jak1 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).

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].

IL-4 inhibitor is an inhibitor of IL-4.1It binds to IL-4 with a Kdvalue of 1.8 μM and inhibits IL-4 activity in a cell-based reporter assay (EC50= 1.81 μM). It is selective for IL-4 over IL-13 (EC50= 18.2 μM). IL-4 inhibitor inhibits IL-4-induced STAT6 phosphorylation in THP-1 monocytes (EC50= 3.1 μM), indicating inhibition of the IL-4-JAK1-STAT6 signaling pathway.

JAK1/2-IN-1 is a potent inhibitor of JAK1 and JAK2, with IC50 values of 0.4 nM and 8.1 nM, respectively. Additionally, JAK1/2-IN-1 inhibits IL-4 and IL-13, with IC50 values of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a).

LY2784544(Gandotinib (LY2784544)) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3.

JAK2/FLT3-IN-1 (TFA) is an orally active dual inhibitor of JAK2 (IC50: 0.7 nM) and FLT3 (IC50: 4 nM) that demonstrates anticancer effects, also affecting JAK1 (IC50: 26 nM) and JAK3 (IC50: 39 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].

Flonoltinib maleate is an orally effective dual JAK2/FLT3 inhibitor, with IC50 values of 0.7 nM for JAK2, 4 nM for FLT3, 26 nM for JAK1, and 39 nM for JAK3. Known as JAK2/FLT3-IN-1, it exhibits anticancer activity.

Gusacitinib-d4 (ASN-002-d4) is the deuterium-labeled form of Gusacitinib. Gusacitinib (ASN-002) is an orally effective dual kinase inhibitor targeting SYK and JAK. It exhibits IC50 values of 5, 46, 4, 11, and 8 nM for SYK, JAK1, JAK2, JAK3, and TYK2, respectively. This compound effectively and rapidly suppresses key inflammatory pathways involved in the pathogenesis of atopic dermatitis. Gusacitinib is also used in research for conditions such as chronic hand eczema and basal cell carcinoma.