PROTAC Linker-10

Boc-NH-PEG3 (PROTAC Linker 10) is a PEG derivative featuring a hydroxyl group and a Boc-protected amino group, used as a PROTAC linker.

MS 39 is a potent Proteolysis Targeting Chimera (PROTAC) designed to degrade the Epidermal Growth Factor Receptor (EGFR). The molecule is composed of three structural motifs: an EGFR target ligand (red part), a VHL E3 ligase ligand (S,R,S)-AHPC (blue part), and an undecanedioic acid linker (black part). By facilitating the formation of a ternary complex between EGFR and the VHL E3 ubiquitin ligase, MS 39 triggers the polyubiquitination and subsequent proteasomal degradation of the receptor. MS 39 effectively reduces EGFR protein levels and inhibits downstream oncogenic signaling in HCC-827 and H3255 cell lines, leading to significant suppression of H3255 cancer cell proliferation.

Tetraethylene glycol is a PEG-based PROTAC linker that can be oxidised as a substrate of polyethylene glycol dehydrogenase (Km = 10 mM).

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.

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

Amino-PEG10-acid is a PEG-based PROTAC linker utilized in PROTAC synthesis.

Fmoc-NH-PEG10-acid, a PEG-based PROTAC linker, is utilized in the synthesis of PROTACs.

Hydroxy-PEG10-acid (HO-PEG10-CH2CH2COOH) is a PEG-based PROTAC linker that can be used to synthesize PROTACs[1].

(10-BRomodecyl)phosphonic acid is an alkyl chain-derived PROTAC linker suitable for PROTAC synthesis [1].

The compound [10-(diethoxy-phosphoryl)-decyl]-phosphonic acid is a suitable alkyl chain-based PROTAC linker for the synthesis of PROTACs [1].

Diethyl 10-bromodecylphosphonate is an alkyl-based PROTAC linker utilized for the synthesis of PROTACs[1].

m-PEG10-alcohol, also known as Decaethylene glycol monomethyl ether, is a non-cleavable 10 unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1]. Additionally, m-PEG10-alcohol serves as a PEG-based PROTAC linker, enabling its application in the synthesis of PROTACs[1].

Propargyl-PEG1-acid, a PEG-based PROTAC linker, enables the synthesis of BTK-CRBN PROTACs, specifically Ibrutinib-based PROTAC 4 and PROTAC 5. At a concentration of 10 μM, PROTAC 5 facilitates the degradation of BTK and induces the degradation of CSK, LYN, and LAT2[1].

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate, comprising an (S,R,S)-AHPC-based VHL ligand and a linker, designed for BET-targeted PROTAC applications.

cIAP1 Ligand-Linker Conjugates 10 comprise of an IAP ligand and a PROTAC linker, which facilitates the design of SNIPERs. These conjugates incorporate an IAP ligand that interacts with the E3 ubiquitin ligase, and a PROTAC linker. SNIPERs can be developed using cIAP1 Ligand-Linker Conjugates 10.

Pomalidomide-PEG1-C2-N3, a conjugate of an E3 ligase ligand-linker, incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, commonly used in PROTAC technology. This compound enables the design of the selective CDK6 PROTAC degrader CP-10, which effectively induces CDK6 degradation with a DC50 value of 2.1 nM[1].

Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1].

Desmethyl-QCA276, the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM[1].

(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-linker 10) is a synthesized E3 ligase ligand-linker conjugate, incorporating an (S,R,S)-AHPC-based VHL ligand and a linker[1].

SJFδ is a 10-atom linker PROTAC that selectively degrades p38δ with a DC50 of 46.17 nM, without degrading p38α, p38β, or p38γ[1].

E3 Ligase Ligand-linker Conjugate 134 is a crucial intermediary in synthesizing the complete PROTAC molecule STING-IN-10. It consists of a conjugate of an E3 Ligase Ligand and a linker, which facilitates the assembly of the target molecule.

Acepromazine-1-Piperazinepropanamine (compound 10) is an E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugate) consisting of a cereblon ligand and a linker. This compound can target protein ligands to form the PROTAC molecule, TrimTAC1.

PROTAC BTK Degrader-10 (Example 1P) is a PROTAC compound that targets BTK for degradation. It is applicable in the research of chronic lymphocytic leukemia (CLL). [Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon].

PROTAC JNK1-targeted-1 (PA2) is a JNK1 PROTAC degrader with a DC50 of 10 nM. It effectively reduces fibronectin levels and is useful in lung fibrosis research. [Pink: JNK1 inhibitor; Black: linker; Blue: CRBN Ligand]