jak2/jak3

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.

Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9/5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

Itacitinib (INCB039110) is an orally bioavailable Janus-associated kinase 1 (JAK1) inhibitor with potential antineoplastic activity.

Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3/2/1 (IC50=1/20/112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.

Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

TG-89 is an inhibitor of JAK2, JAK3, RET and FLT3, and has an IC50 value of 11.2 μM against JAK2, showing anticancer activity in the treatment of ovarian and cervical cancer.

TG-46 (TG46) inhibits JAK2, FLT3, RET, JAK3 and can be used to study glaucoma.

JAK3i is a selective covalent inhibitor of JAK3 kinase. JAK3i reveals two distinct temporal waves of STAT5 phosphorylation and more potently targets the second wave, which is required for cell cycle progression and T cell proliferation.

Izencitinib (JNJ-8398) is an orally active and gut-selective JAK inhibitor with potential anti-inflammatory activity for the study of ulcerative colitis and Crohn;s disease.

NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.

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].

Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).

Ruxolitinib phosphate (INCB18424 phosphate) is a JAK1/2 inhibitor with IC50 of 3.3 nM/2.8 nM. Its selectivity for JAK1/2 is more than 130 times that of JAK3.

Ilginatinib maleate (NS-018 maleate) is a highly active, orally bioavailable inhibitor of JAK2.

Golidocitinib (AZD4205) is a selective JAK1 inhibitor with an IC50 of 73 nM, while it weakly inhibits JAK2 and JAK3 with IC50 values greater than 14.7 μM and 30 μM, respectively.

JAK-IN-1 shows improved selectivity for JAK3 over JAK1. JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively.

JAK-IN-3 is a potent JAK inhibitor that inhibits JAK3, JAK1, TYK2, and JAK2, and can be used for the study of immune system disorders.

Flonoltinib (JAK2/FLT3-IN-1) is an orally active and potent JAK2/FLT3 inhibitor, inhibiting JAK2, FLT3, JAK1, and JAK3. Flonoltinib has anti-cancer activity and can be used for studying myeloproliferative neoplasms.

Ilginatinib (NS-018) is a highly active, orally bioavailable JAK2 inhibitor.

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor.

Brepocitinib P-Tosylate (PF-06700841 P-Tosylate) is a potent dual inhibitor of Janus kinase 1 (JAK1) and TYK2 (IC50s of 17 nM and 23 nM, respectively).