crbn ligand-9

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

FN-1501-propionic acid, a CDK2 9 ligand, in conjunction with a CRBN ligand, has been utilized in the design of a PROTAC CDK2 9 degrader.

Thalidomide-C2-amido-C2-COOH is a compound that includes a CRBN ligand for the E3 ubiquitin ligase, as well as a linker. It is utilized in the development of PROTAC CDK2 9 Degrader-1[1].

JQ dS-4 is a degrader of Brahma-related gene 1 (BRG1) BRM SMARCA4 (PROTAC®; DC50 range = 9 - 390 nM in glioma models and cell lines), featuring a BRG1 inhibitor connected through a linker to a cereblon (CRBN) E3 ligase ligand. It effectively degrades BRG1 completely over 48 and 72 hours in HSJD-DIPG007 and SU-DIPGXIIIP cells. Additionally, it lessens the viability of various cancer cell lines, including those of H3K27M glioma, prostate, thyroid, and salivary gland.

E3 ligase Ligand 48 is the CRBN ligand of PROTACAR Degrader-9. PROTACAR Degrader-9 (Compound c6) functions as a PROTAC degrader targeting the androgen receptor, effectively degrading AR in human dermal papilla cells (HDPC) with a DC50 of 262.38 nM.

CRBN ligand-12 (Compound 9) is a ligand for the CRBN-type E3 ubiquitin ligase. It is utilized in the preparation of PROTAC.

ROR1ligand-1 (9-1) serves as the ligand for PROTAC ROR1 degrader-1. By linking with ligands of either the VHL type or CRBN, the first selective and efficient ROR1 PROTAC molecule was designed and synthesized.

PROTAC FGFR1 degrader-1 (compound S2H) is a targeted degrader of FGFR1, demonstrating an IC50 of 26.81 nM and a DC50 of 39.78 nM in KG1a cells. This compound is composed of a CRBN-type E3 ligase ligand (blue part) Pomalidomide, a target protein ligand (red part) FGFR1ligand-1, and a PROTAC linker (black part) 9-Bromononanoic acid, together forming the conjugate E3LigaseLigand-linker Conjugate 164.