jak in 4

JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model.

JAK1 TYK2-IN-4 serves as a dual inhibitor targeting both JAK and TYK2, displaying IC50 values of 39 nM and 21 nM, respectively. It is also orally bioavailable [1].

JAK2-IN-4 is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.

JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).

HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4. This compound not only inhibits cell proliferation but also induces apoptosis in MDA-MB-231 cells and demonstrates in vivo anticancer efficacy [1].

JAK3 BTK-IN-4 is a potent inhibitor of JAK3 BTK, targeting critical pathways in autoimmune diseases. The simultaneous inhibition of the BTK JAK3 signaling pathway exerts a synergistic effect, making JAK3 BTK-IN-4 a promising therapeutic candidate for JAK3 kinase and or BTK-related diseases.

WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays. WHI-P97 effectively inhibited the in vitro invasiveness of EGFR-positive human cancer cells in a concentration-dependent manner.

Gusacitinib, also known as ASN-002 and EN-3351, is a potent dual inhibitor of SYK/JAK kinases. ASN002 showed strong antitumor activity in both hematological and solid tumor xenograft models. ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways as measured in pLAT and pSTAT assays, respectively. When profiled in a panel of 178 cell lines, ASN002 showed strong anti-proliferative activity in many lymphoid/leukemia cell lines, including SU-DHL-6, SU-DHL-4, OCI-LY10, H929 and Pfeiffer.

JAK HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1 2 and HDAC3 6 at nanomolar concentrations. This compound exhibits proapoptotic properties, inhibits histone deacetylation, and impedes STAT3 phosphorylation, demonstrating notable antiproliferative activity against various hematological malignancies and solid tumors [1].

JAK-IN-24, a JAK inhibitor, exhibits IC50 values of 0.534 nM and 24 nM in the presence of 4 μM and 1 mM ATP, respectively. Additionally, it effectively inhibits STAT5 phosphorylation induced by PBMC IL-15 with an IC50 of 86.171 nM.