protac irak4 degrader 1

PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon based PROTAC consisting of the PROTAC IRAK4 ligand-1, the E3 ligase ligand Pomalidomide and the PROTAC linker AM-Imidazole-PA-Boc.

PROTACIRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader, demonstrating DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes within PBMCs, respectively. It significantly induces TIR signaling activation and inhibits the expression of circulating pro-inflammatory cytokines in a psoriasis mouse model induced by Imiquimod. PROTACIRAK4 degrader-13 is applicable in the study of neutrophilic inflammatory diseases driven by TLR and IL-1R, such as hidradenitis suppurativa (HS) and atopic dermatitis (AD).

PROTAC IRAK4 degrader-12, a Cereblon ligand-based PROTAC, induces a maximum degradation of IRAK4 in K562 cells at 108.46% with an IC50 value of 4.87 nM. (Structure Note: Pink, IRAK4 Inhibitor; Blue, E3; Black, linker.)

PROTACIRAK4 degrader-11 (compound 15) is a PROTAC molecule utilizing a Cereblon ligand, achieving a maximal IRAK4 degradation rate of 96.25% in HEK293 cells, with a DC50 value of 2.29 nM.

PROTACIRAK4 degrader-10 (compound 10) is an orally active PROTAC based on a Cereblon ligand, achieving a maximum degradation rate of 95.94% for IRAK4 in HEK293 cells with a DC50 value of 7.68 nM.

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.

AM-Imidazole-PA-Boc is an alkyl chain-derived PROTAC linker used for the synthesis of PROTAC IRAK4 degrader-1[1].

LC-MI-3 is an orally active and potent PROTAC degrader of interleukin-1 receptor-associated kinase 4 (IRAK4), with a DC50 value of 47.3 nM. It effectively inhibits the activation of downstream NF-κB signaling. LC-MI-3 is applicable for research in both acute and chronic inflammatory skin conditions.

APH02174 is a highly selective and orally active IRAK4PROTAC degrader, with a DC50 of 4.01 nM in THP-1 cells. It blocks inflammatory signaling by inhibiting IL-6 release and is applicable for researching inflammatory diseases such as psoriasis and rheumatoid arthritis.

PROTAC IRAK4 degrader-4 (US20190192668A1, compound I-127) is a Cereblon-based PROTAC specifically designed to target and degrade interleukin-1 receptor-associated kinase 4 (IRAK4).

PROTAC IRAK4 degrader-6 is a potent Cereblon-based compound designed to degrade [interleukin-1 receptor-associated kinase 4 (IRAK4)].

PROTAC IRAK4 Degrader-2 (Compound 9) is a PROTAC-based degrader that potently reduces IRAK4 levels, achieving a DC50 of 151 nM in peripheral blood mononuclear cells (PBMCs). It also notably decreases IRAK4 protein levels with a DC50 of 36 nM in the same cell type and inhibits several cytokines in PBMCs [1].

KT-474 (KYM-001) is a PROTAC degrader targeting interleukin-1 receptor-associated kinase 4 (IRAK4) with antitumor activity for the study of autoimmune, inflammatory, and cardiovascular disease disorders.

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.

JNJ-1013 is a potent and selective IRAK1 degrader, with IC50 values of 72 nM for IRAK1, 443 nM for IRAK4, and 1071 nM for VHL FP. It induces apoptosis, increases cleaved PARP expression, and decreases the expression of IRAK1, p-IKBα, and pSTAT3(Tyr705) [1].

PROTAC IRAK4 Degrader-8 (Compound 2) is a PROTAC designed to target IRAK4 with an IC50 of 15.5 nM [1].

PROTAC IRAK4 Ligand-3 serves as a ligand for PROTAC IRAK4 Degrader-7 and is utilized in cancer research [1].