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IRAK

The interleukin-1 receptor (IL-1R) associated kinase (IRAK) family plays a crucial role in the protective response to pathogens introduced into the human body by inducing acute inflammation followed by additional adaptive immune responses. IRAKs are essential components of the Interleukin-1 receptor signaling pathway and some Toll-like receptor signaling pathways. Toll-like receptors (TLRs) detect microorganisms by recognizing specific pathogen-associated molecular patterns (PAMPs) and IL-1R family members respond the interleukin-1 (IL-1) family cytokines. These receptors initiate an intracellular signaling cascade through adaptor proteins, primarily, MyD88. This is followed by the activation of IRAKs. TLRs and IL-1R members have a highly conserved amino acid sequence in their cytoplasmic domain called the Toll/Interleukin-1 (TIR) domain. The elicitation of different TLRs/IL-1Rs results in similar signaling cascades due to their homologous TIR motif leading to the activation of mitogen-activated protein kinases (MAPKs) and the IκB kinase (IKK) complex, which initiates a nuclear factor-κB (NF-κB) and AP-1-dependent transcriptional response of pro-inflammatory genes. Understanding the key players and their roles in the TLR/IL-1R pathway is important because the presence of mutations causing the abnormal regulation of Toll/IL-1R signaling leading to a variety of acute inflammatory and autoimmune diseases.IRAKs are membrane proximal putative serine-threonine kinases. Four IRAK family members have been described in humans: IRAK1, IRAK2, IRAKM, and IRAK4. Two are active kinases, IRAK-1 and IRAK-4, and two are inactive, IRAK-2 and IRAK-M, but all regulate the nuclear factor-κB (NF-κB) and mitogen-activated protein kinase (MAPK) pathways.

  • IRAK4-IN-20
    T627141931994-80-7
    IRAK4-IN-20 is a potent and orally active IRAK4 inhibitor (IC50:3.55 nM). IRAK4-IN-20, which has anti-inflammatory, antitumor and anticancer effects, is often used to treat acute respiratory distress syndrome (ARDS).
    • $195
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  • IRAK4-IN-8
    T633882033070-97-0In house
    IRAK4-IN-8 (VI-177) is an IRAK4 inhibitor for the study of diseases associated with cancer and inflammation.
    • $868 TargetMol
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  • Larotinib
    T733341438072-11-7
    Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.
    • $74
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  • IRAK4-IN-10
    T619312681278-09-9In house
    IRAK4-IN-10 is a potent IRAK4 inhibitor (IC50: 1.5 nM) with potential anticancer and anti-inflammatory activities.IRAK4-IN-10 blocks MyD88 signaling and can be used for the study of autoimmune diseases and cancers.
    • $633
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  • IRAK inhibitor 2
    T7368928333-30-6In house
    IRAK inhibitor 2 (IRAK-IN-2) is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK-4) for the study of inflammation-related diseases.
    • $78
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    TargetMol | Inhibitor Sale
  • HS271
    T370822410393-15-4In house
    HS271 is a selective, highly potent and orally active IRAK4 inhibitor (IC50= 7.2 μM). HS271 shows excellent enzymatic and cellular activities, as well as excellent pharmacokinetic properties.
    • $93
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  • Zabedosertib
    T370761931994-81-8In house
    Zabedosertib (BAY 1834845) is an inhibitor of IRAK4 with immunomodulatory potential. Zabedosertib protects against acute respiratory distress syndrome, a new study suggests.
    • $36
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  • ANTHRAQUINONE-2-CARBOXYLIC ACID
    T7035117-78-2
    Anthraquinone-2-carboxylic acid acts as a potent anti-inflammatory and antinociceptive component in vivo, thus contributing to the immune regulatory role of fruits and herbs.
    • $40
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    TargetMol | Citations Cited
  • IRAK4-IN-4
    T116731850276-58-2
    IRAK4-IN-4 (compound 15) inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor, has an IC50 of 2.8 nM.
    • $129
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  • GLPG2534
    T751132095615-97-5
    GLPG2534 is an orally active, selective and potent IRAK4 inhibitor with anti-inflammatory activity. GLPG2534 inhibits human and mouse IRAK4 and could be used to study psoriasis and atopic dermatitis.
    • $113
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  • IRAK-4 protein kinase inhibitor 2
    T9631301675-24-1
    IRAK-4 protein kinase inhibitor 2 is a potent interleukin-1 receptor-associated kinase-4 (IRAK-4) inhibitor(IC50 = 4 μM).
    • $39
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  • IRAK4-IN-24
    T78744
    IRAK4-IN-24 (compound 16), a potent IRAK4 inhibitor, exhibits high clearance (Cl) and low oral bioavailability. It is utilized in research pertaining to inflammatory and autoimmune disorders.
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  • AZ1495
    T143672196204-23-4
    AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).
    • $148
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  • IRAK4-IN-25
    T79447
    IRAK4-IN-25 (compound 38), a potent oral IRAK4 inhibitor (IC50 = 7.3 nM) with low clearance (Cl = 12 mL/min/kg), effectively suppresses pro-inflammatory cytokine production and demonstrates favorable in vitro safety and ADME profiles. It is suitable for research on inflammatory and autoimmune disorders [1].
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  • Thalidomide 4-fluoride
    T7755835616-60-9
    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.
    • $29
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  • JH-X-119-01
    T92032227368-54-7
    JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK-1.
    • $60
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  • Zimlovisertib
    TQ01671817626-54-2
    Zimlovisertib (PF-06650833) is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay).
    • $39
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  • IRAK4-IN-7
    T53541801343-74-7
    IRAK4-IN-7 (CA-4948) is a selective and potent IRAK4 kinase inhibitor with in vivo activity in a TLR4-induced cytokine release model.
    • $31
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    TargetMol | Inhibitor Sale
  • IRAK4-IN-1
    T41401820787-94-7
    IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
    • $64
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  • IRAK4-IN-28
    T793372952532-92-0
    IRAK4-IN-28 (compound 42), an orally-active IRAK4 inhibitor (IC50=8.9 nM), exhibits strong binding affinity with a Kd of 0.58 nM for the target enzyme. It is utilized for research purposes in the study of inflammation and autoimmune diseases [1].
    • $1,970
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  • IRAK4-IN-27
    T79485
    IRAK4-IN-27 (Compound 22) is a potent and selective IRAK4 inhibitor, demonstrating an IC50 of 8.7 nM. It effectively suppresses cell growth and induces apoptosis in the MYD88 L265P diffuse large B-cell lymphoma (DLBCL) cell line, positioning it as a valuable agent for DLBCL research [1].
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  • IRAK inhibitor 1
    T50941042224-63-4
    IRAK inhibitor 1 is an effective IRAK-4 inhibitor (IC50: 216 nM), is poorly active against JNK-1 (IC50: 3.801 μM) and JNK-2 (IC50>10 μM).
    • $87
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  • AS-2444697
    T42991287665-60-4
    AS-2444697 is an inhibitor of IRAK-4 (C50 = 21 nM). AS-2444697 exhibits renoprotective effects through anti-inflammatory action. AS-2444697 potently inhibits human and rat IRAK-4 activity.
    • $38
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  • CA-4948
    T90271801344-14-8
    CA-4948 (Emavusertib) is a potent IRAK4 FLT3 inhibtor. CA-4948 with anti-tumor activity.
    • $30
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  • Ginsenoside Rb1
    T282241753-43-9
    Ginsenoside Rb1 (Gypenoside Ⅲ) is part of a class of steroid glycosides; may have properties that inhibit or prevent the growth of tumors.
    • $39
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  • IRAK4-IN-26
    T79448
    IRAK4-IN-26 (Compound 21), an IRAK4 inhibitor with an IC50 of 6.2 nM, exhibits an oral bioavailability of 21%. It is utilized for the study of inflammatory and autoimmune disorders [1].
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  • IRAK inhibitor 6
    T51101042672-97-8
    IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK-4, IC50: 160 nM).
    • $48
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  • IRAK-1-4 Inhibitor I
    T2457509093-47-4
    IRAK-1-4 Inhibitor I is a dual inhibitor of IRAK4 and IRAK1.
    • $37
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  • HS-243
    T60012848249-10-5
    HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.
    • $48
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  • PROTAC IRAK4 degrader-8
    T790972911615-06-8
    PROTAC IRAK4 Degrader-8 (Compound 2) is a PROTAC designed to target IRAK4 with an IC50 of 15.5 nM [1].
    • Inquiry Price
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  • IRAK inhibitor 3
    T116701012343-93-9
    IRAK inhibitor 3 is an interleukin-1 (IL-1) receptor-associated kinase (IRAK) modulator.
    • $143
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