JAK

Prim-O-glucosylcimifugin (Cimifugin 7-glucoside) can inhibit the proliferation of SMC(smooth muscle cell) stimulated by TNF-alpha, increase the proportion of G0 G1 phase.

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.

1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

Kurarinone is a flavonoid extracted from the shrub Sophora flavescens, which has anti-tumor, estrogenic and anti-inflammatory activities, and also has a strong inhibitory effect on immune responses.

Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2 STAT3 with anti-cancer activity.

1. Linderalactone showed significant inhibitory effects on superoxide anion generation by human neutrophils in response to fMLP CB, values of IC5 is 8.48 μg mL.

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.

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

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.

Protosappanin A (PTA) has anti-oxidative nitrative activities on brain immune and neuroinflammation through regulation of CD14 TLR4-dependent IKK IκB NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

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

Curcumol ((-)-Curcumol), a pure monomer derived from Rhizoma Curcumaeis, exhibits antitumor activities.

Ganoderic acid B is a chemical marker in quality control of G. lucidum and related products. Ganoderic acid B-containing herbs has potential influence towards therapeutic window of trifluoperazine.Ganoderic acid B has antinociceptive effect

1. Curculigoside (Curculigoside A) can prevent bone loss , improve osteogenesis and inhibit osteoclastogenesis of hAFSCs, suggesting its potential use to regulate hAFSC osteogenic differentiation for treating bone disorders. 2. Curculigoside can promote calcium deposition and increase the levels of ALP and Runx2 in osteoblasts under oxidative stress via anti-oxidative character. 3. Curculigoside possesses potent antioxidant properties against oxidative stress insults. can protect endothelial cells against oxidative injury induced by H2O2, suggesting that this compound may constitute a promising intervention against cardiovascular disorders.

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.

Bayer-18 is an inhibitor of TYK2. It inhibits the viability of anaplastic large cell lymphoma cells, including K299, SR786, Mac1, and Mac2a, with an IC50 ranging from 2-3 µM. Additionally, Bayer-18 induces apoptosis in K299 and SR786 cells.