Catalog No.
Product Name
Application
Product Information
Citations
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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. -
JAK1/2 inhibitor
iJak-381 is a selective inhibitor of JAK1 and JAK2, exhibiting significant anti-inflammatory properties. This compound effectively disrupts IL-13 signaling, along with inhibiting the IL-4 and IL-6 pathways, leading to a reduction in phosphorylated STAT6 levels. Additionally, iJak-381 demonstrates the ability to diminish the influx of inflammatory cells in the lungs of murine models, thereby alleviating airway hyperresponsiveness (AHR). It serves as a valuable tool for research into therapeutic strategies targeting inflammatory diseases. -
JAK Inhibitor
JAK-IN-20 is a potent, pan-selective Janus kinase (JAK) inhibitor, exhibiting IC50 values of 7 nM, 5 nM, and 14 nM for JAK1, JAK2, and JAK3, respectively. This orally active compound demonstrates favorable pharmacokinetic properties and exerts significant anti-inflammatory effects in vivo. JAK-IN-20 is suitable for research applications targeting JAK signaling pathways, particularly in the contexts of autoimmune diseases and chronic inflammation. -
JAK Inhibitor
Nimucitinib is a Janus kinase (JAK) inhibitor that interferes with the JAK-STAT signaling pathway. It exhibits anti-inflammatory properties and is utilized in various research applications, including the study of autoimmune diseases and inflammatory conditions. Nimucitinib's ability to modulate cytokine signaling makes it a valuable tool for investigating therapeutic strategies in hematological and oncological research. -
JAK2/STAT3 Inhibitor
SD-1029 is a selective JAK2/STAT3 inhibitor that impedes the phosphorylation of JAK2, thereby obstructing STAT3 activation. By inhibiting STAT3 nuclear translocation, SD-1029 serves as a valuable tool for studying the JAK2/STAT3 signaling pathway. This compound is relevant in research applications involving cancer, autoimmune disorders, and other diseases associated with dysregulated STAT3 activity. -
JAK3 Inhibitor
JAK 3i is a highly selective inhibitor of JAK3, exhibiting an IC50 of 0.43 nM. It forms a covalent bond with a specific cysteine residue in the JAK3 kinase domain, demonstrating minimal interaction with JAK1, JAK2, or TYK2. JAK 3i effectively inhibits IL-2-driven T-cell proliferation in vivo, making it a valuable tool for research applications in autoimmune diseases and related therapeutic studies. -
Tubulin/JAK2-IN-1 inhibitor, Antitumor
Tubulin/JAK2-IN-1 is a dual inhibitor targeting Janus kinase 2 (JAK2) and microtubules, exhibiting potent antitumor activity. This compound demonstrates significant antiproliferative effects against various cancer cell lines, making it a valuable tool in cancer research. Its dual mechanism of action supports investigations into therapies that disrupt cell division and signaling pathways in malignancies. -
JAK1 Inhibitor
Blovacitinib is a selective inhibitor of Janus kinase 1 (JAK1), demonstrating high potency with IC50 values of 3, 37, 1517, and 36 nM against JAK1, JAK2, JAK3, and TYK2, respectively. This oral agent is primarily utilized in research focused on rheumatoid arthritis, targeting inflammatory pathways associated with this condition. Its specificity for JAK1 makes it an important tool for investigating JAK-STAT signaling mechanisms in various cellular contexts. -
JAK Inhibitor
(1R)-AZD-1480 is an ATP-competitive inhibitor targeting Janus kinase 1 (JAK1) and Janus kinase 2 (JAK2). It exhibits potent inhibitory activity and is utilized in research applications focused on cytokine signaling, immune response modulation, and the investigation of various hematological malignancies. This compound serves as a valuable tool for exploring JAK-related pathways and therapeutic strategies in malignancies and autoimmune disorders. -
JAK Inhibitor
JAK-IN-11 is a potent and selective Janus kinase (JAK) inhibitor designed for the treatment of skin disorders, including cutaneous lupus. This compound exhibits significant biological activity by modulating JAK signaling pathways, making it a valuable tool for research in inflammatory conditions. Additionally, JAK-IN-11 functions as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating its application in chemical biology studies. -
JAK Inihibitor
AC-430 hydrobromide is a potent JAK2 inhibitor that specifically targets the Janus kinase family, playing a crucial role in the signaling pathways of hematopoiesis. This compound demonstrates significant biological activity in the context of myeloproliferative disorders and certain cancers, making it a valuable reagent for research in these areas. Its inhibition of JAK2 provides insights into therapeutic strategies for related malignancies and inflammatory conditions. -
JAK Inhibitor
JAK-IN-10 is a selective Janus kinase (JAK) inhibitor that modulates inflammatory pathways by inhibiting JAK signaling. It is particularly valuable in the study of dry eye disorders, providing insights into the underlying mechanisms of inflammation. Additionally, JAK-IN-10 features an alkyne functional group and is suitable for click chemistry applications, enabling efficient copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds. This property enhances its utility in chemical biology and medicinal chemistry research. -
JAK Inhibitor
Frevecitinib is a potent pan-JAK inhibitor, targeting JAK1, JAK2, JAK3, and TYK2. This compound is useful for investigating mechanisms involved in asthma and other respiratory conditions, including chronic obstructive pulmonary disease (COPD). Its ability to modulate JAK signaling pathways makes it a valuable tool in research focused on inflammatory diseases and immune response. -
JAK2 Inhibitor
JAK-IN-35 is a selective JAK2 inhibitor that targets the Janus kinase 2 enzyme. This compound demonstrates significant anti-proliferative activity in various cancer cells, making it a valuable tool for cancer research. Its ability to modulate JAK2 signaling pathways can aid in the exploration of therapeutic strategies for malignancies driven by aberrant JAK2 activity. -
JAK Inhibitor
JAK-IN-26 is an orally active Janus kinase (JAK) inhibitor that effectively targets the JAK-STAT signaling pathway. It demonstrates significant inhibitory activity on IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells, with an IC50 value of 17.2 nM. This compound is valuable for research applications focused on cytokine signaling, immune response modulation, and the study of JAK-related signaling pathways in various disease contexts. -
JAK1 Inhibitor
JAK-IN-14 is a selective inhibitor of Janus kinase 1 (JAK1), exhibiting an IC50 of less than 5 μM. This compound demonstrates over eightfold selectivity for JAK1 compared to JAK2 and JAK3. JAK-IN-14 is valuable for research applications focused on elucidating the role of JAK1 in various inflammatory and autoimmune conditions. -
JAK Inhibitor
Lirucitinib is a selective JAK inhibitor with significant anti-inflammatory activity. It effectively inhibits the signaling of various cytokines involved in itch and inflammation, particularly those that rely on JAK1 enzyme activity, as well as cytokines related to allergic responses. This compound is valuable for research applications focused on pruritic skin diseases and associated inflammatory conditions. -
JAK2 V617F Inhibitor
JAK2-IN-10 is a potent inhibitor targeting the JAK2 V617F mutation, exhibiting an IC50 value of ≤10 nM. This compound demonstrates significant activity in suppressing the JAK/STAT signaling pathway, which is often dysregulated in various hematological malignancies. JAK2-IN-10 is suitable for research applications focused on understanding myeloproliferative neoplasms and developing targeted therapies. -
JAK Inhibitor
JAK-IN-21 is a selective and potent inhibitor of Janus kinase (JAK), demonstrating inhibitory concentrations (IC50) of 1.73 nM for JAK1, 2.04 nM for JAK2, 109 nM for the J2V617F mutant, and 62.9 nM for TYK2. This compound is useful in research applications focused on elucidating the role of JAK signaling pathways in various diseases, including hematological malignancies and autoimmune disorders. JAK-IN-21 serves as a valuable tool for studying the therapeutic potential of JAK inhibition. -
PROTAC JAK2 Degrader
SJ1008030 is a PROTAC compound designed to selectively degrade Janus kinase 2 (JAK2). This compound exhibits potent inhibitory activity against MHH–CALL-4 cell growth, with an IC50 of 5.4 nM. SJ1008030 is valuable for research applications focusing on leukemia, facilitating the study of JAK2-related pathways and therapeutic interventions. -
Cathepsin L/JAK Inhibitor
Dual Cathepsin L/JAK-IN-1 is a dual inhibitor targeting Cathepsin L (CTSL) and Janus kinases (JAK), exhibiting IC50 values of 0.68 μM for CTSL, 337.1 nM for JAK1, 5.251 nM for JAK2, 27.29 nM for JAK3, and 172.6 nM for TYK2. This compound effectively inhibits the activation of key signaling pathways, including MAPK, NF-κB, and JAK/STAT, thereby providing substantial anti-inflammatory effects. Dual Cathepsin L/JAK-IN-1 is useful for investigating mechanisms underlying acute lung injury (ALI) and other inflammatory conditions. -
JAK1 Inhibitor
Upadacitinib tartrate tetrahydrate is a selective inhibitor of Janus kinase 1 (JAK1) with an IC50 value of 43 nM. It exhibits approximately 74-fold selectivity for JAK1 over JAK2 in assays utilizing specific cytokines. This compound is widely applicable in research focused on autoimmune disorders, providing insights into the modulation of immune responses through JAK1 inhibition. -
JAK Inhibitor
JAK1/TYK2-IN-1 is a potent dual inhibitor targeting Janus kinase 1 (JAK1) and tyrosine kinase 2 (TYK2), with reported IC50 values of 29 nM and 41 nM, respectively. This compound exhibits significant anti-inflammatory and immunomodulatory effects, making it a valuable tool for research related to autoimmune disorders and cytokine signaling pathways. Its ability to selectively inhibit JAK1 and TYK2 enhances its potential for studying the mechanisms of JAK-mediated signaling in various biological contexts. -
JAK Inhibitor
Peficitinib hydrobromide is a selective Janus kinase (JAK) inhibitor, exhibiting IC50 values of 3.9 nM for JAK1, 5.0 nM for JAK2, 0.7 nM for JAK3, and 4.8 nM for Tyk2. This compound is primarily utilized in research related to autoimmune diseases and inflammatory conditions, demonstrating potential therapeutic efficacy in modulating immune responses. Its oral bioavailability makes it a valuable tool for studying JAK signaling pathways in various biological models. -
JAK1/JAK2 Inhibitor
RAI-20 is a potent orally active dual inhibitor of JAK1 and JAK2, demonstrating IC50 values of 15.1 nM and 22.7 nM, respectively. This compound features favorable pharmacokinetic characteristics, including enhanced plasma stability and extended systemic exposure. In preclinical studies using a collagen-induced arthritis rat model, RAI-20 exhibited significant anti-inflammatory and anti-arthritic effects, effectively decreasing paw swelling volume and overall arthritis index. RAI-20 serves as a valuable tool for investigating the mechanisms underlying rheumatoid arthritis pathology.
