jak-1-in-4

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).

PTPN2/1-IN-4 (Compound WS35) is an orally active dual inhibitor of PTPN1 and PTPN2, with IC50 values of 12.8 nM and 5.8 nM, respectively. It modulates the IFNγ-JAK-STAT signaling pathway and significantly enhances CD8+ T cell tumor infiltration. PTPN2/1-IN-4 demonstrates potent anticancer activity, effectively inhibiting tumor growth in the B16-OVA syngeneic mouse model both as a monotherapy and in combination with anti-PD-1 antibody treatment.

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.

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].

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].