vhl-in-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].

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

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.

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.

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

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].

VH032-PEG3-acetylene is a synthesized conjugate compound comprising a VH032-based VHL ligand and a linker, intended for use in PROTAC technology as an E3 ligase ligand-linker conjugate[1].

BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7 9 inhibitor), interacts with a VHL ligand via a linker to form the PROTAC VZ185 (targeting BRD7 9 with DC50 values of 4.5 and 1.8 nM, respectively)[1].

BRD7-IN-1, a modified derivative of BI7273 (BRD7 9 inhibitor), forms PROTAC VZ185 via linkage to a VHL ligand, demonstrating potent activity against BRD7 9 with DC50 values of 4.5 and 1.8 nM, respectively [1].

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

(S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC, comprising the (S,R,S)-AHPC based VHL ligand and a 2-unit PEG linker, that induces the degradation of GFP-HaloTag7 in cell-based assays[1].

(S,R,S)-AHPC-C6-PEG3-C4-Cl is a small molecule HaloPROTAC incorporating the (S,R,S)-AHPC based VHL ligand and a 3-unit PEG linker, 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 incorporating the (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker, capable of inducing degradation of GFP-HaloTag7 in cell-based assays [1].

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

(S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC comprising the (S,R,S)-AHPC based VHL ligand and a 6-unit PEG linker, capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

EED226-COOH, derived from EED226, serves as a ligand targeting the EED protein for PROTAC applications. It attaches to a VHL ligand through a linker, culminating in the formation of UNC6852, which specifically degrades PRC2[1].

VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule that includes the VH032-based VHL ligand and a 5-unit PEG linker, capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells [1].

K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in synthesizing PROTAC K-Ras Degrader-1, a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound comprising a ligand for the K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential for synthesizing PROTAC K-Ras Degrader-1, a potent degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

K-Ras ligand-Linker Conjugate 4 is a chemical compound combining a K-Ras recruiting ligand with a PROTAC linker, responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. It has the potential to be used in synthesizing PROTAC K-Ras Degrader-1, which shows a degradation efficacy of ≥70% in SW1573 cells[1].

K-Ras ligand-Linker Conjugate 5 is a chemical compound combining a K-Ras recruiting ligand with a PROTAC linker for E3 ligases, such as VHL, CRBN, MDM2, and IAP. This conjugate is crucial for synthesizing PROTAC K-Ras Degrader-1, displaying a degradation efficacy of ≥70% in SW1573 cells [1].

(S,R,S)-AHPC-amido-C5-acid is a chemical compound containing a VHL ligand for E3 ubiquitin ligase and a PROTAC linker, utilized in designing XY028-133[1].