linker

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

Br-C10-methyl ester, a PROTAC linker characterized by its alkyl ether composition, plays a crucial role in the synthesis of a series of PROTACs (MS432). This compound incorporates a dual-ligand system connected via a linker; notably, one ligand interacts with the VHL portion.

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

NH2-C4-NH-Boc (compound 15) is a PROTAC linker of the Alkyl ether class, suitable for synthesizing various PROTAC molecules.

NH2-C6-NH-Boc is a PROTAC linker used in the synthesis of the Mcl-1 inhibitor [based on PROTAC].

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

Azido-PEG10-alcohol, a PEG-based PROTAC linker, is utilized in PROTAC synthesis [1].

Hydroxy-PEG4-(CH2)2-Boc is an uncleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs) and can also be employed in the synthesis of PROTAC.

Mal-PEG1-NHS ester is a cleavable, PEG-based linker utilized in the synthesis of antibody-drug conjugates (ADCs) and PROTACs, serving as both an ADC linker and a PROTAC linker. [Mal-PEG1-NHS ester]

Azido-PEG11-alcohol, a PEG-based PROTAC linker, is utilized in PROTAC synthesis.

Boc-NH-C4-acid is a PROTAC linker of the Alkyl ether class, utilized in the synthesis of PROTAC1 for the degradation of EED, EZH2, and SUZ12 in [PRC2].

m-PEG12-OH (Dodecaethylene Glycol Monomethyl Ether) is a PEG-based PROTAC linker. m-PEG12-OH can be used in the synthesis of PROTACs. m-PEG12-OH is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

tert-Butyl 11-aminoundecanoate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

Vipivotide tetraxetan Linker (PSMA-617 Linker) is a noncleavable peptide linker utilized in the synthesis of Vipivotide tetraxetan (PSMA-617), a ligand instrumental in producing 177Lu-PSMA-617. This radioactive molecule is applied in the treatment of prostate cancer[1].

Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) is a drug-linker conjugate for antibody-drug conjugates (ADCs), combining the ADC linker (Acetylene-linker-Val-Cit-PABC) with the potent tubulin inhibitor MMAE.

AhR Ligand-Linker Conjugates 1, also known as E3 Ligase Ligand-Linker Conjugates 57, is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a SNIPER linker. It is specifically designed to be used in the development of SNIPER[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].

CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1 2 ~20 hours)[1][2].

cIAP1 Ligand-Linker Conjugates 11 Hydrochloride is a chemical compound comprising an IAP ligand that targets the E3 ubiquitin ligase and a PROTAC linker, mainly used in the development of SNIPERs for targeted protein degradation[1].

cIAP1 Ligand-Linker Conjugates 11 is a chemical compound that combines an IAP ligand specifically designed for the E3 ubiquitin ligase with a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 11, is useful in the development of SNIPERs[1], allowing for the targeted degradation of proteins.

cIAP1 Ligand-Linker Conjugates 15 hydrochloride is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker, useful in the development of SNIPERs [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].

cIAP1 Ligand-Linker Conjugates 6 hydrochloride combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker, and is utilized for designing SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 14 consist of an IAP ligand that targets the E3 ubiquitin ligase and a PROTAC linker. These conjugates, known as cIAP1 Ligand-Linker Conjugates 14, are used in the development of SNIPERs[1].