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Cat. No. Product Name CAS No. Information
PC-50002

CA-4948

1801343-74-7

CA-4948 (AU-4948) is a novel potent, selective, orally bioavailable IRAK4 inhibitor; shows in vivo activity in TLR4-induced cytokine release model, exhibits dose-dependent efficacy in ABC-DLBCL MYD88-L265P xenograft tumor models; a therapeutic agent for hematological cancers with dysregulated TLR/MYD88/IRAK4 signaling, induces tumor regression in an ABC-DLBCL xenograft model combined with Venetoclax.

Blood Cancer

Phase 1 Clinical

PC-45740

PF-06650833

1817626-54-2

PF-06650833 (PF06650833) is a potent and selective IRAK4 inhibitor with IC50 of 0.2 nM; has IC50 of 2 nM in the PBMC assay as well as in a human whole blood assay; shows excellent kinase selectivity in a panel of 278 kinases; significantly inhibits LPS-induced TNFα in a dose dependent manner in rats model (0.3-30 mg/kg); has favorable in vitro and in vivo ADME profiles and orally active.

Rheumatoid Arthritis

Phase 2 Clinical

PC-35595

R191

R191 (R-191) is a potent, small molecule IRAK1/4 kinase inhibitor (IRAK4 IC50=3 nM), exhibits good selectivity against a broad panel of kinases; blocks TLR- and IL-1R-induced cytokine production in primary cells with potencies below 50nM while sparing unrelated pathways with at least 20-fold window; potently inhibits expression of PD-L1, potentially promoting recognition of AML blasts by the immune system in multiple AML lines, exhibits strong synergy with Bcl2 and BCR pathway inhibitors against a number of DLBCL lines in vitro; also decreases serum IL-6 in an acute mouse model of IL-1β-induced cytokine release and blocks joint inflammation in the collagen-induce arthritis model.
PC-35553

PF-06426779

1817628-40-2 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; displays excellent selectivity against the human kinome, and >100-fold selectivity for IRAK4 over IRAK1.
PC-35135

Compound 7004

Compound 7004 (IRAK2 mimetic 7004) is a small molecule mimetic of a-helical domain of IRAK2, inhibit IL-33–induced NF-κB transcriptional activity (IC50=9.7 uM) by disrupting Myddosome formation; decreases the IRAK2-IRAK4 association, attenuates IL-33-induced and OVA-induced asthma mouse models in vivo, attenuates the proinflammatory effects in asthma-like models.
PC-43498

IRAK-1-4 Inhibitor I

509093-47-4 IRAK-1-4 Inhibitor I is a potent, dual inhibitor of IRAK4 and IRAK1 with IC50 of 0.2 uM and 0.3 uM, respectively; displays IC50 of >10 uM against a panel of 27 other kinases, including the most closely homologous (outside of the IRAK family) Lck and pp60SRC; eliminates the LPS-induced increases in Bcl10, NF-κB, and IL-8 in human intestinal epithelial cells.
PC-43455

IRAK inhibitor 2

928333-30-6 IRAK inhibitor 2 is a potent IRAK inhibitor.

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