vhl ligand 1

(S,R,S)-AHPC (VH032-NH2) is a VH032-based ligand for recruiting the von Hippel-Lindau (VHL) protein, potentially useful for the targeted degradation of the androgen receptor.

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

(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.

SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

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

(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.

PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

SMARCA-BD ligand 1 for Protac dihydrochloride binds to the BAF ATPase subunit SMARCA2 and is used for degrading SMARCA2 based on PROTAC.

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].

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].

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].

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].

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

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].

(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-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].

BRD4 Ligand-Linker Conjugate 1 is a compound consisting of a ligand and a linker, specifically designed to bind to the target protein BRD4. This conjugate serves as a valuable tool for synthesizing PROTACs, molecules utilized for targeted protein degradation.

TSPO Ligand-Linker Conjugates 1, comprising a translocator protein (TSPO) ligand and a linker, is instrumental in synthesizing mitochondria-targeting autophagy-targeting chimera (AUTAC). This compound binds TSPO on the outer mitochondrial membrane (OMM), facilitating the degradation of malfunctioning mitochondria and proteins through mitophagy, thereby enhancing mitochondrial function. It holds potential applications in research related to mitochondrial dysfunction, encompassing neurodegenerative diseases, cancer, and diabetes [1].

CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].

CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. This thiadiazole-dioxide ligand suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.

TSPO ligand-1 has affinity for peripheral and central benzodiazepine receptors.TSPO ligand-1 is an AUTAC4-binding protein in the transmembrane domain of the outer mitochondrial membrane, which induces mitochondrial autophagy and promotes intracellular mitochondrial regeneration.TSPO ligand-1 is involved in intracellular cholesterol transport, and can be used as a biomarker for brain injury and neurodegeneration. TSPO ligand-1 is involved in intracellular cholesterol transport and can be used as a biomarker for brain damage and neurodegeneration.

PROTAC Bcl-xL ligand-1 serves as a ligand targeting Bcl-xL, essential in synthesizing PROTACs [1].

PROTAC PTK6 ligand-1 serves as an intermediate in the synthesis of BTK kinase inhibitors [1] and is utilized in the preparation of ARD-61 [2].

SMARCA-BD Ligand 1 Hydrochloride, used in PROTAC technology, targets and binds to the BAF ATPase subunits SMARCA2, facilitating its degradation.

cIAP1 Ligand-Linker Conjugates 1 is composed of an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 1, is particularly useful in the development of SNIPERs[1].

AhR Ligand-Linker Conjugates 1, also known as E3 Ligase Ligand-Linker Conjugates 57, is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a SNIPER linker. It is specifically designed to be used in the development of SNIPER[1].

GID4 Ligand 1 is a cell-permeable, highly selective GID4 binder with an IC50 value of 5.4 μM and a Kd value of 5.6 μM. GID4 Ligand 1 is capable of binding GID4 in cells with an EC50 value of 558 nM. GID4 Ligand 1 is capable of being used in the synthesis of PROTACs.

ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1].

PROTAC BCR-ABL1 ligand 1 is the ligand of PROTAC .

cIAP1 ligand 1 (E3 ligase Ligand 12) is an apoptotic protein ligand based on the LCL161 derivative that recruits IAP ubiquitin ligases to degrade target proteins, and can be used in conjunction with androgen receptor ligands for the development of protein degradation agents that can be used in the study of prostate cancer.

PROTAC IRAK4 ligand-1 is a synthetic ligand targeting interleukin-1 receptor-associated kinase 4 (IRAK4).

PROTAC CDK9 ligand-1, a CDK9 ligand, is used in the synthesis of PROTACs.

PROTAC PARP EGFR ligand 1 is a potent compound used in developing dual PARP-EGFR degraders via Proteolytic Targeting Chimera (PROTAC) technology [1].

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

(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-linker 10) is a synthesized E3 ligase ligand-linker conjugate, incorporating an (S,R,S)-AHPC-based VHL ligand and a linker[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.

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

(S,R,S)-AHPC-Me (E3 ligase Ligand 1A) (VHL ligand 2) is an (S,R,S)-AHPC-based VHL ligand used to recruit the von Hippel-Lindau (VHL) protein. It is utilized in the synthesis of ARV-771, a VHL E3 ligase-based BET PROTAC degrader that effectively degrades BET proteins in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.

MS9715 is a potent and selective NSD3-targeting PROTAC, designed by leveraging BI-9321, which targets the PWWP1 domain of NSD3, in conjunction with an E3 ligase VHL ligand. This compound holds potential for research in NSD3-dependent cancer treatments [1].

Functionalized von-Hippel-Lindau protein ligand (VHL) 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 1 PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells. Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use. Negative control dTAGV-1-NEG (Cat. No. 6915) also available. FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire. Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

(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].

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].

PROTAC CRBN Degrader-1 is a chemical compound consisting of a cereblon (CRBN) ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group. It functions as a cereblon (CRBN) degrader[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.

K-Ras ligand-Linker Conjugate 6 is a chemical compound that combines a ligand for the K-Ras recruiting moiety and a PROTAC linker. It can recruit E3 ligases, including VHL, CRBN, MDM2, and IAP. K-Ras ligand-Linker Conjugate 6 is particularly useful in synthesizing PROTAC K-Ras Degrader-1, which achieves ≥70% degradation efficacy in SW1573 cells[1].

(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].