 2 unit PEG linker.

(S,R,S)-AHPC hydrochloride (Protein degrader 1 hydrochloride) is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).

VH032-thiol-C6-NH2, also known as VHL Ligand-Linker Conjugates 14, is a synthesized compound that functions as an E3 ligase ligand-linker conjugate. This compound combines the VH032 based VHL ligand with a linker commonly utilized in PROTAC technology.

(S,R,S)-AHPC-PEG3-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 5) is an E3 ligase ligand-linker conjugate incorporating the (S,R,S)-AHPC-based VHL ligand and 3-unit PEG linker.

(S,R,S)-AHPC is a VHL ligand that used in the recruitment of the VHL protein.

cis VH 032, amine dihydrochloride ((S,S,S)-AHPC) is a negative control for the functionalized VHL ligand VH 032, amine .

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate, comprising the (S,R,S)-AHPC-based VHL ligand and a linker, designed for BET-targeted PROTAC applications.

(S,R,S)-AHPC-Me-C10-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating a VHL ligand and a linker.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

VH032 commonly used as a precursor to a PROTAC that hijacks VHL as the E3 ubiquitin ligase component.VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs, which can recruit von Hippel-Lindau (VHL) proteins as a ligand of VHL.

MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827(exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively). However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 μM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.

C004019 is a small molecule PROTAC capable of targeting tau for selective protein degradation from the cell, while recruiting tau and E3 ligase (Vhl) for selective enhancement of tau ubiquitination and proteollyzation. C004019 is a candidate for AD and related tau protein diseases.

Selective peptide-based β-catenin Degrader. Comprises a β-catenin-targeted stapled peptide, xStAx, linked to a VHL-binding peptide. Reduces β-catenin levels in HEK293T cells and colorectal cancer cell lines. Selectively degrades β-catenin over other Wnt signaling pathway components. Inhibits tumor growth in APCmin/+ mice, with constitutively active Wnt signaling, and reduces survival of patient-derived colorectal cancer cell organoids.

Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC.

VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.

HIF-1 alpha (556-574) is a hypoxia-inducible factor-1 19-mer fragment. HIF-1 functions as master regulator of response to oxygen homeostasis. Hypoxia-induced gene expression is initiated when HIF-1subunit is stabilized in response to a lack of oxygen. Thi

Functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development; incorporates an E3 ligase ligand plus a PEG linker ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. This product has been recently renamed. The previous name for this product was VH 032 - linker 4 PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus alkylC4 linker with terminal carboxylic acid ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. This product has been recently renamed. The previous name for this product was VH 032 - linker 5 PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

(S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-linker 12) is a synthesized E3 ligase ligand-linker conjugate incorporating the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker[1].

FAK ligand-Linker Conjugate 1 is a chemical compound designed to facilitate PROTAC-mediated protein degradation. This compound consists of a ligand specifically targeting FAK and a PROTAC linker module, which acts as a recruitment agent for E3 ligases including VHL, CRBN, MDM2, and IAP[1].