cereblon (crbn) e3 ligase

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

Dicyclanil is an insect growth regulator with a chemical structure similar to that of cyclopromazine.

CFT7455 (Cemsidomide) is an anti-cancer agent showing high affinity to the cereblon E3 ligase with a Kd of 0.9 nM. CFT7455 is an orally active degrader of zinc finger transcription factors Ikaros (IKZF1), and Aiolos (IKZF3).

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.

Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.

Lenalidomide-Br (Compound 41), a derivative of Lenalidomide, acts as a ligand for cereblon (CRBN) - an E3 ubiquitin ligase involved in protein recruitment. This compound can be conjugated to a protein ligand via a linker to create PROTACs, such as the PROTAC STAT3 degrader SD-36.

Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN) and is commonly used in the synthesis of PROTAC products.

Thalidomide 4-fluoride (E3 ligase Ligand 4) (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand. Thalidomide 4-fluoride can be used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

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

CC-885 is a modulator of cereblon (CRBN). It has potent anti-tumour activity.

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].

Lenalidomide-C4-NH2 hydrochloride is a PROTAC linker that can be used to construct small-molecule linkers or PROTAC molecules to induce the degradation or regulation of target proteins. Lenalidomide-C4-NH2 hydrochloride acts as a ligand for the E3 ubiquitin ligase CRBN and is used to study protein degradation, signaling pathway regulation, and pharmacological mechanisms.

Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for the target protein AKT used in PROTAC, binding to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 for AKT degradation[1].

Lenalidomide-OH is an analog of Lenalidomide, a cereblon ligand for E3 ubiquitin ligase (CRBN), used for CRBN protein recruitment. It is able to attach to protein ligands using linkers to form PROTAC.

Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride is a chemical compound comprising a cereblon (CRBN) ligand that functions as an E3 ubiquitin ligase, along with a linker. It is utilized to create the PROTAC MD-224[1].

Lenalidomide-propargyl-C2-NH2 hydrochloride is a compound that features a cereblon (CRBN) ligand for the E3 ubiquitin ligase, as well as a linker. It is utilized in the development of the PROTAC MD-224[1] system.

Pomalidomide-C2-amide-C4-Br is an E3 ligase ligand-linker conjugate (E3 Ligase Ligand-linker conjugate) comprising a Pomalidomide-based Cereblon (CRBN) ligand and one linker unit. This compound is utilized in the synthesis of PROTACs.

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.

AB3067 is a PROTAC degrader targeting BET protein, efficiently recruiting two distinct E3 ligases, Cereblon and VHL, with strong affinity (demonstrated by IC50 values of 559 nM for VHL and 190 nM for CRBN in vivo HEK293). It degrades BRD2, BRD3, BRD4, and CRBN with DC50 values of 2.1~2.3, 1.6, 15, and 75 nM, respectively. Additionally, AB3067 inhibits the proliferation of RKO cells, with an EC50 of 111 nM. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL and CRBN)

CRBN ligand-47 is a ligand for the cereblon (CRBN) type E3 ubiquitin ligase, suitable for use in the development of PROTAC.

CRBN ligand-63 is a ligand for the cereblon (CRBN) type E3 ubiquitin ligase and can be utilized in the creation of PROTACs.

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)

BMS-986458 is an oral heterobifunctional degrader that targets the Cereblon (CRBN) E3 ubiquitin ligase. By binding to the BTB domain of BCL6, it induces the formation of a ternary complex between BCL6 and CRBN, thereby promoting the ubiquitination and proteasomal degradation of BCL6. BMS-986458 exhibits high selectivity for BCL6 degradation while showing weak degradation activity toward known new CRBN substrates (such as Ikaros, Aiolos, SALL4, and GSPT1), making it a valuable tool for studying BCL6-related tumor signaling pathways and antitumor mechanisms.

E3LigaseLigand-linker Conjugate 184 is a conjugate consisting of an E3 ligase ligand and a linker (E3LigaseLigand-Linker Conjugates), composed of CDK2ligand-2 and its corresponding linker. E3LigaseLigand-linker Conjugate 184 can act as a Cereblon ligand to recruit CRBN protein and serves as a key intermediate in the synthesis of CDK2 degrader2.