IRAK

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.

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

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

IRAK-IN-6, also known as IRAK inhibitor 6, is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor. IRAK-4 is reported to be essential for the activation of the intracellular signalling cascades including NF-kB and MAPK pathways, which are critical for the production of inflammatory cytokines.

JNK-IN-7 is a relatively selective JNKs inhibitor(IC50= 1.54/1.99/0.75 for JNK1/2/3); also bound to IRAK1, PIK3C3, PIP5K3 and PIP4K2C.

2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.

CA-4948 is a potent, and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. CA-4948 exhibited the greatest efficacy in four of the five ABC-DLBCL PDX models tested as compared to GBC-DLBCL and ABC/GCB DLBCL PDX models.

AS-2444697 is a potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with IC50 value of 21 nM.

PF-06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4).

AZ1495 (compound 28) 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.

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

HS-243 is an inhibitor of transforming growth factor-?beta kinase. HS-243 can be used in treatment of cancer, malaria, inflammatory and other TAK1-?mediated diseases.

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.

Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation.