JAK

CEE321 is an effective pan-JAK inhibitor with an IC50 of 54 nM. It effectively inhibits biomarkers associated with atopic dermatitis.

(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib is a JAK3 inhibitor(IC50 : 1 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].

JAK1-IN-9 (compound 23a) is a potent, selective inhibitor of JAK1, demonstrating an IC50 of 72 nM.

JAK2-IN-11 is a JAK2 kinase inhibitor with potent antitumor activity, exhibiting an IC50 of ≤10 nM against JH2 BIND WT/V617F. This compound effectively suppresses tumor growth.

Ten01 exhibits a 5.0 nM inhibition of JAK1 kinase.

"JAK-IN-23: oral dual JAK/STAT & NF-κB inhibitor; JAK1 (IC50: 8.9 nM), JAK2 (15 nM), JAK3 (46.2 nM); for IBD research."

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-11: potent oral JAK3 inhibitor (IC50=1.7 nM), noncytotoxic, >588-fold selectivity, blocks T-cell growth; useful in autoimmune research.

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

Cenacitinib is an effective inhibitor of Janus kinase (Janus kinase) and possesses anti-inflammatory activity.

JAK-IN-19 inhibits JAK (pIC50: 7.2, 7.7), less so for VEGFR2 (7.0) and Aurora B (5.8).

iBFAR2, an inhibitor of BFAR, restores the CD8+ tumor-resident memory T cell subset against solid tumors. It promotes the binding of JAK2-STAT1 and enhances the phosphorylation of STAT1.

TYK2ligand 2 is the TYK2 ligand of PROTACTYD-68. TYD-68 is a highly potent and selective CRBN-recruiting TYK2 PROTAC degrader with a DC50 value of 0.42 nM.

YLIU-4-105-1 is a type II JAK2 inhibitor. Demonstrating in vivo pharmacological activity, YLIU-4-105-1 reduces splenic weight, decreases blood reticulocyte counts in a dose-dependent manner, and inhibits pSTAT5.

JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.