jaks

Oclacitinib (PF-03394197)(PF03394197) is a potent and selective JAKs inhibitor with IC50 of 10-99 nM; not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nM).

Cerdulatinib (PRT2070) is an novel oral dual Syk JAK inhibitor.

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and demonstrating a 246-fold selectivity compared to other JAKs.

Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 μM) in Cancer Cells.Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K AKT mTOR inactivation in colon adenocarcinoma cell CT26.antitumour

Ritlecitinib, also known as PF-06651600, is a potent and selective JAK3 inhibitor. PF-06651600 is a potent and low clearance compound with demonstrated in vivo efficacy. The favorable efficacy and safety profile of this JAK3-specific inhibitor PF-06651600 led to its evaluation in several human clinical studies. JAK3 was among the first of the JAKs targeted for therapeutic intervention due to the strong validation provided by human SCID patients displaying JAK3 deficiencies.

Tofacitinib maleate, also known as tasocitinib, CP-690550, is a Janus kinase (JAK) inhibitor. Tofacitinib maleate modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1 JAK3, JAK1 JAK2, JAK1 TyK2, JAK2 JAK2). Tofacitinib maleate inhibited the in vitro activities of JAK1 JAK2, JAK1 JAK3, and JAK2 JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively.

Tofacitinib HCl, also known as tasocitinib, CP-690550, is a Janus kinase (JAK) inhibitor. Tofacitinib HCl modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1 JAK3, JAK1 JAK2, JAK1 TyK2, JAK2 JAK2). Tofacitinib HCl inhibited the in vitro activities of JAK1 JAK2, JAK1 JAK3, and JAK2 JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively.

JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM for TYK2, 7.7 nM for JAK1, and 629.6 nM for JAK3. Moreover, JAK-IN-27 impedes IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells with an IC50 of 23.7 nM [1].

JAK-IN-30 (compound 31) is a water-soluble Janus kinase (JAK) inhibitor with IC50 values of 2 nM for JAK2, 15 nM for JAK1, 18 nM for JAK3, and 2 nM for TYK2, identified for its research potential in treating dry eye disease (DED) [1].

JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3, and 1.95 nM for TYK2. It effectively reduces joint swelling while maintaining a good safety profile [1].