| Cat. No. |
Product Name |
CAS No. |
Information |
| H9361 |
Copanlisib
|
1032568-63-0 |
BAY-1830839 is a potent and selective IRAK4 inhibitor with IC50 values of 3 nM respectively. |
| H9360 |
BAY 1834845
|
1931994-80-7 |
BAY 1834845 is a potent and selective IRAK4 inhibitor with IC50 values of 3.4 nM respectively. |
| H9126 |
BMS986126
|
1610017-20-3 |
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;demonstrates equipotent activity against multiple MyD88-dependent responses both in vitro and in vivo; inhibits cytokine production induced by injection of several different TLR agonists, also significantly suppresses skin inflammation induced by imiquimod; demonstrates synergy with prednisolone in assays of TLR7- and TLR9-induced IFN target gene expression using human PBMCs. |
| H8507 |
CA-4948
|
1801344-14-8 |
CA-4948(Emavusertib) is a potent IRAK4/FLT3 inhibtor with anti-tumor activity;CA-4948 is over 500-fold more selective for IRAK-4 compared to IRAK-1. CA-4948 reduces TNF-α, IL-1β, IL-6 and IL-8 release from TLR-Stimulated THP-1 Cells with an IC50 <250 nM. CA-4948 also has antiproliferative activity due to inhibition of receptor-type tyrosine-protein kinase FLT3. |
| H4011 |
Thymoquinone
|
490-91-5 |
An anticancer phytochemical commonly found in black cumin; exhibits anticancer activity via numerous mechanisms of action, specifically by showing selective antioxidant and oxidant activity; directly suppresses IRAK1, strongly inhibits the production of nitric oxide (NO) and repressed NO synthase (iNOS),TNF-α, COX-2, IL-6, and IL-1β expression in LPS-activated RAW264.7 cells; significantly ameliorates disease symptoms in LPS/D-GalN-induced hepatitis and EtOH/HCl-induced gastritis mouse models. |
| H4009 |
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. |
| H4008 |
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. |
| H4007 |
PF-05388169
|
1604034-78-7 |
A potent, selective IRAK4 inhibitor with IC50 of 0.094 nM, >500-fold selectivity over IRAK1 (IC50=65 nM); exhibits low nM potency in LPS- and R848-induced cytokine assays (IC50=85 nM) in human PBMCs; inhibits LPS-induced TNFα in an in vivo murine model. |
| H4006 |
PF-05387252
|
1604034-71-0 |
A potent, selective IRAK4 inhibitor with IC50 of 1.3 nM, 200-fold selectivity over IRAK1 (IC50=290 nM); exhibits low nM potency in LPS- and R848-induced cytokine assays (IC50=18 nM) in human PBMCs; inhibits LPS-induced TNFα in an in vivo murine model. |
| H4005 |
AZ1495
|
2196204-23-4 |
A novel potent, selective IRAK4 inhibitor with IC50 of 51 nM; demonstrates inhibition of NF-κB activation and growth of the ABC subtype of DLBCL cell lines in vitro in combination with ibrutinib; shows tumor regression against mutant MYD88L265P DLBCL. |
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