protac-i

PROTAC-I targets steroid hormone receptors for ubiquitination and degradation.

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.

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 ligand-1 is a synthetic ligand targeting interleukin-1 receptor-associated kinase 4 (IRAK4).

Bestatin-amido-Me, a derivative of Bestatin, acts as an IAP ligand and interacts with ABL inhibitor through a linker to produce SNIPER[1].

MV-1-NH-Me, an MV-1-derived IAP ligand, connects to an ABL inhibitor through a linker, resulting in the formation of SNIPER[1].

PROTAC IRAK4 ligand-5, a ligand for the target protein of PROTAC, is instrumental in the synthesis of KT-413.

PROTAC IRAK4 ligand-4, a Ligand for Target Protein for PROTAC (Ligand for Target Protein for PROTAC), exhibits anti-tumor activity and is utilized in synthesizing PROTAC IRAK4 degrader-12. This compound serves as a targeted ligand with specific applications in the development of cancer therapeutics.

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-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 IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

PROTAC IRAK4 degrader-5 is a Cereblon-based compound designed to selectively degrade IRAK4.

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

PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau (VHL).

PROTAC IRAK3 degrade-1 is a potent and selective degrader of IRAK3 ( IC 50 = 5 nM).

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.

PROTAC IRAK3 Degrade-1 (Compound 23) is a selective and potent IRAK3 degrader, demonstrating an IC50 value of 5 nM [1].

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

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.

I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).

Compound I-291, also known as PROTAC SMARCA2/4-degrader-30, targets the catalytic subunits of the SWI/SNF complex, specifically SMARCA2 and SMARCA4. It effectively degrades SMARCA2 in A549 and MV411 cells, as well as SMARCA4 in MV411 cells, with a degradation concentration (DC50) of less than 100 nM.

PROTAC SMARCA2/4-degrader-29 (Compound I-279) serves as a degrader for the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. In A549 cells, this compound effectively degrades SMARCA2 with a DC50 value of less than 100 nM, and similarly degrades SMARCA4 in MV411 cells with a DC50 under 100 nM.

PROTAC SMARCA2 degrader-6 (compound I-427) is a PROTAC molecule targeting SMARCA2, exhibiting a DC50 of less than 100 nM and a maximum degradation rate (Dmax%) of over 90% in A549 cells after 24 hours of treatment.