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

JAK-IN-39 (compound 11) is a JAK inhibitor with IC50 values of 0.05 nM for JAK1, 1.18 nM for JAK2, and 0.03 nM for JAK3. It reduces cell viability in TF-1 cells and inhibits the production of TNFα and INFγ in lymphocytes in vitro.

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-31 (Example 75), a JAK inhibitor, demonstrates IC50 values of ≤0.01 µM for JAK1, ≤0.01 µM for JAK2, 0.01-0.1 µM for JAK3, and ≤0.01 µM for Tyk2, indicating potent activity across these targets. It is utilized in cancer research [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].

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.

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).

Clifutinib (Compound 9e) is an orally active, selective inhibitor of FMS-like tyrosine kinase 3 (FLT3-ITD) with an IC50 of 15.1 nM. It inhibits FLT3-ITD kinase activity and blocks downstream signaling pathways, including RAS/MAPK, PI3K/AKT, and JAK/STAT5. Clifutinib induces apoptosis in FLT3-ITD mutated acute myeloid leukemia (AML) cells and is a potential candidate for research in relapsed/refractory FLT3-ITD positive AML.

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. 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

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.