ligand for e3 ligase

E3 ligase Ligand 23 is a cereblon binding agent that degrades Ikaros or Aiolos via the ubiquitin proteasome.

E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. The E3 ligase Ligand 8 can be linked to protein ligands through linkers to form PROTACs, which are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.

TSPO ligand-3, functioning as an AUTAC2 ligand, incorporates both a p-fluorobenzylguanine (FBnG) and a synthetic ligand of FKBP (SLF) moiety, leading to the substantial inhibition of FKBP12 in HeLa cells [1].

PROTAC IRAK4 Ligand-3 serves as a ligand for PROTAC IRAK4 Degrader-7 and is utilized in cancer research [1].

E3 ligase Ligand 13 is an E3 ubiquitin ligase ligand that can be employed to create PROTACs, which are connected to the ligand for the protein through a linker. PROTACs serve as inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].

cIAP1 Ligand-Linker Conjugates 3 are chemical compounds comprising an IAP ligand designed specifically for the E3 ubiquitin ligase and a PROTAC linker. These conjugates, denoted as cIAP1 Ligand-Linker Conjugates 3, find utility in the design of SNIPERs, short for Specific and Non-genetic IAP-dependent Protein Erasers [1].

E3 ligase Ligand 10 serves as a ligand for E3 ubiquitin ligase and can be conjugated to a protein ligand through a linker, resulting in the formation of PROTACs. These PROTACs act as inducers of ubiquitination-mediated degradation, specifically targeting cancer-promoting proteins[1].

E3 ligase Ligand 9 is a compound that serves as a ligand for E3 ubiquitin ligase. It can be linked to the protein ligand through a linker, forming PROTACs or SNIPERs. These PROTACs are known to induce the degradation of cancer-promoting proteins through ubiquitination-mediated mechanisms[1].

E3 ligase Ligand 14 is a ligand that binds to E3 ubiquitin ligase and can be conjugated to a protein ligand via a linker to create PROTACs. These PROTACs are capable of promoting ubiquitination-mediated degradation of cancer-promoting proteins[1].

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

E3 ligase Ligand 18 is a ligand that binds to E3 ubiquitin ligase, and it can be chemically attached to a protein ligand through a linker to create PROTACs. The resulting PROTACs function as inducers of ubiquitination-mediated degradation, targeting cancer-promoting proteins[1].

Lenalidomide-Br is an analog of the cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, which is used in the recruitment of CRBN proteins. It is able to utilize linkers to attach to protein ligands to form PROTACs such as the PROTAC STAT3 degrader SD-36.

Thalidomide-O-amido-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate, integrating a Thalidomide-based cereblon ligand with a linker, suitable for PROTAC synthesis.

(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-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.

Lenalidomide (CC-5013) is a potent inhibitor of TNF-α that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines.

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1].

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].

Ipatasertib-NH2 dihydrochloride is a ligand for the target protein AKT in PROTAC INY-03-041. INY-03-041 consists of Ipatasertib-NH2, a ten-hydrocarbon linker, and the CRBN ligand Lenalidomide, which acts as an E3 ubiquitin ligase.

Thalidomide-4-OH (E3 ligase Ligand 2) (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used to recruit of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) is a linker to form PROTACs

cIAP1 Ligand-Linker Conjugates 5 is a chemical compound consisting of an IAP ligand that targets the E3 ubiquitin ligase, and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 5, is specifically designed for the development of SNIPERs[1].

Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker composed of PEGs. It is utilized in the synthesis of various PROTACs, which involve the connection of two distinct ligands through a linker. One ligand is specific for an E3 ubiquitin ligase, while the other ligand is designed for targeting the specific protein of interest. Through leveraging the intracellular ubiquitin-proteasome system, PROTACs are capable of selectively degrading target proteins [1].

(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) serves as an E3 ligase ligand-linker conjugate, integrating a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is utilized in PROTAC EED degrader-1, a PROTAC that targets EED with a potency (pKD) of 9.02[1].

(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.

Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTACs.

Lenalidomide hemihydrate is a derivative of Thalidomide, an orally active immunomodulator that acts as a molecular gel. It is a ligand for the ubiquitin E3 ligase cereblon, which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase.

Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent featuring an azide group and serves as a crosslinker-E3 ligase ligand conjugate. This compound is utilized as a click-reactive protein degrader building block within PROTAC research and as a template for the synthesis of targeted protein degraders [1].

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.

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

(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].

Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1].

Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is an E3 ligase ligand-linker conjugate which is designed using Thalidomide-based cereblon ligand and a 3-unit PEG linker. This compound is synthesized specifically for utilization in PROTAC technology.

Thalidomide-O-amido-C3-PEG3-C1-NH2 is a synthesized conjugate compound that serves as an E3 ligase ligand-linker. It features a cereblon ligand based on Thalidomide and a 3-unit PEG linker. This compound is specifically designed for use in PROTAC technology.

Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate, combines a Thalidomide-based cereblon ligand with a two-unit PEG linker for use in PROTAC technology[1].

Lenalidomide-OH is an analog of Lenalidomide, a cereblon ligand for E3 ubiquitin ligase (CRBN), used for CRBN protein recruitment. It is able to attach to protein ligands using linkers to form PROTAC.

Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride incorporates an E3 ligase ligand and a linker. Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride can be used as an immunomodulator for the treatment of cancer.

Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC, binds to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 to degrade AKT[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.

Pomalidomide-amino-PEG3-NH2 is a compound obtained through synthesis, consisting of a conjugation between the E3 ligase ligand linker and Pomalidomide, a cereblon ligand. This compound is specifically designed for application in PROTAC technology, incorporating a linker that enables effective binding with the targeted proteins.

Tz-Thalidomide is a tetrazine-modified Thalidomide (E3 ligase ligand) with some affinity for BRD4.

Nutlin-C1-amido-PEG4-C2-N3 is a novel compound that functions as a ligand-linker conjugate for the E3 ligase. It is a synthesized molecule incorporating the MDM2 ligand derived from Nutlin 3, and a 4-unit PEG linker. This compound is specifically designed for utilization in PROTAC technology.

(S,R,S)-AHPC-amido-C5-acid is a chemical compound that contains a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. It can be utilized in the design of XY028-133[1].

(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized conjugate designed for E3 ligase ligand-linker applications, combining the VH032 VHL-based ligand with a linker for PROTAC development. VH-032 acts as a selective and potent VHL/HIF-1α interaction inhibitor, with a dissociation constant (Kd) of 185 nM, offering potential in anemia and ischemic diseases research[1].

Functionalized cereblon ligand for PROTAC research and development; incorporates an E3 ligase ligand plus an alkylC8 linker with terminal acid ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

SNIPER(ER)-87 is a chemical compound composed of a derivative of the inhibitor of apoptosis protein (IAP) ligand LCL161 conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen using a PEG linker. It effectively degrades the ERα protein with an IC50 value of 0.097 μM. Within cells, SNIPER(ER)-87 selectively recruits XIAP to ERα, and XIAP functions as the primary E3 ubiquitin ligase responsible for the degradation of ERα induced by SNIPER(ER)-87[1][2].

Functionalized von-Hippel-Lindau protein ligand (VHL) for research and development; incorporates an E3 ligase ligand plus alkylC3 linker with terminal carboxylic acid ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules.

(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.

DCAF1 Binder 1 selectively targets the CRL4 DCAF1 E3 ligase complex as a ligand, playing a role in targeted protein degradation (TPD) [1].

Thalidomide-Piperazine 5-fluoride hydrochloride, a derivative of the cereblon (CRBN) inhibitor Thalidomide, serves as a ligand for E3 ubiquitin ligase (Ligands for E3 Ligase), facilitating the synthesis of PROTACs [1].