ikzf3

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.

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

Lenalidomide hemihydrate is a derivative of Thalidomide, an orally active immunomodulator that acts as a molecular gel. It is a ligand for the ubiquitin E3 ligase cereblon, which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase.

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).

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)

CARM1/IKZF3 ligand 1 functions as an inhibitor of CARM1 and serves as a target protein ligand for the synthesis of PROTAC CARM1/IKZF3 degrader-1.

IKZF3 Degrader 1 (compound 19a) acts as an effective IKZF3 degrader with an EC50 of 0.012 μM and a minimal yield of 9.2%. It enhances the association of IKZF3 with Cereblon (CRBN), subsequently facilitating the ubiquitination and degradation of IKZF3.

MGD-28 is a potent, orally active Cullin-CRBN-dependent IKZF family protein degrader that dose-dependently degrades IKZF1 (Ikaros), IKZF2 (Helios), and IKZF3 (Aiolos) at nanomolar strengths.MGD-28 also degrades CK1α, and has shown antiproliferative activity against a variety of hematologic cancer cell lines showing antiproliferative activity in vitro and antitumor effects in in vivo assays, and is commonly used in multiple myeloma (MM) and hematological disorders.

MGD-4 is an orally active, Cereblon (CRBN)-dependent degrader of IKAROS proteins that demonstrates dose-dependent degradation of IKZF1 (DC50=67.2 nM), IKZF2 (DC50=918.2 nM), and IKZF3 (DC50=95.8 nM). The compound effectively inhibits the growth of multiple myeloma.

Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.

MS40 is a WDR5 PROTAC that selectively degrades WDR5 and serves as a novel degrader for immune-modulating compounds (IMiDs), including the new substrates CRBN and Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3. MS40 facilitates the degradation of WDR5, resulting in the dissociation of the MLL/KMT2A complex from chromatin, thereby reducing H3K4me2 levels. In vitro, MS40 inhibits the growth of primary leukemia patient cells, and in vivo, it suppresses the expansion of patient-derived xenografts.

Thalidomide-NH-C4-Boc is a compound that acts as a ligand and linker for the E3 ligase (Cereblon). It is utilized in the synthesis of PROTAC CARM1/IKZF3 degrader-1.

Tert-Butyl 6-aminocaproate (Tert-butyl 6-aminohexanoate) is a PROTAC linker. It is utilized in the synthesis of the PROTAC CARM1/IKZF3 degrader-1.

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].

NX-2127 (ETX2514 Triethylamine) is an orally active BTK inhibitor that induces degradation of mutant BTKC481S in cells.NX-2127 has potent antiproliferative activity and inhibits the proliferation of BTKC481S mutant TMD8 cells.NX-2127 potently catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) at 25 nM and 54 nM, respectively. NX-2127 is associated with the immune system, stimulating T cell activation and increasing IL-2 production in primary human T cells.

Zomiradomide is a PROTAC degradation agent targeting IRAK4, with oral bioavailability, and can also degrade Ikaros (IKZF1) and Aiolos (IKZF3), thereby inhibiting the NF-κB signalling pathway and activating the type I interferon signalling pathway, exhibiting anticancer activity against B-cell lymphoma.

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].

Lenalidomide-13C5,15N is a variant of Lenalidomide labeled with 15N and 13C. Lenalidomide (CC-5013), a derivative of Thalidomide, is an orally active immunomodulatory agent acting as a molecular glue. It serves as a ligand for the E3 ubiquitin ligase cereblon (CRBN), facilitating the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 ubiquitin ligase. Notably, Lenalidomide (CC-5013) suppresses the growth of mature B cell lymphomas, including multiple myeloma, and stimulates T cells to release interleukin-2 (IL-2).

Lenalidomide-d5 is a deuterated form of Lenalidomide. Lenalidomide (CC-5013) is a derivative of Thalidomide and acts as an orally active immunomodulator in a molecular glue manner. It serves as a ligand for the ubiquitin E3 ligase cereblon (CRBN). Through the CRBN-CRL4 ubiquitin ligase complex, Lenalidomide selectively ubiquitinates and degrades the lymphocyte transcription factors IKZF1 and IKZF3. It effectively inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and induces T cells to release interleukin-2 (IL-2).