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Catalog No.
Product Name
Application
Product Information
Citations
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JAK inhibitor
Baricitinib phosphate is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. -
JAK inhibitor
CYT387 sulfate salt is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. -
JAK2 inhibitor
1,2,3,4,5,6-Hexabromocyclohexane is a potent and specific inhibitor of JAK2 autophosphorylation. -
Mnk2/JAK3 inhibitor
Cercosporamide, an usnic amide, was originally identified in Cercosporidium henningsii as a host-selective phytotoxin and broad-spectrum antifungal agent and is a potent inhibitor of MAP-kinase interacting kinase-2 (Mnk2; IC50 = 11 nM), JAK3 (IC50 = 31), and Mnk1 (IC50 = 116 nM). -
JAK2/STAT3 inhibitor
Cucurbitacin I, Cucumis sativus L. has been found to suppress levels of phosphotyrosine Stat3 (signal transducer and activator of transcription 3) in v-Src-transformed NIH 3T3 cells. -
JAK1 Inhibitor
Ivarmacitinib is a potent inhibitor of the Janus kinase 1 (JAK1) enzyme with notable selectivity against JAK2, JAK3, and Tyk2. This compound effectively inhibits JAK1-STAT3 phosphorylation and promotes apoptosis in hepatic stellate cells, highlighting its potential for anti-proliferative and anti-inflammatory research applications. Ivarmacitinib is valuable for studies focused on diseases involving the JAK-STAT signaling pathway. -
AKR1C1/JAK2/STAT3/NF-κB Inhibitor
Zingiberen Newsaponin is a potent inhibitor of the AKR1C1/JAK2/STAT3 and NF-κB signaling pathways. This steroid saponin compound demonstrates significant anti-hepatocellular carcinoma (HCC) activity by promoting cancer cell apoptosis through the induction of oxidative stress, as evidenced by the upregulation of ROS and MDA levels. Additionally, Zingiberen Newsaponin mitigates cerebral ischemia-reperfusion injury by reducing pro-inflammatory cytokines and enhancing superoxide dismutase (SOD) activity, thereby protecting neuronal cells. Furthermore, it has been shown to induce platelet aggregation, broadening its application in cardiovascular research. -
JAK2 Inhibitor
G5-7 is an orally active allosteric inhibitor of Janus kinase 2 (JAK2), selectively disrupting JAK2-mediated phosphorylation and activation of epidermal growth factor receptor (EGFR) at Tyr1068 and signal transducer and activator of transcription 3 (STAT3). This compound induces cell cycle arrest and apoptosis, demonstrating significant antiangiogenic effects. G5-7 shows promise for research applications in glioma studies, making it a valuable tool for understanding JAK2-related signaling pathways and their implications in cancer. -
JAK2 Inhibitor
JAK2-IN-7 is a selective inhibitor of JAK2, demonstrating IC50 values of 3 nM for JAK2 and 11.7 nM for SET-2 cells, with an IC50 of 41 nM for Ba/F3V617F cells. This compound exhibits over 14-fold selectivity towards JAK2 compared to JAK1, JAK3, and FLT3. JAK2-IN-7 induces cell cycle arrest in the G0/G1 phase and promotes apoptosis in tumor cells, showcasing its potential for antitumor applications. This efficacy makes JAK2-IN-7 a valuable tool for studying JAK2-related signaling pathways in cancer research. -
JAK1 Inhibitor
Povorcitinib is a selective Janus kinase 1 (JAK1) inhibitor known for its ability to significantly reduce abscesses and inflammatory nodules. Its primary research applications include the study of cutaneous lupus erythematosus (CLE) and lichen planus (LP), making it a valuable tool for understanding and potentially treating these dermatological conditions. -
JAK1 Inhibitor
VVD-118313 is a selective inhibitor of JAK1, acting through an isoform-restricted allosteric cysteine mechanism to prevent JAK1-dependent trans-phosphorylation and cytokine signaling. This compound is instrumental in cancer research, facilitating the study of JAK1-related pathways. Additionally, VVD-118313 functions as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
JAK Inhibitor
Ilunocitinib is a selective inhibitor of the Janus kinase (JAK) signaling pathway, which plays a crucial role in various inflammatory and autoimmune diseases. By inhibiting JAK activity, Ilunocitinib can modulate cytokine signaling, making it a valuable tool in research focused on conditions such as rheumatoid arthritis and psoriasis. Its mechanism of action positions it as a significant candidate for studying JAK-associated pathways and therapeutic interventions in related diseases. -
JAK1 Inhibitor
JAK1-IN-13 is a highly selective inhibitor of Janus kinase 1 (JAK1), exhibiting an IC50 value of 0.044 nM. This compound effectively reduces the phosphorylation of signal transducer and activator of transcription 3 (STAT3), which plays a critical role in various signaling pathways. JAK1-IN-13 is valuable for research focused on JAK1-related pathways, immune responses, and related therapeutic applications. -
JAK1 Inhibitor
Atinvicitinib is a selective inhibitor of JAK1, targeting the signaling pathways involved in the regulation of pruritogenic and pro-inflammatory cytokines, particularly those associated with IL-31, IL-4, and IL-13. This compound demonstrates significant potential for studying pruritus linked to allergic dermatitis as well as canine atopic dermatitis. Its oral bioavailability and specificity make it a valuable tool for researchers investigating inflammatory skin conditions and related therapeutic interventions. -
pan JAK Inhibitor
Izencitinib is a pan Janus kinase (JAK) inhibitor with oral bioavailability and specificity for gut tissue. It exhibits potent inhibition of JAK pathways, making it a valuable tool for investigating therapeutic approaches in ulcerative colitis and other inflammatory bowel diseases. Its non-selective action on multiple JAK isoforms may provide insights into the modulation of immune responses in gastrointestinal disorders. -
JAK2/STAT3/NF-κB Inhibitor
Reticuline acts as a JAK2/STAT3 and NF-κB signaling pathway inhibitor, displaying notable anti-inflammatory properties. It effectively downregulates the mRNA expression of pro-inflammatory cytokines such as TNF-α and IL-6 while also reducing the phosphorylation levels of JAK2 and STAT3. Additionally, Reticuline demonstrates potential cardiovascular effects, making it a valuable tool for research in inflammation and cardiovascular studies. -
JAK2 Inhibitor
JAK2-IN-6 is a selective JAK2 inhibitor that demonstrates significant potency, with an IC50 value of 22.86 μg/mL. This aminothiazole derivative specifically targets JAK2 without exhibiting activity against JAK1 and JAK3. JAK2-IN-6 is primarily utilized in research focused on cancer biology due to its anti-proliferative effects on cancer cells. -
JAK Inhibitor
Ifidancitinib is a potent and selective inhibitor of Janus kinase 1 and 3, effectively disrupting gamma common chain (γc) cytokine signaling. This orally bioavailable compound is valuable in the study of allergic conditions, asthma pathophysiology, and various autoimmune diseases. Its specificity for JAK kinases makes it an important tool for exploring therapeutic interventions in these areas of research. -
JAK Inhibitor
JAK-IN-5 hydrochloride is a selective inhibitor of Janus kinase (JAK), targeting the JAK signaling pathway involved in various cellular processes. This compound demonstrates significant activity in modulating cytokine signaling, which is crucial for the regulation of immune responses and hematopoiesis. JAK-IN-5 hydrochloride is applicable in research focused on inflammatory diseases, autoimmune disorders, and hematological malignancies, providing valuable insights into therapeutic interventions targeting the JAK pathway. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib hydrochloride is a potent inhibitor of CDK2, JAK2, and FLT3, exhibiting IC50 values of 13 nM, 73 nM, and 56 nM, respectively. This orally active compound demonstrates significant efficacy in inhibiting the proliferation of various cancer cell lines. It is a valuable tool for research into therapeutic strategies targeting cell cycle regulation and signal transduction pathways in cancer. -
JAK1/2 Inhibitor
Deuruxolitinib is an orally active inhibitor of Janus kinases JAK1 and JAK2. It has been shown to significantly promote hair regrowth, making it a valuable tool for investigating alopecia areata and related disorders. This compound is essential for research focused on JAK-mediated signaling and therapeutic approaches to hair loss. -
JAK/STAT and NF-κB Inhibitor
JAK-IN-23 is a potent dual inhibitor of the JAK/STAT and NF-κB signaling pathways, targeting JAK1, JAK2, and JAK3 with IC50 values of 8.9 nM, 15 nM, and 46.2 nM, respectively. This compound effectively modulates the expression of interferon-stimulated genes (ISG) and inhibits NF-κB activation, exhibiting IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 demonstrates significant anti-inflammatory properties by reducing the release of various pro-inflammatory cytokines. Its applications include research into inflammatory bowel disease (IBD) and other related inflammatory conditions. -
JAK Inhibitor
(3S,4S)-Tofacitinib is a selective JAK inhibitor, primarily targeting JAK3 with an IC50 of 1 nM. This compound exhibits significant anti-inflammatory activity, making it valuable for research in autoimmune diseases and inflammatory conditions. Its unique S-enantiomeric structure contributes to its efficacy and specificity in modulating JAK signaling pathways. -
JAK Inhibitor
JAK-IN-24 is a selective Janus kinase (JAK) inhibitor, demonstrating IC50 values of 0.534 nM and 24 nM in the presence of 4 μM and 1 mM ATP, respectively. This compound effectively inhibits IL-15-induced STAT5 phosphorylation in peripheral blood mononuclear cells (PBMCs) with an IC50 of 86.171 nM. Additionally, JAK-IN-24 features an alkyne functional group, making it suitable for click chemistry applications via copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
JAK Inhibitor
Lorpucitinib is an orally active pan-JAK inhibitor that targets the JAK/STAT signaling pathway. It demonstrates the ability to reduce serum levels of inflammatory biomarkers, making it a valuable tool for studying inflammatory responses. Research applications of Lorpucitinib include investigations into familial adenomatous polyposis and gastrointestinal inflammatory diseases. Its selectivity and safety profile enhance its utility in both preclinical and clinical research settings. -
JAK1 Inhibitor
Filgotinib maleate is a selective JAK1 inhibitor that exhibits significant anti-inflammatory and antiviral properties. It effectively inhibits JAK1, JAK2, JAK3, and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM, and 116 nM, respectively. Additionally, Filgotinib maleate has been shown to inhibit HIV-1 driven gene transcription and reduce the proliferation of HIV-1 infected cells. This compound is valuable for research applications related to rheumatoid arthritis and inflammatory bowel disease. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib citrate is a potent inhibitor targeting CDK2, JAK2, and FLT3 kinases. This compound demonstrates significant biological activity in disrupting cell cycle progression and signaling pathways associated with cell proliferation and survival. It is utilized in cancer research applications, particularly for studies involving hematological malignancies and solid tumors where these kinases are dysregulated. -
JAK1 Inhibitor
JAK1-IN-11 is a selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 0.02 nM, demonstrating strong potency. It also exhibits inhibitory activity against JAK2 with an IC50 of 0.44 nM. Due to its high selectivity for JAK1, JAK1-IN-11 is an essential tool for investigating JAK-dependent signaling pathways and exploring therapeutic strategies in various inflammatory and autoimmune diseases. -
JAK1 Inhibitor
Povorcitinib phosphate is a selective JAK1 inhibitor with demonstrated efficacy in reducing abscesses and inflammatory nodules. This compound is valuable for investigating conditions such as cutaneous lupus erythematosus (CLE) and lichen planus (LP), supporting research into inflammatory skin diseases and potential therapeutic interventions. -
JAK1 Inhibitor
JAK1-IN-8 is a potent inhibitor of Janus kinase 1 (JAK1) with an IC50 of less than 500 nM. This compound demonstrates significant inhibition of JAK1-mediated signaling pathways, making it a valuable tool for studying immune responses and inflammatory conditions. Its application extends to research in cancer biology and other diseases where JAK1 plays a critical role in pathophysiology. -
JAK2 Inhibitor
Pacritinib citrate is a selective inhibitor of Janus kinase 2 (JAK2), effective against both wild-type JAK2 (IC50 = 23 nM) and the JAK2V617F mutant (IC50 = 19 nM). In addition to its primary target, Pacritinib citrate also inhibits FLT3 and its mutant FLT3D835Y (IC50 = 22 nM and 6 nM, respectively). This compound is relevant for research focused on acute myeloid leukemia (AML) and myelofibrosis (MF), providing a valuable tool for elucidating the role of JAK2 and FLT3 in these hematological malignancies. -
JAK3 Inhibitor
Ritlecitinib tosylate is a selective, orally active, irreversible covalent inhibitor of JAK3, exhibiting an IC50 value of 33 nM. It does not inhibit JAK1, JAK2, or TYK2, demonstrating a unique specificity for JAK3. This compound effectively interrupts signaling and downstream STAT phosphorylation induced by common gamma chain cytokines like IL-2 and IL-15. Ritlecitinib tosylate has been shown to inhibit Th1/Th17 cell differentiation and function, making it a valuable tool for research applications related to autoimmune diseases, with demonstrated efficacy in preclinical models of alopecia areata, adjuvant-induced arthritis, and experimental autoimmune encephalomyelitis. -
JAK1 Inhibitor
(R,R)-VVD-118313 is a selective inhibitor of Janus kinase 1 (JAK1), targeting its role in cytokine signaling and trans-phosphorylation. This compound demonstrates significant potential in cancer research by modulating JAK1-mediated pathways. Additionally, (R,R)-VVD-118313 serves as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds, further expanding its utility in chemical biology applications. -
JAK1 Inhibitor
Itacitinib adipate is a selective JAK1 inhibitor that exhibits oral bioavailability. This compound has demonstrated efficacy and safety in phase II clinical trials for the treatment of myelofibrosis. Its mechanism of action, targeting the JAK1 pathway, makes it a valuable tool for research in hematological malignancies and associated signaling pathways. -
JAK3 Inhibitor
(2R,5S)-Ritlecitinib is a selective inhibitor of Janus kinase 3 (JAK3) with an IC50 of 144.8 nM. This compound demonstrates significant biological activity in modulating immune responses and is primarily utilized in research focused on autoimmune diseases and hematological disorders. Its ability to inhibit JAK3 signaling pathways makes it a valuable reagent for studies investigating cytokine signaling and immunological reactions. -
JAK Inhibitor
Methyl 6-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-4-oxo-4,5-dihydropyrazolo[1,5-a]pyrazine-2-carboxylate is a selective inhibitor of Janus Kinases (JAK) with demonstrated IC50 values of 6 nM for TYK2, 21 nM for JAK1, 8 nM for JAK2, and 1051 nM for JAK3. This compound effectively inhibits IL-12 production in human whole blood, with an IC50 of 28 nM. It is poised for applications in cancer research and may provide insight into the modulation of signaling pathways mediated by JAK kinases. -
JAK Inhibitor
Lepzacitinib is a selective Janus kinase (JAK) inhibitor specifically targeting JAK1 and JAK3. It demonstrates significant anti-inflammatory activity, making it a valuable tool for investigating therapeutic strategies in atopic dermatitis and other inflammatory skin conditions. This compound is essential for research focused on cytokine signaling pathways and their role in skin disorders. -
JAK1/2 Inhibitor
JAK1/2-IN-1 is a selective inhibitor of Janus Kinase 1 (JAK1) and Janus Kinase 2 (JAK2), exhibiting IC50 values of 0.4 nM and 8.1 nM, respectively. In addition to its action on JAK1 and JAK2, it also demonstrates inhibitory effects on interleukin-4 (IL-4) and interleukin-13 (IL-13) with IC50 values of 136.5 nM and 19.1 nM, respectively. This compound is valuable for research applications focused on cytokine signaling and its role in inflammatory diseases. -
JAK Inhibitor
(3R,4S)-Tofacitinib is a selective JAK inhibitor, primarily targeting JAK3 with an IC50 of 1 nM. This enantiomer exhibits reduced biological activity compared to its counterpart, making it a useful tool for dissecting the role of JAK signaling in various biological processes. It is applicable in research focused on autoimmune diseases, inflammation, and related therapeutic areas. -
JAK1/TYK2 Inhibitor
Quecitinib is an orally active dual inhibitor of JAK1 and TYK2, functioning by obstructing their enzymatic activity. This compound exhibits significant biological activity relevant to the modulation of immune responses, making it valuable in research on atopic dermatitis and various autoimmune diseases. Favorable pharmacokinetic properties, along with a safety profile attributed to its metabolism via cytochrome P450 3A, enhance its potential as a therapeutic agent in related studies. -
JAK Inhibitor
Pumecitinib is a selective Janus kinase (JAK) inhibitor that exhibits significant anti-inflammatory activity. By targeting the JAK signaling pathway, it has been shown to modulate immune responses and reduce inflammation. This compound is valuable for research into inflammatory diseases and conditions driven by aberrant JAK signaling. -
ITK/JAK3 Inhibitor
Modzatinib is a selective, covalent inhibitor targeting ITK and JAK3, demonstrating IC50 values of 8 nM and 23 nM, respectively. Its potent anti-inflammatory properties make it a valuable tool for research in autoimmune and inflammatory diseases, facilitating the exploration of therapeutic interventions in these areas. Researchers can leverage modzatinib to study the mechanistic roles of ITK and JAK3 in immune responses and disease pathology. -
JAK1 Inhibitor
GS-829845 is a JAK1 inhibitor that serves as a significant active metabolite of Filgotinib. This compound preferentially inhibits JAK1, exhibiting approximately 10-fold lower potency than its parent compound while demonstrating an extended half-life. GS-829845 is primarily utilized in research related to autoimmune disorders and other inflammatory conditions, contributing to the understanding of JAK pathway modulation in therapeutic applications. -
JAK1 Inhibitor
GDC-4379 is a selective inhibitor of JAK1, a key enzyme involved in the signaling pathways of various cytokines. This compound demonstrates significant biological activity in the modulation of immune responses, making it relevant for research applications in asthma and other inflammatory diseases. Its ability to inhibit JAK1 signaling offers insights into the therapeutic potential for treating pathologies associated with dysregulated immune function. -
Type II JAK2 Inhibitor
YLIU-4-105-1 is a Type II JAK2 inhibitor that selectively targets the ATP-binding pocket of the JH1 domain. This compound demonstrates significant biological activity, effectively inhibiting phosphorylated STAT5 (pSTAT5) signaling pathways. Research applications include studies on myeloproliferative neoplasms and other diseases associated with JAK2 mutations, with in vivo pharmacodynamic effects such as reduction in spleen-to-body weight ratio and decreased blood reticulocyte counts observed in a dose-dependent manner.
