1,1,1-trifluoroethyl-peg2-propargyl

1,1,1-Trifluoroethyl-PEG2-propargyl is a PEG-based PROTAC linker that can be used to synthesise PROTAC molecules. 1,1,1-Trifluoroethyl-PEG2-propargyl contains an alkyne group that can undergo a click chemistry reaction with molecules containing an azide group using CuAAc.

dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, binding to MCL1 with a KD of 30 nM and activating the apoptosis mechanism by degrading MCL1.

Fmoc-PEA (Example 1-2) is utilized as a cleavable linker for antibody-drug conjugates (ADC).

1,2-Bis(2-iodoethoxy)ethane is a PEG-based PROTAC linker used in the synthesis of MT802 and SJF620, which are potent PROTAC BTK degraders with DC50s of 1 nM and 7.9 nM, respectively [1].

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

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.

m-PEG12-amine is a PEG-based PROTAC linker and a non-cleavable 12-unit PEG ADC linker used in the synthesis of PROTACs [1] and antibody-drug conjugates (ADCs) [2].

NH2-PEG6-Boc is a PEG-based PROTAC linker used in PROTAC synthesis[1] and a non-cleavable 6-unit PEG ADC linker for antibody-drug conjugates (ADCs) synthesis[2].

Desmorpholinyl Navitoclax-NH-Me (Desmorpholinyl ABT-263-NH-Me) is a Bcl-xL inhibitor, which can be employed alongside a CRBN ligand to synthesize XZ739, a PROTAC BCL-XL degrader [1] [2].

Thalidomide-NH-C2-PEG3-OH (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethyl]amino]-) is an E3 ligase ligand-linker conjugate.

PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).

PROTAC CDK2 9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

PROTAC EED degrader-1, a PROTAC targeting EED (pKD = 9.02), is an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.17.

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound used in the synthesis of ARV-771. ARV-771 is a BET PROTAC degrader that relies on von Hippel-Landau (VHL) E3 ligase and exhibits potent degradation of BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound acts as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, facilitating the recruitment of von Hippel-Lindau (VHL) protein.

MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein) and, together with a VHL ligand for the E3 ubiquitin ligase, has been used to design EED-Targeted PROTACs, specifically EED degrader-1 and PROTAC EED degrader-2 [1].

SLF-amido-C2-COOH (ZZY01-083) is an FKBP ligand with potential antimicrobial activity for the synthesis of PROTAC.

Boc-NH-PEG4-CH2CH2COOH is a PEG-based PROTAC linker used in the synthesis of PROTAC[1] and as a cleavable ADC linker for antibody-drug conjugates (ADC)[2].

2-Amino-1,3-bis(carboxylethoxy)propane is a polyethylene glycol (PEG)-based linker utilized for PROTAC synthesis[1].

2-(Azido-PEG2-amido)-13-propandiol is a Polyethylene glycol (PEG)-based PROTAC linker used for synthesizing PROTACs[1].

2-(Biotin-amido)-13-bis(carboxylethoxy)propane is a polyethylene glycol (PEG)-based PROteolysis TArgeting Chimera (PROTAC) linker used in the synthesis of PROTACs[1].