cereblon ligand-3

Thalidomide-O-COOH (Cereblon ligand 3) is a Thalidomide-based Cereblon ligand utilized for recruiting the CRBN protein and can be linked to a protein ligand via a linker to create PROTACs.

FC 11 is a highly potent focal adhesion Ki nase (FAK) PROTAC®Degrader (DC50 values are 40 to 370 pM depending on cell line), which is composed of the FAK inhibitor PF 562217 joined by a linker to the cereblon-binding ligand Pomalidomide. The effects of FC 11 are reversible upon compound wash out. FC 11 also degrades autophosphorylated FAK (pFAKtyr397), displaying near complete degradation after 3 hours at 100 nM in TM3 cells.

E3 ligase Ligand 23 is a cereblon binding agent that degrades Ikaros or Aiolos via the ubiquitin proteasome.

5-Aminothalidomide is a E3 ligase ligand used in PROTAC technology.

Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) is the Thalidomide-based cereblon ligand that used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTAC.

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

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-amido-C3-NH2 TFA (Cereblon Ligand-Linker Conjugates 16 TFA) is a synthesized E3 ligase ligand-linker conjugate incorporating a Thalidomide-based cereblon ligand and a linker used in PROTAC technology.

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

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.

ZXH-3-26 is a PROTAC composed of a Cereblon ligand, an E3 ubiquitin ligase, and a BRD4 ligand that can be used to study cancer.

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.

Pomalidomide-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

Pomalidomide-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 5) is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide based cereblon ligand and 3-unit PEG linker.

Thalidomide-O-amido-C3-COOH is a synthesized conjugate of an E3 ligase ligand-linker compound that combines a cereblon ligand (derived from Thalidomide) with a linker commonly employed in PROTAC technology.

Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is an E3 ligase ligand-linker conjugate developed using a Thalidomide-based cereblon ligand and a 3-unit PEG linker, synthesized specifically for use in PROTAC technology.

Thalidomide-O-amido-PEG1-(C1-PEG)2-C2-NH2 is a synthesized E3 ligase ligand-linker, incorporating a cereblon ligand based on Thalidomide and a 3-unit PEG linker, specifically designed for PROTAC technology applications.

Lenalidomide-PEG3-iodine, an E3 ligase ligand-linker conjugate, consists of a cereblon-based Lenalidomide ligand and a 3-unit polyethylene glycol (PEG) linker. This compound is utilized in creating various proteolysis targeting chimeras (PROTACs), including the highly effective PROTAC BTK degrader SJF620, which has a degradation concentration 50 (DC50) of 7.9 nM[1].

Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate, incorporates a cereblon ligand derived from Thalidomide and a 3-unit PEG linker. This compound is specifically designed for use in PROTAC technology, which utilizes small molecules to induce protein degradation [1].

YB-3-17 is a bifunctional molecule that can inhibit mTOR with an IC50 of 0.22 nM or degrade the G1 to S phase transition 1 gene (GSPT1) through the PROTAC mechanism, with a DC50 of 5 nM. It exhibits antiproliferative activity at nanomolar concentrations in various glioblastoma cell lines. Additionally, YB-3-17 shows antitumor activity in mouse models. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon)

E3 Ligase Ligand-linker Conjugate 168 is a compound composed of a ligand for the E3 ligase Cereblon and a linker. It is utilized in the synthesis of PROTAC c-Met degrader-3.

PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)

PROTAC HDAC6 degrader4 (Compound 17c) is a PROTAC that targets and degrades HDAC6, with a DC50 of 14 nM. It exhibits inhibitory activity against HDAC1, HDAC2, HDAC3, and HDAC6, with IC50 values of 2.2, 2.37, 0.61, and 0.295 μM, respectively. [Pink: ligand for target protein HDAC6 ligand-3; Black: linker; Blue: ligand for cereblon E3 ligase]

PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0/G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)