N3-PEG3-CH2CH2COOH, a PEG-based PROTAC linker, is utilized in the synthesis of BI-3663, BI-4216, and BI-0319. Additionally, Azido-PEG3-acid, a non-cleavable 3-unit PEG ADC linker, is employed in the synthesis of antibody-drug conjugates (ADCs).
dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, which binds to MCL1 with a KD of 30 nM. dmcl-2 activates the apoptosis mechanism by degrading MCL1.This compound is unstable in powder form and other related salt forms are recommended.
CBP p300 ligand 2 is a selective ligand that binds to the target protein for PROTAC of dCBP-1, a potent and selective heterobifunctional degrader of p300 CBP.
PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein. At a concentration of 30 nM, this compound exhibits a remarkable degradation capability, reducing the ERRα protein levels by >80%. Importantly, PROTAC ERRα Degrader-3 shows no activity against the ERRβ and ERRγ proteins.
(2-Pyridyldithio)-PEG4-propargyl is a polyethylene glycol (PEG)-based linker specifically designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs) [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].
S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate, an ADC linker, is a glutathione cleavable compound used for the attachment of monoclonal antibodies (mAb) in antibody-drug conjugates (ADCs). It specifically refers to the Alkyl-Chain composition of the linker portion of these molecules [1].
(2-Pyridyldithio)-PEG4 acid is a four-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. It serves as a crucial component in the conjugation of antibodies and drugs, enabling targeted drug delivery and enhanced therapeutic efficacy. This linker possesses a (2-pyridyldithio) group at one end, facilitating the attachment of the linker to the specific site on the antibody molecule. The PEG4 chain provides the necessary flexibility and biocompatibility for optimal drug release while maintaining stability throughout the circulation in the body. Ultimately, (2-Pyridyldithio)-PEG4 acid is instrumental in the development and advancement of ADCs, a promising approach in cancer therapy.
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader[1].
cIAP1 ligand 2, a derivative of LCL161, is an IAP ligand that can be connected to the ABL ligand for protein via a linker, resulting in the formation of SNIPER.
N-Succinimidyl 3-(Bromoacetamido)propionate is a PEG-based PROTAC linker employed in the synthesis of PROTACs and antibody-drug conjugates (ADCs) [1, 2]. It acts as a cleavable ADC linker, facilitating the conjugation of drugs to antibodies for targeted delivery [2].
2-((Azido-PEG8-carbamoyl)methoxy)acetic acid is a polyethylene glycol (PEG) derivative that serves as a linker for proteolysis targeting chimeras (PROTACs) synthesis [1].
DBCO-NHS ester 3 (Compound 12) is a cleavable linker utilized in the synthesis of antibody-drug conjugate (ADC). It is a derivative of Dibenzylcyclooctyne (DBCO) resulting from the activation of N-hydroxysuccinimide by the carboxylic acid moiety of both methyl-oxanorbornadiene (MeOND) and dibenzoazacyclooctyne (DIBAC)[1][2].
PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD) with an IC50 of 0.6 nM and exhibits anti-proliferative activity.
Thalidomide-NH-CBP p300 ligand 2 (P-007) is a PROTAC-based compound designed to degrade CBP and p300, acting as a functional antagonist (WO2020173440).