3,4 dibromo mal peg2 amine

3,4-Dibromo-Mal-PEG2-amine is a polyethylene glycol (PEG) derivative that functions as a PEG-based PROTAC linker, enabling the synthesis of PROTACs[1].

4-Bromo-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione has potential as an anticancer, prodrug for the treatment of Parkinson's disease, and as an anti-inflammatory agent.

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.

2,3,4,6-Tetra-O-acetyl-alpha-galactosylpyranosyl bromide (2-3-4-6-tetra-o-acetyl-alpha-galactosylpyranosyl-bromide) is an alkyl chain-based PROTAC linker used in PROTAC synthesis.

Butanoic acid, 4-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]- (4-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]butanoic acid) is a Cereblon ligand with alkyl linker and terminal acid for onward chemistry.

Thalidomide-O-C6-NH2 hydrochloride (4-((6-aminohexyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride) is a synthesized E3 ligase ligand-linker conjugate.

CRBN ligand-9 (2-(2,6-dioxopiperidin-3-yl)-5-nitroisoindoline-1,3-dione) exhibit inhibition of CRBN.

Pomalidomide-PEG2-OH enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology.

Thalidomide-NH-CH2-COOH ((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)glycine) is a synthesized E3 ligase ligand-linker conjugate containing a Thalidomide-based cereblon ligand and a linker.

Pomalidomide-PEG3-OH enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology.

PROTAC SMARCA2 4-degrader-26 is a PROTAC targeting the SMARCA2 4 proteins. It is composed of the ligand for PROTAC targeting proteins, 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid, an E3 ligase component (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, and a PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid. The coupled complex of the E3 ubiquitin ligase ligand + Linker is referred to as (S,R,S)-AHPC.

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. It effectively induces apoptosis in MYD88 MT DLBCL and has demonstrated efficacy in inducing in vivo tumor regressions in a lymphoma model [1] [2] [3].

Pomalidomide-C2-NH2 (4-[(2-Aminoethyl)amino]-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione) is a synthesized E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a linker.

3-(4-Bromo-2-chlorophenyl)piperidine-2,6-dione acts as a ligand for CRBN type E3 ubiquitin ligase and is useful in the synthesis of PROTAC.

Thalidomide-NH-PEG1-NH2 hydrochloride (4-[(2-(2-Aminoethoxy)ethyl)amino]-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione HCl) is a synthetic E3 ligase ligand-linker conjugate that incorporates the Thalidomide-based cereblon ligand and a linker[1].

PROTAC ER Degrader-14 (compound 86) is a PROTAC-type estrogen receptor ERR degrader. It comprises an E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide, a PROTAC linker (black part) N-Boc-piperazine, and a target protein ligand (red part) ER ligand-6. The combination of the E3 ligase and linker forms tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate.

LL-K9-3, a selective hydrophobic tagging technology (HyT)-based degrader, specifically targets the CDK9-cyclin T1 complex, displaying DC50 values of 589 nM for cyclin T1 and 662 nM for CDK9. This compound consists of the CDK9 inhibitor, SNS 032, linked to a hydrophobic tag via a glycol linker. Notably, LL-K9-3 does not affect the degradation of other CDKs (CDK1, 2, 4, 5, 6, and 7). Tested in 22RV1 cells, it effectively reduces androgen receptor (AR) and cMyc expression by inducing the selective and synchronous degradation of CDK9 and cyclin T1.

PROTAC SMARCA2 4-degrader-25 is a PROTAC that targets SMARCA2 4. It consists of the E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, a PROTAC Linker (S)-2-Amino-3,3-dimethylbutanoic acid, and the target protein ligand SMARCA2 4-ligand-3. The conjugate of the E3 ubiquitin ligase ligand and Linker is (S,R,S)-AHPC.

3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione is a CRBN-type E3 ubiquitin ligase ligand, which can be used in the preparation of PROTACs.

DZ-837 is a PROTAC that targets the BCL6 protein. The composition of DZ-837 includes the BCL6 ligand-2, the E3 ubiquitin ligase ligand Thalidomide-4-OH, and a PROTAC Linker. The configuration notably features a conjugate of the E3 ubiquitin ligase ligand and the Linker, designated as 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione.

APN-C3-NH-Boc is a alkyl ether-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

Tetraethylene glycol (PROTAC Linker 18) is a PEG-based linker used in PROTAC synthesis[1].

ALV1 is a potent degradation agent of Ikaros and Helios, with similar degradation activity against IKZF1 2 3. ALV1 significantly reduced the protein abundance of IKZF1-4, CK1α (casein kinase 1α, CSNK1A1) and ribosomal protein RPL4, and induced Helios CRBN dimerization, which promoted IL-2 secretion.