jak3in1

JAK3-IN-1 is an orally active, selective and potent JAK3 inhibitor that can be used to study immune system diseases.

JAK3-IN-14 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.

JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].

JAK3-IN-15 (compound 22) is a JAK3 inhibitor that reduces the secretion of p-JAK3 induced by LPS. It is utilized in research for rheumatoid arthritis.

JAK3-IN-16 (compound 6) is a covalent inhibitor of JAK3.

JAK3-IN-17 is an orally active JAK3 inhibitor with an IC50 of 14.56 nM. It demonstrates anti-inflammatory activity by inhibiting the production of IL-2 and IL-6 in a DNCB-induced mouse model of atopic dermatitis.

JAK3-IN-18 is a selective and orally active dual inhibitor targeting JAK3 and TEC, with IC50 values of 0.5391 nM and 12.40 nM, respectively. It demonstrates remarkable selectivity for AK1, AK2, and TYK2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 exhibits exceptional therapeutic efficacy in a mouse model of experimental autoimmune encephalomyelitis and is applicable for multiple sclerosis research.

JAK3-IN-12 (compound 15k) is a potent inhibitor of JAK3 (IC50: 9.5 nM) and can be used in the study of rheumatoid arthritis.

JAK3-IN-13 is a potent, selective, orally active JAK3 inhibitor with IC50 values of 4728 nM for NK1, 2039 nM for JNK2, 8 nM for JNK3, and 365 nM for Tyk2. JAK3-IN-13 also exhibits anti-tumor effects.