(s)thalidomide

(S)-Thalidomide ((S)-(-)-Thalidomide) is the S-isomer of Thalidomide with immunomodulatory, anti-inflammatory, anticancer, anti-angiogenic, and pro-apoptotic activities, used in studying leprosy erythema nodosum and myeloma.

(S)-Deoxy-thalidomide functions as a ligand for E3 ubiquitin ligases. It is linked to target protein ligands via a linker, forming PROTACK-Ras Degrader-3. This compound specifically targets and degrades mutant KRAS proteins.

(S)-Deoxy-thalidomide-Br is a ligand for E3 ligase, utilized in the synthesis of PROTACFHD-609.

(S)-Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 is a conjugate that serves as both an E3 ubiquitin ligase ligand and a linker for NX-2127.

(S)-Deoxy-thalidomide-2,7-diazaspiro[3.5]nonane-C-Pip is a conjugate of an E3 ubiquitin ligase ligand and a linker, employed in the synthesis of PROTACFHD-609.

Compound C63 (S)-Thalidomide-NH-cyclohexane-NH-Ph-NH2 is an E3 ligase plus linker for PROTAC, comprising a cereblon ligand based on Thalidomide and one linker, suitable for PROTAC synthesis.

Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).

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.

JB170, a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM), achieves its selectivity by linking Alisertib to the Cereblon-binding molecule Thalidomide. It demonstrates a strong preference for AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). The mechanism of JB170 involves S-phase arrest, specifically through AURORA-A depletion, and it is notably effective in inhibiting the non-catalytic functions of AURORA-A kinase [1].