PROTAC IRAK3 degrade-1 is a potent and selective degrader of IRAK3 (IC50 = 5 nM).

A Novel PROTACs building block.

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.

CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.

RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.

ATP-PEG8-Biotin is a PEG-based linker that incorporates ATP. ATP is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.

AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.

Biotin-PEG7-C2-NH-Vidarabine-S-CH3 is a PEG-based linker that incorporates adenosine analog Vidarabine. Vidarabine is an antiviral agent which is active against herpes simplex and varicella zoster viruses.

Biotin-PEG7-C2-S-Vidarabine is a PEG-based linker that incorporates adenosine analog Vidarabine. Vidarabine is an antiviral agent which is active against herpes simplex and varicella zoster viruses.

Biotin-PEG8-Vidarabine is a PEG-based linker that incorporates adenosine analog Vidarabine. Vidarabine is an antiviral agent which is active against herpes simplex and varicella zoster viruses.

Folate-MS432, a PROTAC, is capable of degrading MEKs in a folate receptor-dependent manner in cancer cells.

Lenalidomide-C5-amido-Boc is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-amido-Boc can be connected to the ligand for protein by a linker to form PROTAC.

SJ995973 (PROTAC) is a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins.

Thalidomide-O-amido-C6-NH2 (Cereblon Ligand-Linker Conjugates 11), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.

Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader. (From patent WO2017180417A1 compound s7).

TLR4-IN-C34-C2-amide-C6-OH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

MDK7526, also known as VHL Ligand 1; Protein degrader 1, is a potent and selective protein degrader.

ZXH-4-130 is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC).

ZXH-4-137 is a potent and selective CRBN degrader (PROTAC).

Thalidomide-O-C6-NHBoc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

Thalidomide-Piperazine-Piperidine hydrochloride is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-Piperazine-Piperidine hydrochloride incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

Thalidomide-4-O-C10-COOH is a E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs.

PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs.

PROTAC BRD4 ligand-2 is a ligand for target BRD4 protein for PROTAC CFT-2718.

Propargyl-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.

PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.

MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.