2-phthalimidehydroxy-acetic acid

2-Phthalimidehydroxy-acetic acid is an alkyl chain-based PROTAC linker utilized in PROTAC synthesis.

AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells. [2]

CDK9-IN-10 is a potent inhibitor of CDK9 and serves as the ligand for the PROTAC CDK9 degrader-2.

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).

Pomalidomide-PEG1-CO2H is a synthetic E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a 2-unit PEG linker.

dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) is a glue degrader. dCeMM3 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, result in inducing ubiquitination and degradation of cyclin K.

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].

5-Ethynyl-2'-deoxyuridine (EdU) is a nucleoside analog of thymidine used to monitor de novo DNA synthesis through click chemistry and serves as an alkyl chain-based PROTAC linker for synthesizing PROTACs.

m-PEG-NH2 (MW 1000) is a PEG-based PROTAC linker. m-PEG-amine (MW 1000) can be used to synthesize PROTAC.

m-PEG2-Br is a PEG-based PROTAC linker used in the synthesis of PROTACs.

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].

NH2-C2-NH-Boc (PROTAC Linker 22), an alkyl chain-based PROTAC linker, can be used in the synthesis of PROTACs.

NH2-C5-NH-Boc (PROTAC Linker 23) is an alkyl chain-based PROTAC linker used in the synthesis of PROTACs.

(+)-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.

5-Aminothalidomide is a E3 ligase ligand used in PROTAC technology.

Thalidomide-4-OH (E3 ligase Ligand 2) (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used to recruit of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) is a linker to form PROTACs

Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) is the Thalidomide-based cereblon ligand that used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTAC.

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.

Nrf2 degrader 30 is a small molecule PROTAC that inhibits the degradation of Nrf2, thereby enhancing its activity. Nrf2 is a key transcription factor that regulates cellular antioxidant responses and various protective mechanisms. The activity of Nrf2 is primarily regulated by its interaction with Keap1, which serves as an E3 ubiquitin ligase complex adapter to promote Nrf2 ubiquitination and proteasomal degradation。

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)

N-Boc-cis-4-hydroxy-L-proline methyl ester serves as a non-cleavable linker in antibody-drug conjugate (ADC) synthesis and functions as an alkyl chain-based PROTAC linker for PROTAC construction [2].