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.

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.

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.

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)