A novel potent, selective IRAK4 inhibitor with IC50 of 51 nM.

CA4948-Analog is an analog of Emavusertib. It has similar property to CA-4948, which is a potent, and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. It was reported in patent WO 2015104688. Emavusertib, also known as CA-4948 i

Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor is a benzimidazole compound that acts as a cell-permeable, potent selective inhibitor of IL-1 kinases.

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

IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor .

IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.

PF-06426779 (PF06426779) is a potent, selective IRAK4 inhibitor with IC50 of 1 nM against full-length IRAK4 kinase and cell-based IC50 of 12 nM.

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.

BMS-986126 is a potent, highly selective inhibitor of IRAK4 kinase with IC50 of 5.3 nM, displays >100-fold selective for IRAK4 over a panel of 214 kinases.

JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice.

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

HS271 is a highly potent, orally active and selective IRAK4, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.

IRAK-4 protein kinase inhibitor 2 (compound 1) is a potent inhibitor of interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4), with an IC50 of 4 μM. IRAK-4 protein kinase inhibitor 2 can be used for the research of inflammatory and immune-related conditions or disorders.

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

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.

IRAK4-IN-8 (VI-177) is a potent IRAK4 inhibitor.

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).

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.

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.

THZ-2-118 is a potent selective inhibitor of IRAK1 with IC50 of 14.2 nM; THZ-2-118 does not inhibitor IRAK4 at 10 uM, also potently inhibits JNK1/2/3 (IC50=1-2 nM).

Edecesertib (GS-5718) is a selective, potent, orally active IRAK-4 inhibitor. Edecesertib has anti-inflammatory activity. Edecesertib can be used for rheumatoid arthritis (RA) and lupus erythematosus (LE) research.

KTX-497 is a IRAK4 degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology.

KTX-612 is an orally active IRAK4 degrader with a DC50 value of 7 nM. KTX-612 can be used for the research of oncology.

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model.

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.

KME-2780 (KME2780) is a potent and selective dual IRAK1 and IRAK4 (IRAK1/4) inhibitor with IC50 of 19 and 0.5 nM, respectively.

KME-3859 is a potent, selective IRAK4 inhibitor with IC50 of 5 nM, 100-fold selective over IRAK1.