JAK

JAK2-IN-14 is a highly selective JAK2 inhibitor with an IC50 of 2 nM, demonstrating significant selectivity with 89.5-fold over JAK1, 80.5-fold over JAK3, and 51-fold over TYK2. This compound effectively inhibits the STAT5 signaling pathway, leading to tumor cell cycle arrest and apoptosis. JAK2-IN-14 is a valuable tool for investigating myeloproliferative neoplasms (MPNs) and their underlying mechanisms.

NSC114792 is a selective inhibitor of Janus kinase 3 (JAK3), which plays a critical role in immune signaling pathways. This compound effectively induces apoptosis in target cells and significantly reduces the protein expression of phosphorylated JAK3 and phosphorylated STAT5. NSC114792 is primarily utilized in research focused on immune responses and related signaling cascades.

Tubulosine is an alkaloid that functions as a selective inhibitor of the Janus kinase 3 (JAK3) with an IC50 of 9.9 nM. It exhibits enhanced inhibition of JAK3 compared to other JAK family members, with IC50 values of 69.5 nM for JAK1, 84.9 nM for JAK2, and 76.3 nM for TYK2. Tubulosine induces both apoptotic and necrotic/autophagic cell death in cancer cells and disrupts peptide chain elongation in eukaryotic polysomes. This compound demonstrates promising anticancer activity, particularly in breast cancer cell lines, making it a valuable tool for cancer research.

DPP is a Platinum(IV) complex featuring a pterostilbene-derived axial ligand that specifically targets the JAK2/STAT3 signaling pathway. This compound displays significant antiproliferative activity against breast cancer cells by inducing apoptosis through the activation of caspase-3 and cleavage of poly ADP-ribose polymerase. Additionally, DPP enhances the maturation and antigen presentation capability of dendritic cells, demonstrating favorable safety profiles in in vivo studies, making it a promising candidate for cancer immunotherapy research.

JAK2/FLT3-IN-3 is a potent dual inhibitor of FLT3 and JAK2, exhibiting IC50 values of 2.01 nM for JAK2, 0.51 nM for FLT3, and 104.40 nM for JAK3. This compound induces apoptosis in cancer cells and demonstrates significant antitumor activity. Its ability to inhibit both FLT3 and JAK2 pathways makes it a valuable tool for research related to hematological malignancies and targeted cancer therapies.

Cernuumolide J is a selective inhibitor of JAK2/STAT3 signaling pathway. It induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, while promoting the phosphorylation of JNK and p38 MAPK. Cernuumolide J exhibits a concentration-dependent growth inhibition of HEL leukemia cells, with an IC50 value of 1.79 μM, making it a valuable compound for research in anti-cancer therapy.

JAK3 covalent inhibitor-2 is a selective covalent inhibitor targeting Janus kinase 3 (JAK3), exhibiting an IC50 of 7.2 nM. This compound demonstrates anti-inflammatory activity, low toxicity, and favorable bioavailability, making it suitable for research applications involving autoimmune diseases and inflammatory disorders. Its specificity for JAK3 supports investigations into therapeutic strategies aimed at modulating immune responses.

Flonoltinib sulfate is a potent, orally active dual inhibitor targeting JAK2 and FLT3. It demonstrates significant biological activity with IC50 values of 0.7 nM for JAK2 and 4 nM for FLT3, along with activity against JAK1 and JAK3 at 26 nM and 39 nM, respectively. This compound is primarily utilized in cancer research, particularly in the study of hematological malignancies influenced by aberrant JAK2 and FLT3 signaling pathways.

Ivarmacitinib sulfate is a selective inhibitor of the Janus kinase 1 (JAK1) pathway, exhibiting a significant preference over JAK2, JAK3, and Tyk2. This compound effectively inhibits JAK1-STAT3 phosphorylation, leading to the apoptosis of hepatic stellate cells. Ivarmacitinib sulfate demonstrates notable anti-proliferative and anti-inflammatory properties, making it a valuable tool for research on hepatic diseases and inflammation-related disorders.

AT9283 lactic acid is a multi-targeted kinase inhibitor primarily targeting Aurora A/B and JAK2/3. It demonstrates potent biological activity against various cancers, exhibiting IC50 values between 1 to 30 nM for its targets. AT9283 lactic acid effectively inhibits the growth and survival of multiple solid tumors in both in vitro and in vivo models, making it a valuable reagent for cancer research applications.

JAK-2/3-IN-3 is a potent inhibitor of JAK2 and JAK3, demonstrating IC50 values of 13.00 nM and 14.86 nM, respectively. It effectively inhibits the autophosphorylation of JAK2 and promotes apoptosis in a dose- and time-dependent manner. This compound is valuable for research into lymphoid malignancies and leukemia, providing insights into the role of JAK signaling pathways in these diseases.

Fedratinib hydrochloride hydrate is a selective, ATP-competitive inhibitor targeting the JAK2 kinase. With an IC50 of 3 nM for both JAK2 and the mutant JAK2V617F, it demonstrates significant potency. This compound exhibits 35-fold selectivity over JAK1 and 334-fold selectivity over JAK3. Fedratinib hydrochloride hydrate effectively induces apoptosis in cancer cells, making it a valuable tool for research in myeloproliferative disorders.

Brevilin A is a potent inhibitor of the STAT3/JAK signaling pathway, with an IC50 value of approximately 10.6 μM for STAT3. It exhibits anti-tumor properties and effectively inhibits the proliferation of cancer cells. Additionally, Brevilin A has been shown to induce both apoptosis and autophagy, making it a valuable tool for cancer research and therapeutic investigations.

Phenylpyropene C is a JAK/STAT pathway inhibitor known to effectively inhibit interferon-gamma (IFN-γ) mediated expression of reporter genes, with an IC50 range of 5.4 to 10.8 μM. Additionally, it serves as an inhibitor of acyl-CoA, exhibiting an IC50 of 16.0 μM. This compound is valuable for research applications focusing on the modulation of immune responses and the exploration of cytokine signaling pathways.

Plodicitinib is an inhibitor of Janus tyrosine kinase 3 (JAK3) and TEC family kinases. This compound exhibits significant anti-inflammatory activity, making it valuable for research in inflammation-related disorders. It is applicable in studies exploring the modulation of immune responses and potential therapeutic interventions in autoimmune diseases.

NUAK1-IN-3 is a selective inhibitor of NUAK1 with a high potency, exhibiting an IC50 of 0.49 nM. It also demonstrates inhibitory activity against NUAK2 and JAK3 with IC50 values of 265 nM and 225 nM, respectively. This compound disrupts the NUAK1-MYPT1 signaling pathway, leading to reduced MYPT1 phosphorylation and inhibition of proliferation, migration, and invasion in triple-negative breast cancer cells. Additionally, NUAK1-IN-3 counteracts TGF-β1-induced epithelial-mesenchymal transition effects by modulating critical markers such as Snail, N-cadherin, and E-cadherin. It holds potential for exploring therapeutic strategies for triple-negative breast cancer.

YYSW001 is a selective Janus kinase 1 (JAK1) inhibitor with an IC50 of 6 nM, demonstrating significant efficacy in blocking JAK1-mediated phosphorylation of STAT6 as well as IL-6-induced phosphorylation of STAT3. This compound effectively suppresses pro-inflammatory cytokine levels, reduces paw swelling, and lowers clinical arthritis scores, thereby alleviating joint damage and diminishing bone loss. YYSW001 is particularly valuable for research related to rheumatoid arthritis and inflammation-related disorders.

JAK3-IN-20 is a selective and orally active JAK3 inhibitor, demonstrating an IC50 of 0.7473 nM. By covalently binding to JAK3 Cys909 and outcompeting ATP at the catalytic site, JAK3-IN-20 effectively blocks JAK-STAT pathway activation. This compound exhibits anti-tumor properties by inhibiting migration, proliferation, and growth of Bortezomib-resistant cancer cells, as well as inducing dose-dependent apoptosis. JAK3-IN-20 is a valuable tool for researching Bortezomib-resistant multiple myeloma.

oJak-989 is a selective inhibitor of Janus kinase 1 (JAK1), demonstrating a Ki of 2.8 nM for JAK1, 110 nM for JAK3, and 31 nM for TYK2. This compound is particularly relevant in the study of inflammatory diseases, as it may help elucidate the role of JAK1 in various pathological conditions and facilitate the development of targeted therapeutics. Research applications include investigating JAK1-mediated signaling pathways and the potential therapeutic impact on autoimmune disorders.