jak-2

JAK-2/3-IN-1 is a highly effective inhibitor targeting both JAK-2 and JAK-3 isoforms, exhibiting remarkable potency with Ki values below 250 nM for both isoforms.

JAK-2-/3-IN-3 (compound ST4j) is a potent inhibitor of JAK2/3, with IC50 values of 13.00 and 14.86 nM for JAK2 and JAK3, respectively. It inhibits JAK2 autophosphorylation, induces apoptosis in a time- and dose-dependent manner, and can be used in lymph-derived diseases and leukemia research [1].

JAK-2/3-IN-2 (Compound 3h) is a potent dual inhibitor of JAK2 and JAK3, exhibiting inhibitory activity with IC50 values of 23.85 nM and 18.9 nM against JAK2 and JAK3, respectively [1].

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.

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.

Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).

CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.

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.

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.

FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).

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.

Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling. Icaritin at low concentration (4 or 8 μMol/L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.

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

JAK2 inhibitor G5-7 (JAK2 inhibitor G5-7) is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 has the potential for glioma study

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.

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.

Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046), a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.

Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens that exhibits immunoregulatory, anti-inflammatory, anti-viral, and anti-cancer activity. Ponicidin induces apoptosis of gastric carcinoma cells, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on the protein levels of JAK2 and STAT3.