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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.

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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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).
  • $30
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Edecesertib
T624732408839-73-4
Edecesertib (GS-5718) is a selective, orally active IRAK-4 inhibitor with anti-inflammatory properties, applicable for the study of rheumatoid arthritis (RA) and lupus erythematosus (LE).
  • $699
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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.
  • $30
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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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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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IRAK-1-4 Inhibitor I
T2457509093-47-4
IRAK-1-4 Inhibitor I is a dual inhibitor targeting IRAK1 and IRAK4.
  • $37
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TargetMol | Inhibitor Sale
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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PROTAC IRAK4 degrader-1
T138422360533-90-8
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.
  • $471
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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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TargetMol | Inhibitor Sale
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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TargetMol | Inhibitor Sale
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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JH-X-119-01
T92032227368-54-7
JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK-1 (Interleukin-1 Receptor-Associated Kinase 1).
  • $60
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TargetMol | Inhibitor Sale
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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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.
  • $56
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GLPG2534
T751132095615-97-5In house
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 inhibitor 3
T116701012343-93-9
IRAK inhibitor 3 is a modulator of interleukin-1 (IL-1) receptor-associated kinase (IRAK).
  • $143
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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.
  • $58
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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.
  • $34
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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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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).
  • $89
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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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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-4 protein kinase inhibitor 2
T9631301675-24-1
IRAK-4 protein kinase inhibitor 2 is a potent inhibitor of interleukin-1 receptor-associated kinase-4 (IC50 = 4 μM).
  • $37
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