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.

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.

PROTAC BRD4 Degrader-10, also known as compound 8b, is a dual ligand-based PROTAC that combines ligands for von Hippel-Lindau and BRD4. To degrade the BRD4 protein in PC3 prostate cancer cells, PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies, with respective DC 50 values of 1.3 nM and 18 nM.

PROTAC BET Degrader-10 (WO2017007612A1, example 37) is a highly efficient and selective small molecule compound designed to degrade BET protein BRD4. PROTAC BET Degrader-10 functions by utilizing specific ligands that connect Cereblon and BRD4, with a DC 50 value of 49 nM.

PROTAC ER Degrader-10 is a potent PROTAC ER degrader, suitable for cancer research.

PROTACSMARCA2 4-degrader-10 (compound I-399) is an effective SMARCA2 degrader with a DC50 value of less than 100 nM. It holds potential for use in cancer research.

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.

(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.

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

AP-1, a miniaturized proteolysis-targeting chimera (PROTAC) incorporating an anaplastic lymphoma kinase (ALK) ligand connected to (±)-thalidomide via an ultrashort linker, effectively degrades ALK fusion proteins such as NPM-ALK in Karpas-299 cells and EML4-ALK and ALKF1174L in SN-N-SH and NCI H3122 cells, respectively. Concentrations ranging from 10 to 300 nM are sufficient for its action, which is hindered by the proteasome inhibitor MG-132. Demonstrating selectivity, AP-1 exhibits cytotoxicity towards ALK-dependent Karpas-299 cells with an IC50 value of 0.1265 nM, while showing significantly less toxicity to non-ALK-dependent THP-1 cells (IC50 = 2,704 nM). Furthermore, it effectively reduces tumor volume in NCI H3122 mouse xenograft models at doses of 25, 50, and 100 mg/kg.

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].

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

Boc-10-Aminodecanoic acid can be used as a PROTAC linker in the synthesis of PROTACs and other conjugation applications. Boc-10-Aminodecanoic acid is an alkane chain with terminal carboxlic acid and Boc-protected amino groups. 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. The Boc group can be deprotected under mild acidic conditions to form the free amine.

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].

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].

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

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

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].