brd-4 ligand-linker conjugate 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.

N-Boc-4-pentyne-1-amine is an alkyl chain-based PROTAC linker compound used in the synthesis of PROTAC MG-277 [1].

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.

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.

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].

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].

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].

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].

MAC glucuronide linker-1 is a noncleavable ADC linker used in antibody-drug conjugations (ADCs).

cIAP1 Ligand-Linker Conjugates 9 feature an IAP ligand specifically targeting the E3 ubiquitin ligase, along with a PROTAC linker. It is valuable tools for developing SNIPERs[1].

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].

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].

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].

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].

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.

N-(m-PEG4)-N'-(4-Hydroxycyclohexyl-1-amido-PEG4)-Cy5 is a polyethylene glycol (PEG)-based linker compound primarily used in the synthesis of proteolysis-targeting chimeras (PROTACs)[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].

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

cIAP1 Ligand-Linker Conjugates 8 comprises an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is specifically utilized for the purpose of SNIPER design[1].

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

cIAP1 Ligand-Linker Conjugates 12 is a chemical compound that combines an IAP ligand, which targets the E3 ubiquitin ligase, with a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 12, is valuable for creating SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 2 Hydrochloride is a chemical compound that combines an IAP ligand, targeting the E3 ubiquitin ligase, with a PROTAC linker and is utilized in the creation of SNIPERs[1].

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

cIAP1 Ligand-Linker Conjugates 13, containing an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker, are utilized in the development of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 10 comprise of an IAP ligand and a PROTAC linker, which facilitates the design of SNIPERs. These conjugates incorporate an IAP ligand that interacts with the E3 ubiquitin ligase, and a PROTAC linker. SNIPERs can be developed using cIAP1 Ligand-Linker Conjugates 10.

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].

Tetraethyl butane- 1, 4- diylbis(phosphoramid ate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

cIAP1 Ligand-Linker Conjugates 15 consists of an IAP ligand that targets the E3 ubiquitin ligase, along with a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 15, is suitable for the development of SNIPERs[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].

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

SNIPER(BRD)-1 is a chemical compound composed of a derivative of the IAP antagonist LCL-161 and the BET inhibitor (+)-JQ-1, linked together. It promotes the degradation of BRD4 through the ubiquitin-proteasome pathway and effectively degrades cIAP1, cIAP2, and XIAP with IC50 values of 6.8 nM, 17 nM, and 49nM, respectively[1].

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

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.

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].

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.

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].