Ligand for Target Protein for PROTAC

AKT ligand-2 is a selective ligand targeting the AKT protein. It can be utilized in the synthesis of PROTACs, specifically by linking with VHL ligand (S,R,S)-AHPC, to create compounds like PROTAC MS21. This reagent is instrumental in cellular research focused on targeted protein degradation and the modulation of AKT signaling pathways.

TRIB2 ligand-1 is a specific ligand for the TRIB2 protein, facilitating the development of PROTACs designed for targeted protein degradation. This compound plays a crucial role in the synthesis of PROTAC TRIB2 degrader-1, which can be employed in research focused on protein regulation and degradation pathways. Its application in such studies supports investigations into various cellular mechanisms and potential therapeutic targets.

SMARCA2/4-ligand-2 is a selective ligand designed for the targeted degradation of SMARCA2 and SMARCA4 proteins via the PROTAC (proteolysis-targeting chimeras) approach. This compound facilitates the ubiquitination and subsequent proteasomal degradation of these essential chromatin remodeling proteins, making it a valuable tool in studies focused on cancer biology and epigenetic regulation. Researchers can utilize SMARCA2/4-ligand-2 to investigate the role of SMARCA2/4 in various cellular processes and to explore therapeutic strategies for diseases linked to their dysregulation.

Nrf2 activator-22 is a ligand specifically targeting the Nrf2 protein, playing a crucial role in the development of PROTAC-based therapeutics. This compound facilitates the synthesis of PROTAC K-Ras Degrader-7, highlighting its potential in targeted protein degradation research. Nrf2 activator-22 is valuable for studies aimed at manipulating oxidative stress responses and related signaling pathways.

Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor.

Desmethyl-QCA276, the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM.

SMARCA-BD ligand 1 for Protac is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.

PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain.

Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .

GNF5-amido-Me, the GNF5 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.

Imatinib carbaldehyde (CGP-57148B carbaldehyde), the Imatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.

Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.

Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.

ATRA-hydroxyimino (CRABP-II ligand 1), the Retinoic acid (ATRA)-based moiety, binds to cIAP1 ligand (Bestatin) via a linker to form SNIPER to degrade CRABP-II in IMR-32 cells.

SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM.

SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.

PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors.

N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825), the Dasatinib-based moiety, binds to IAP ligand via a linker to form SNIPER to degrade ABL.

PROTAC BRD9-binding moiety 1 is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.

BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC.

AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.

DUPA, belongs to a class of glutamate ureas, is used as the targeting moiety in drug conjugate to selectively deliver cytotoxic drugs to prostate cancer cells.

(Rac)-BMS-1 is a racemic compound that serves as a ligand for target proteins in the development of proteolysis-targeting chimeras (PROTACs). It plays a crucial role in synthesizing D5B PROTAC, facilitating targeted protein degradation. This compound is valuable for researchers investigating protein regulation and therapeutic applications in cancer and other diseases.

SHP2-IN-43 is a potent inhibitor of SHP2, demonstrating an IC50 of 98.7 nM. This compound serves as a valuable ligand for targeted protein degradation (PROTAC) applications, facilitating the synthesis of SHP2-D26. Researchers can utilize SHP2-IN-43 to explore the therapeutic potential of modulating SHP2 activity in various biological contexts.

GNF-8625 is a potent TRK inhibitor that functions by targeting TRK receptor tyrosine kinases, specifically TRKA, TRKB, and TRKC, with IC50 values of 0.8 nM, 22 nM, and 5.4 nM, respectively. This compound can be utilized in conjunction with Thalidomide to create a PROTAC degrader, enabling targeted protein degradation. GNF-8625 is valuable in research applications investigating TRK-mediated pathways and offers potential in therapeutic strategies for cancers involving aberrant TRK signaling.

BTK ligand 12 is a potent ligand for Bruton's tyrosine kinase (BTK), functioning as a valuable component in the development of PROTACs targeting this protein. It exhibits strong binding affinity, facilitating the effective ubiquitination and degradation of BTK in various cellular contexts. This compound is essential for researchers investigating targeted protein degradation and the modulation of signaling pathways associated with BTK in therapeutic applications.

BTK/IKZF1/3 ligand 1 is a PROTAC ligand targeting Bruton's tyrosine kinase (BTK) and the Ikaros family zinc finger proteins (IKZF1/3). This compound can be conjugated with E3 ligase ligands and linkers to produce PROTAC BTK/IKZF1/3 Degrader-1, facilitating targeted protein degradation. It is valuable for cancer research, supporting investigations into therapeutic strategies aimed at modulating BTK and IKZF1/3 activity in malignant cells.

ALK protein ligand-1 is a specific ligand for anaplastic lymphoma kinase (ALK) that plays a crucial role in targeted protein degradation using PROTAC technology. This compound exhibits potent inhibitory effects on ALK, making it a valuable tool for studying ALK-related signaling pathways and their implications in cancer biology. ALK protein ligand-1 is essential for the synthesis of AP-1, facilitating the exploration of novel therapeutic approaches in oncology research.