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.
N-Fmoc-8-aminooctanoic acid can be used as a PROTAC linker in the synthesis of PROTACs. N-Fmoc-8-aminooctanoic acid is an alkane chian with terminal Fmoc-protected amine and carboxylic acid groups. The Fmoc group can be deprotected under basic condition to obtain the free amine which can be used for further conjugations. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond.
(2-Pyridyldithio)-PEG4-propargyl is a polyethylene glycol (PEG)-based linker specifically designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs) [1].
N-(Propargyl-PEG4-carbonyl)-N-bis(PEG1-methyl ester) is a polyethylene glycol (PEG) based linker, employed in the synthesis of proteolysis-targeting chimeras (PROTACs)[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.
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].
Fmoc-N-bis-PEG3-NH-Boc is a cleavable ADC linker compound consisting of three PEG units, employed in the synthesis of antibody-drug conjugates (ADCs)[1].
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].
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].
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.
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).
Thalidomide-O-amido-PEG1-(C1-PEG)2-C2-NH2 is a synthetic conjugate compound that combines a Thalidomide-based cereblon ligand and a linker, which is commonly utilized in PROTAC technology. This compound acts as a connector between the target protein and the E3 ligase, facilitating targeted protein degradation.
DSPE-PEG-2-Aminoethyl-alpha-mannopyranoside (MW 2000) is a polyethylene glycol (PEG) derived linker. This specific linker is utilized in the synthesis of PROTACs, or proteolysis targeting chimeras [1].
N-Methyl-N'-methyl-O-(m-PEG4)-O'-(azide-PEG4)-Cy3 is a polyethylene glycol (PEG) based linker commonly employed in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.
N-Methyl-N'-(azido-PEG2-C5)-Cy5 is a polyethylene glycol (PEG)-based linker that incorporates an azide functionality. This linker is primarily utilized in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker. This compound is capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC K-Ras Degrader-1, which is a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].