2. Signaling Pathways
  3. Immunology/Inflammation
  4. IRAK
  5. IRAK Degrader

IRAK Degrader

IRAK Isoform Comparison

IRAK Degraders (23):

Cat. No. Product Name Effect Purity
  • HY-174455A
    APH02174 hemiformic
    		Degrader
    APH02174 hemiformic is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 hemiformic blocks inflammatory signals by inhibiting IL-6 release. APH02174 hemiformic can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis.
  • HY-145483A
    KT-474 hydrochloride
    		Degrader ≥98.0%
    KT-474 (KYM-001; PROTAC IRAK4 degrader-7) hydrochloride is an orally active PROTAC IRAK4 degrader with anti-tumor effects. KT-474 inhibits the cell cycle and induces apoptosis. KT-474 induces tumor regression in a xenograft model of MYD88-mutated ABC DLBCL. KT-474 is a click chemistry reagent, containing an alkyne group, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing azide groups.
  • HY-153368
    Zomiradomide
    		Degrader 98.04%
    Zomiradomide is an orally active PROTAC degrader for IRAK4 (DC50=6 nM), thereby inhibiting the NF-κB signaling pathway. Zomiradomide acts also as a molecular glue, recruiting Ikaros and Aiolos, and mediating their degradation (DC50 for Ikaros is 1 nM), thereby activating the type I IFN signaling pathway. (Pink: target protein ligand PROTAC IRAK4 ligand-5 (HY-168311), Blue: E3 ligase ligand Thalidomide-4-Br (HY-W039116), Black: linker (HY-168313))
  • HY-153188
    JNJ-1013
    		Degrader 99.97%
    JNJ-1013 is a potent and selective IRAK1 PROTAC degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) (Pink: ligand for target protein (HY-138834); black: linker (HY-Y1760); Blue: E3 ligase ligand (HY-112078)).
  • HY-142662A
    PROTAC IRAK3 degrade-1 formic
    		Degrader 99.26%
    PROTAC IRAK3 degrade-1 (compound 23) formic is a potent and selective degrader of IRAK3 (IC50=5 nM).
  • HY-129966
    PROTAC IRAK4 degrader-1
    		Degrader 99.77%
    PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon-based IRAK4 PROTAC. PROTAC IRAK4 degrader-1 is composed of IRAK4 ligand (red part) PROTAC IRAK4 ligand-1 (HY-129967), E3 ligase ligand (blue part) Pomalidomide (HY-10984), and PROTAC linker (black part) AM-Imidazole-PA-Boc (HY-129968).
  • HY-137342
    SB1-G-187
    		Degrader 98.70%
    SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research. (Pink: multi-target kinase ligand (HY-125142); Blue: CRBN ligand (HY-A0003); Black: linker).
  • HY-148290
    KTX-951
    		Degrader 99.60%
    KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader (Kd = 3.5 nM). KTX-951 has DC50s of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. KTX-951 has IC50 of 35 nM for OCl-Ly10 CTG. KTX-951 has antitumor activity.(Pink: IRAK4 ligand-12 (HY-48932); Black: Linker (HY-W382009); Blue: CRBN Ligand Pomalidomide (HY-10984)).
  • HY-175022
    PROTAC IRAK4 degrader-13
    		Degrader 99.47%
    PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC50s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research. Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker
  • HY-179094
    PSP-0119
    		Degrader 98.65%
    PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC50 = 2.83 nM). PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML).
  • HY-175764
    FIP22
    		Degrader 98.53%
    FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871)).
  • HY-153673
    PROTAC IRAK4 degrader-8
    		Degrader 99.70%
    PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively.
  • HY-172590
    LZ-07
    		Degrader
    LZ-07 is a IRAK4 PROTAC degrader (DC50 = 1.14 nM). LZ-07 leads to marked suppression of cytokines including IL-6, IL-1β, TNF-α, and IL-10 upon degradation of IRAK4. LZ-07 can be studied in research for autoimmune diseases (Pink: IRAK4 ligand (HY-172591); Blue: CRBN ligand (HY-34590); Black: linker (HY-B0149); CRBN ligand + linker: HY-172593).
  • HY-174455
    APH02174
    		Degrader
    APH02174 is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 blocks inflammatory signals by inhibiting IL-6 release. APH02174 can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis.
  • HY-168611
    PROTAC IRAK4 ligand-4
    		Degrader
    PROTAC IRAK4 ligand-4 is a Ligand for Target Protein for PROTAC with antitumor activity. PROTAC IRAK4 ligand-4 can be used to synthesize PROTAC IRAK4 degrader-12 (HY-168586).
  • HY-168586
    PROTAC IRAK4 degrader-12
    		Degrader
    PROTAC IRAK4 degrader-12 is a PROTAC based on Cereblon ligand, inducing a maximum degradation rate of IRAK4 of 108.46% in K562 cells with an IC50 value of 4.87 nM ( Structure Note: Pink, IRAK4 inhibitor (HY-168611); Blue, E3 (HY-W733885); Black, linker (HY-168613)).
  • HY-181898
    PROTAC IRAK3 degrader-2
    		Degrader
    PROTAC IRAK3 degrader-2 (Compound 17) is a IRAK3 PROTAC degrader with a DC50 ≤ 50 nM. It promotes ubiquitination and degradation of IRAK3, and is applicable to the research of immune diseases.
  • HY-183799
    GSI526
    		Degrader
    GSI526 is a IRAK4 PROTAC degrader (DC50=40.17 nM, Dmax=97%; THP-1) based on the VHL ubiquitin-proteasome system. GSI526 inhibits IRAK4-mediated NF-κB and MAPK inflammatory signaling pathways, and induces IRAK4 degradation in myeloid cells. GSI526 is applicable to inflammation-related research.
  • HY-142662
    PROTAC IRAK3 degrader-1
    		Degrader
    PROTAC IRAK3 degrade-1 (compound 23) is a potent and selective degrader of IRAK3 (IC50 = 5 nM).
  • HY-158758
    PROTAC IRAK4 degrader-10
    		Degrader
    PROTAC IRAK4 degrader-10 (compound 10) is an oral active PROTAC based on Cereblon ligand, and induces the degradation of IRAK4 with maximum degradation of 95.94% and the DC50 of 7.68 nM in HEK293 cells (Sturcture Note:(Blue: Cereblon ligand, Black: linker；Pink: IRAK4 ligand).