Interleukin-1 receptor-associated kinase (IRAK) is first described as a signal transducer for the proinflammatory cytokine IL-1 and is later implicated in signal transduction of other members of the Toll-like receptor (TLR)/IL-1R family. Four different IRAK-like molecules have been identified: two active kinases, IRAK-1 and IRAK-4, and two inactive kinases, IRAK-2 and IRAK-M. All IRAKs mediate activation of NF-κB and MAPK pathways. IRAKs are protein kinases involved in signalling innate immune responses from TLRs. After TLR-4 and TLR-2 recognize pathogen-associated molecular patterns, such as LPS and peptidoglycan, all IRAK members form multimeric receptor complexes. IRAKs are essential signaling intermediates in the TLR/IL-1R pathway to both IKK and MAPKs activation. These two pathways are central to the activation of several transcription factors, including NF-κB and AP-1, which contribute to the establishment of an immune response.


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JAK/STAT Signaling >
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NF-κB >
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Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
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Vitamin D Related >
VD/VDR
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ND2158

ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM;ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1.ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models.IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway.In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199.

  • CAS Number: 1388896-07-8
  • MF: C22H30N4O4S
  • MW: 446.566
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AS 2444697

A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1; inhibited IL-1β- or TLR ligand lipopolysaccharide (LPS)-induced IL-6 production in human lung alveolar epithelial cells, fibroblast-like synoviocytes, and peripheral blood mononuclear cells; significantly reduces urinary protein excretion and preventd the development of glomerulosclerosis and interstitial fibrosis without affecting the blood pressure in mice model of chronic kidney disease.

  • CAS Number: 1287665-60-4
  • MF: C19H21ClN6O4
  • MW: 432.861
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Larotinib mesylate hydrate

Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM[1].

  • CAS Number: 2097129-93-4
  • MF: C26H36ClFN4O11S2
  • MW: 699.17
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ginsenoside Rb1

Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .

  • CAS Number: 41753-43-9
  • MF: C54H92O23
  • MW: 1109.295
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 1145.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 646.8±34.3 °C

Emavusertib hydrochloride

Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity[1][2][3].

  • CAS Number: 2376399-42-5
  • MF: C24H26ClN7O5
  • MW: 527.96
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK4-IN-21

IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].

  • CAS Number: 2170694-04-7
  • MF: C28H28FN7O2
  • MW: 513.57
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-8

PROTAC IRAK4 degrader-8 (compound 2) is a PROTAC targeting to IRAK4 (IC50=15.5 nM)[1].

  • CAS Number: 2911615-06-8
  • MF: C43H50ClF2N11O5
  • MW: 874.38
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK4-IN-22

IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].

  • CAS Number: 2170694-05-8
  • MF: C28H28FN7O2
  • MW: 513.57
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-5

PROTAC IRAK4 degrader-5 is a PROTAC-based IRAK4 degrader extracted from patent US20190192668A1, compound I-171[1].

  • CAS Number: 2360530-61-4
  • MF: C41H40F3N11O9
  • MW: 887.82
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK inhibitor 1

IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.

  • CAS Number: 1042224-63-4
  • MF: C17H19N5
  • MW: 293.36600
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK-1-4 Inhibitor I

IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.

  • CAS Number: 509093-47-4
  • MF: C20H21N5O4
  • MW: 395.41200
  • Catalog: IRAK
  • Density: 1.4
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-1

PROTAC IRAK4 degrader-1 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively[1].

  • CAS Number: 2360533-90-8
  • MF: C44H39F3N12O7
  • MW: 904.85
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HG-12-6

HG-12-6 is a small-molecule inhibitor that bind preferentially to unphosphorylated IRAK4 with IC50 of 165.1 nM, displays 15-fold selectivity over phosphorylated IRAK4 (IC50=2876 nM); binds as type II inhibitor with IRAK4 in a “DFG-out” conformation.

  • CAS Number: 2222354-57-4
  • MF: C29H27F3N6O2S
  • MW: 580.63
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HS-243

HS-243 (HS243) is a highly potent, super-selective IRAK-1/4 inhibitor with IC50 of 24/20 nM, respectively.HS-243 shows exquisite potency toward IRAK-1/4 over all other human kinases with only minimal TAK1-inhibiting activity (IC50=0.5 uM).HS-243 binds in the ATP-binding pocket of IRAK-4.HS-243 potently reduces the proinflammatory response of RA cells and macrophages, has distinct cytokine profile from TAK1.HS-243 reduces percentage of survival in pancreatic and breast cancer cell lines.

  • CAS Number: 848249-10-5
  • MF: C17H16N4O3
  • MW: 324.34
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK inhibitor 3

IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.

  • CAS Number: 1012343-93-9
  • MF: C21H21N5O4S
  • MW: 439.48800
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK inhibitor 6

IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4) with IC50 of 160 nM.

  • CAS Number: 1042672-97-8
  • MF: C20H20N4O3S
  • MW: 396.463
  • Catalog: IRAK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-7

PROTAC IRAK4 degrader-7 (Compound I-417) is an orally active PROTAC IRAK4 degrader with antitumor activities[1].

  • CAS Number: 2432994-31-3
  • MF: C44H49F2N11O6
  • MW: 865.93
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK4-IN-13

IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg[1].

  • CAS Number: 2667681-57-2
  • MF: C24H27N9O
  • MW: 457.53
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-2256

GNE-2256 (GNE2256) is a potent, selective inhibitor of IRAK4 with biochemical Ki of 1.4 nM.GNE-2256 displays high selectivity in the CEREP panel with off-targets with >50% inhibition are TACR1, HTR2B and ACHE.GNE-2256 is potent in the NanoBRET assay (IC50 = 3.3 nM), the IL-6 human whole blood assay (IC50=190 nM) and the IFNα human whole blood assay (IC50=290 nM).

  • CAS Number: 2102170-43-2
  • MF: C24H27FN6O4
  • MW: 482.516
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-2

PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs[1].

  • CAS Number: 2374122-27-5
  • MF: C57H68FN11O8S
  • MW: 1086.28
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK4-IN-17

IRAK4-IN-17 (Compound 5) is a potent IRAK4 inhibitor with the IC50 of 1.3 nM[1]. IRAK4-IN-17 can be used in large B-cell lymphoma (DLBCL) research[1].

  • CAS Number: 2183503-33-3
  • MF: C17H20F2N8O
  • MW: 390.39
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-4

PROTAC IRAK4 degrader-4 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127[1].

  • CAS Number: 2360528-45-4
  • MF: C41H38F3N11O10
  • MW: 901.80
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK4-IN-16

IRAK4-IN-16 (compound 4) is a potent IRAK4 (interleukin-1 receptor associated kinase 4) inhibitor, with an IC50 of 2.5 nM. IRAK4-IN-16 shows cytotoxicity activity against OCI-LY10, TMD8, Ramos and HT cells, with IC50 values of 0.2, 0.2, 0.6, and 2.7 μM, respectively[1].

  • CAS Number: 1812188-83-2
  • MF: C17H20F2N8O
  • MW: 390.39
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK inhibitor 4

IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.

  • CAS Number: 1012104-68-5
  • MF: C33H35F3N6O3
  • MW: 620.66500
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KTX-951

KTX-951 is an IRAK4 degrader (DC50=18 nM). KTX-951 (10 mg/kg) shows the oral bioavailability (F%) of 22% in a rat model. KTX-951 has good anticancer potential[1].

  • CAS Number: 2573298-36-7
  • MF: C46H52F2N8O6
  • MW: 850.95
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KTX-497

KTX-497 is an orally active IRAK4 degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology[1].

  • CAS Number: 2432993-46-7
  • MF: C45H49F3N8O6
  • MW: 854.92
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Zabedosertib

Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors[1].

  • CAS Number: 1931994-81-8
  • MF: C20H21F3N4O4S
  • MW: 470.47
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: 620.7±55.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

KTX-955

KTX-955 is a potent IRAK4 degrader with DC50 values of 5 nM and 130 nM for IRAK4 and Ikaros, respectively. KTX-955 can be used to research anticancer[1][2].

  • CAS Number: 2573302-50-6
  • MF: C46H51F3N8O7
  • MW: 884.94
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CA-4948

CA-4948 is a selective and potent IRAK4 inhibitor.

  • CAS Number: 1801343-74-7
  • MF: C21H19N7O3
  • MW: 417.42
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRAK4-IN-4

IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM[1].

  • CAS Number: 1850276-58-2
  • MF: C22H16N2O2
  • MW: 340.37
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A