JAK IN 3

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.

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].

JAK HDAC-IN-3 (13a), a dual inhibitor of JAK and HDAC, exhibits IC50 values of 25.36 nM for JAK2, 0.2 μM for HDAC, and 0.43 μM for HDAC1, respectively [1].

JAK3-IN-7 is a potent and selective JAK3 inhibitor (IC50<0.01 μM) intended for the treatment of organ transplantation rejection, graft-versus-host reaction post-transplantation, autoimmune disorders, allergic diseases, and chronic myeloproliferative disorders.

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].

JAK3 BTk-in-2 is a potent JAK3 BTK inhibitor. JAK3 BTk-in-2 inhibits both BTK and JAK3, which are two important targets IN autoimmune diseases. JAK3 BTk-in-2 simultaneously inhibits the BTK JAK3 signaling pathway, showing a synergistic effect. JAK3 BTk-in-2 has the potential to treat diseases associated with abnormal JAK3 and BTK activity.

JAK3 BTk-in-1 is a dual JAK3 BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3 BTk-in-1 simultaneously inhibited the BTK JAK3 signaling pathway, showing a synergistic effect. JAK3 BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays. WHI-P97 effectively inhibited the in vitro invasiveness of EGFR-positive human cancer cells in a concentration-dependent manner.

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.

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

DualCathepsinL JAK-IN-1 (Compound A8) serves as a dual inhibitor of Cathepsin L (CTSL) and JAK, exhibiting IC50 values of 0.68 μM for CTSL and 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for JAK1 2 3 and TYK2, respectively. This compound effectively prevents the activation of MAPK, NF-κB, and JAK STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. DualCathepsinL JAK-IN-1 is applicable in research on acute lung injury (ALI).

Ifidancitinib (ATI-50002) is a specific JAK kinase 1 3 inhibitor that induces hair growth in AA-affected C3H HeJ mice.Ifidancitinib can be used to study autoimmune diseases.

JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM

WP-1034 is a novel Jak-Stat inhibitor, which is active against AML blasts. WP-1034 effectively inhibited proliferation of OCIM2 cells and fresh AML samples. WP-1034 caused cell cycle arrest of OCIM2 cells in sub-Go phase. WP-1034 induced apoptosis of OCIM2 cells and that induction of apoptosis involved cleavage of caspase 3 and the DNA repair enzyme poly (adenosine diphosphate [ADP]-ribose) polymerase (PARP).

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.

JAK-IN-29 (Compound 3) is a potent inhibitor of Janus kinases (JAK) [1].

JAK-IN-33 (Compound 3 (R)) is a selective inhibitor of the Janus kinase (JAK) family [1].

Upadacitinib-15N-d2 the 15N and deuterated compound of Upadacitinib. Upadacitinib has a CAS number of 1310726-60-3. Upadacitinib (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.

Agrimonolide, a compound derived from isocoumarins and found mainly in the herb Agrimonia pilosa Ledeb, has significant biological activity. agrimonolide exerts anti-inflammatory effects by inhibiting lipopolysaccharide (LPS)-induced activation of JAK-STATs and p38 MAPKs signaling pathways. Agrimonolide and its derivative, desmethyl agonolide, have been shown to be effective in increasing insulin-mediated glycogen levels in hepatocytes and may play a key role in regulating insulin-resistant HepG2 cells. agrimonolide exhibits inhibitory effects on cancer progression and induction of cell death and apoptosis by targeting SCD1 in ovarian cancer cells. In particular, Agrimonolide exhibited a dose-dependent inhibition of proliferation, migration and invasion of A2780 and SKOV-3 cells, while promoting apoptosis. The compound was also found to induce iron-mediated cell death while increasing reactive oxygen species (ROS) and total iron levels.Agrimonolide readily crosses the blood-brain barrier, suggesting its potential for therapeutic applications in neurological disorders.