cereblon ligand-2

Thalidomide-4-OH (E3 ligase Ligand 2) (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used to recruit of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) is a linker to form PROTACs

TSPO ligand-2 (Carbonic acid) is a ligand of AUTAC1 which contains a p-fluorobenzylguanine and a Fumagillol moiety.

PROTAC ERRα ligand 2 is an inverse agonist for the estrogen-related receptor α (ERRα) with an IC50 of 5.67 nM.

Thalidomide-O-amido-PEG1-(C1-PEG)2-C2-NH2 is a synthetic conjugate that combines a Thalidomide-based cereblon ligand and a linker, commonly utilized in PROTAC technology. This compound serves as a connector between the target protein and the E3 ligase, facilitating targeted protein degradation.

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.

Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2) is a synthesized E3 ligase ligand-linker conjugate containing a Thalidomide-based cereblon ligand and a linker, useful in the synthesis of PROTACs, as per reference [1].

PROTAC BRD4 ligand-2 is a ligand for the target BRD4 protein used in the development of PROTAC CFT-2718.

CBP p300 ligand 2 is a selective ligand that binds to the target protein for PROTAC[dCBP-1], a potent and selective heterobifunctional degrader of p300 CBP.

cIAP1 ligand 2, a derivative of LCL161, is an IAP ligand that can be connected to the ABL ligand for protein via a linker, resulting in the formation of SNIPER.

Thalidomide-NH-CBP p300 ligand 2 (P-007) is a PROTAC-based compound engineered to degrade the proteins CBP and p300, functioning as a molecular antagonist (WO2020173440).

cIAP1 Ligand-Linker Conjugates 2 Hydrochloride is a chemical compound that combines an IAP ligand, targeting the E3 ubiquitin ligase, with a PROTAC linker and is utilized in the creation of SNIPERs[1].

K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in synthesizing PROTAC K-Ras Degrader-1, a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

PROTAC BRD4 Ligand-2 Hydrochloride serves as a ligand targeting the BRD4 protein, specifically designed for use with PROTAC CFT-2718.

cIAP1 Ligand-Linker Conjugates 2 is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker. This compound is particularly useful in the design of SNIPERs [1].

GID4 Ligand 2 (compound 67) is a selective binder for GID4 with an IC50 of 18.9 μM and a Kd of 17 μM, and can be used for the synthesis of PROTACs [1].

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-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.

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].

Pomalidomide-PEG1-CO2H is a synthetic E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a 2-unit PEG linker.

Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and a linker used in [PROTAC] technology.

Thalidomide-O-amido-PEG2-C2-NH2 TFA (E3 Ligase Ligand-Linker Conjugates 24 TFA) is a synthesized E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and a 2-unit PEG linker, utilized in PROTAC 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.

Thalidomide-O-amido-PEG3-C2-NH2 TFA, a synthesized E3 ligase ligand-linker conjugate, combines the cereblon ligand based on Thalidomide and a 2-unit PEG linker for use in PROTAC technology[1].

Pomalidomide-PEG4-Ph-NH2 is a synthetic E3 ligase ligand-linker conjugate that integrates a Pomalidomide-based cereblon ligand with a 4-unit PEG linker.

Thalidomide-O-amido-PEG3-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology[1].

Pomalidomide-PEG2-Tos is a compound that consists of an E3 ligase ligand-linker conjugate. It is composed of a cereblon ligand conjugated to a two-unit PEG linker[1].

SirReal1-O-propargyl, a moiety based on SirReal1, is a selective and highly potent inhibitor of Sirtuin 2 (Sirt2), demonstrating an IC50 of 2.4 μM. It operates by binding to the cereblon ligand through a linker, facilitating the formation of PROTAC for the degradation of Sirt2[1].

Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a chemically synthesized E3 ligase ligand-linker conjugate, incorporating the cereblon ligand from Pomalidomide and a linker used in PROTAC technology. It facilitates targeted protein degradation by modulating E3 ligase activity, thereby enabling the selective elimination of specific proteins of interest.

Thalidomide-NH-(CH2)2-NH2 TFA, an alkyl-modified derivative of Thalidomide, functions as a Cereblon ligand to recruit CRBN proteins and serves as a crucial intermediate in the synthesis of CRBN-based PROTAC molecules targeting the SHP2 protein.

Lenalidomide hydrochloride (CC-5013 hydrochloride), a Thalidomide derivative, functions as molecular glue and serves as an orally active immunomodulator. As a ligand for the ubiquitin E3 ligase cereblon (CRBN), it facilitates the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase. Specifically, Lenalidomide hydrochloride inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and promotes IL-2 release from T cells [1] [2].

Thalidomide-O-PEG2-propargyl (E3 Ligase Ligand-Linker Conjugates 32) is a chemical compound that has been synthesized as a conjugate of an E3 ligase ligand and a linker. It incorporates the cereblon ligand based on Thalidomide, along with a 2-unit PEG linker. This compound is specifically designed for use in PROTAC technology, which utilizes ligand-induced protein degradation [1].

Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1].

C-02, a proteolysis-targeting chimera (PROTAC) that combines the hexokinase inhibitor lonidamine with the cereblon ligand thalidomide, effectively induces the degradation of hexokinase 2 in 786-O and PANC-1 cells at a concentration of 20 µM. This compound exhibits cytotoxicity to a range of cancer cells, including 786-O, 4T1, PANC-1, HGC-27, and MCF-7, with IC50 values of 34.07 µM, 5.08 µM, 31.53 µM, 6.11 µM, and 21.65 µM, respectively. Additionally, at 20 µM, C-02 diminishes both the extracellular acidification rate (ECAR) and oxygen consumption rate (OCR) in 4T1 cells, suggesting a suppression of glycolysis and mitochondrial damage. In vivo studies reveal that at a dosage of 50 mg/kg, C-02 not only reduces tumor volume but also promotes intratumoral cytokine accumulation and triggers pyroptosis in a 4T1 murine mammary carcinoma model.

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.

Pomalidomide-amido-C4-amido-PEG2-C2-NH-Boc is a novel synthesized conjugate compound functioning as an E3 ligase ligand-linker in PROTAC technology. Incorporating a Pomalidomide-derived cereblon ligand that selectively binds to the E3 ligase cereblon and a 2-unit PEG linker, it provides stability and flexibility to the conjugate.

Pomalidomide-PEG2-CO2H is a synthetic E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a 2-unit PEG linker.

Thalidomide-O-amido-PEG2-C2-NH2, which combines an E3 ligase ligand with a linker, serves as an immunomodulator for cancer treatment.

Pomalidomide-PEG2-azide is a synthetic conjugate consisting of a cereblon ligand derived from Pomalidomide and a 2-unit PEG linker, designed for use in PROTAC technology as a ligand-linker conjugate of E3 ligase.

Lenalidomide (sodium), a Thalidomide derivative, serves as a molecular glue and an orally active immunomodulator. It acts as a cereblon (CRBN) ligand and triggers selective ubiquitination and subsequent degradation of the lymphoid transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 ubiquitin ligase. Echoing its specificity, Lenalidomide (sodium) inhibits the proliferation of mature B-cell lymphomas, notably multiple myeloma, and promotes IL-2 secretion from T cells [1] [2].

Abemaciclib metabolite M18 (LSN3106729) is a potent cyclin-dependent kinase (CDK) inhibitor with antitumor properties. It has been incorporated alongside a cereblon (CRBN) ligand to develop a proteolysis-targeting chimera (PROTAC) that selectively degrades CDK4/6 [1] [2].