Catalog No.
Product Name
Application
Product Information
Citations
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Aurora Kinase A/JAK2 Inhibitor
AJI-214 is a dual-target inhibitor that simultaneously inhibits Aurora kinase A and Janus kinase 2 (JAK2). It directly blocks Aurora A activity, disrupting T cell mitotic progression and polarity, while also inhibiting JAK2-mediated STAT3 phosphorylation, thereby suppressing the differentiation of pro-inflammatory TH1 and TH17 cells. AJI-214 holds therapeutic potential for modulating immune responses and is being investigated for the prevention and treatment of graft-versus-host disease (GVHD). -
PROTAC JAK2 degrader
SJ1008030 (Compound 8) formic is a selective PROTAC degrader of JAK2, designed to target and eliminate JAK2 protein via the ubiquitin–proteasome pathway. It effectively inhibits the growth of MHH–CALL-4 leukemia cells with an IC₅₀ of 5.4 nM. SJ1008030 formic is a valuable tool for leukemia research and the study of JAK2-driven signaling pathways. -
JAK2/3 PROTAC Degrader
SJ10542 is a potent and selective PROTAC degrader targeting JAK2 and JAK3. With DC50 values of 14 nM for JAK2 and 11 nM for JAK3 in patient-derived xenograft cells (PDX), SJ10542 demonstrates significant antitumor activity. This compound is valuable for research in hematological malignancies and autoimmune diseases, facilitating the exploration of targeted degradation mechanisms in these therapeutic areas. -
PROTAC JAK2 Degrader
SJ988497 is a potent PROTAC JAK2 degrader that targets JAK2 for degradation, playing a critical role in the inhibition of CRLF2-rearranged (CRLF2r) cell proliferation. Functionally, SJ988497 induces degradation of the neosubstrate GSPT1 through its architecture consisting of a Ruxolitinib derivative, a linker, and the CRBN ligand Pomalidomide. This compound is particularly valuable for research focused on acute lymphoblastic leukemia (ALL). -
JAK1 PROTAC Degrader
PROTAC JAK1 Degrader 1 is a selective PROTAC agent targeting JAK1, exhibiting a DC50 of 214 nM. This compound initiates rapid degradation of JAK1, leading to significant antitumor activity. It serves as a valuable tool for investigating JAK1-related signaling pathways and developing therapeutic strategies for malignancies driven by JAK1 dysregulation. -
TYK2 Degrader
PROTAC TYK2 degradation agent1 is a selective degrader targeting TYK2, effectively facilitating its degradation with a DC50 value of 14 nM. This compound highlights significant biological activity in modulating TYK2 levels, making it a useful tool for investigating autoimmune diseases. Research applications include studying the role of TYK2 in inflammatory pathways and evaluating potential therapeutic strategies. -
PTPN1/PTPN2 Inhibitor
Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction. -
JAK-STAT Inhibitor
WP-1034 is a selective JAK-STAT inhibitor that exhibits pro-apoptotic and antileukemic properties, particularly in acute myeloid leukemia (AML) models. By blocking the activation of Stat 3 and Stat 5, WP-1034 effectively induces cell cycle arrest and triggers apoptosis in affected cells. This reagent is valuable for research focused on understanding the mechanisms and therapeutic avenues in AML. -
JAK2 Inhibitor
Itacnosertib is a selective inhibitor of JAK2, with an IC50 value of 8540 nM, and it also targets FLT3 and ACVR1 (ALK2) with an IC50 of 8 nM. This compound demonstrates significant anti-leukemic activity, making it valuable for research in hematological malignancies. Itacnosertib is utilized in studies investigating the mechanisms of JAK2-mediated signaling pathways and the development of targeted therapies for related disorders. -
JAK Inhibitor
JAK-IN-39 is a potent inhibitor of the Janus kinase (JAK) family, specifically targeting JAK1, JAK2, and JAK3 with IC50 values of 0.05, 1.18, and 0.03 nM, respectively. This compound effectively reduces the viability of TF-1 cells and inhibits the production of pro-inflammatory cytokines, including TNFα and IFNγ, in vitro. JAK-IN-39 is valuable for research into immune regulation and potential therapeutic applications in inflammatory diseases and hematological malignancies. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-3 is a dual inhibitor targeting Janus kinase (JAK) and histone deacetylases (HDAC). It exhibits potent inhibitory activity with IC50 values of 25.36 nM for JAK2, and 0.2 μM and 0.43 μM for HDAC and HDAC1, respectively. This compound is valuable for investigating the roles of JAK and HDAC pathways in cellular processes and disease models, particularly in cancer and inflammatory research. -
JAK3 Inhibitor
DPPY is a potent JAK3 inhibitor with an IC50 of less than 10 nM, demonstrating high selectivity for protein tyrosine kinases including EGFR and BTK. It exhibits significant anti-proliferative activity against B-cell lymphoma cells. DPPY holds potential for research applications related to idiopathic pulmonary fibrosis (IPF) and other conditions involving aberrant JAK3 signaling. -
JAK Inhibitor
MJ04 is a selective inhibitor targeting Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. This compound effectively inhibits T cell differentiation and reduces pro-inflammatory cytokine production in lipopolysaccharide-induced macrophages. Additionally, MJ04 exhibits favorable pharmacokinetic properties in mice and has demonstrated the ability to promote hair growth in a dihydrotestosterone-induced model of androgenetic alopecia (AGA), showing minimal toxicity (LD50 > 2 g/kg). -
JAK2/FLT3 Inhibitor
Flonoltinib TFA is a potent and orally bioavailable inhibitor that targets both JAK2 and FLT3, exhibiting IC50 values of 0.7 nM and 4 nM, respectively, alongside 26 nM and 39 nM for JAK1 and JAK3. This compound possesses significant anti-cancer activity, making it a valuable tool for research in oncology and therapeutic development against malignancies driven by these pathways. Its dual inhibition profile highlights its potential in addressing cancers associated with aberrant JAK2 and FLT3 signaling. -
JAK2 Inhibitor
ZT55 is a potent and selective inhibitor of JAK2, exhibiting an IC50 value of 0.031 μM. This compound effectively inhibits the proliferation of JAK2V617F-expressing HEL cell lines, inducing apoptosis and cell cycle arrest. In vivo, ZT55 demonstrates significant efficacy in inhibiting the growth of HEL xenograft tumors in mouse models. It serves as a valuable tool for research in myeloproliferative neoplasms, including polycythemia vera and primary thrombocythemia. -
JAK2 Inhibitor
ON044580 is a potent non-ATP-competitive inhibitor of the JAK2 kinase, demonstrating IC50 values of 1.23 μM and 1.09 μM for wild-type and V617F mutant JAK2, respectively. This compound functions by either binding to the STAT-5 binding domain or an allosteric site of JAK2, leading to the suppression of JAK2 kinase activity. ON044580 effectively induces apoptosis in chronic myelogenous leukemia cells that exhibit resistance to Imatinib, and it also inhibits both wild-type and T315I mutant forms of the BCR-ABL kinase. This reagent holds promise for therapeutic applications in myeloproliferative disorders characterized by dysregulated JAK/STAT signaling. -
JAK Inhibitor
Dehydrocrenatidine is a natural alkaloid that functions as a selective inhibitor of Janus kinases (JAK). This compound exhibits significant biological activity by inhibiting voltage-gated sodium channels, which may alleviate mechanical allodynia in neuropathic pain models. Dehydrocrenatidine serves as a valuable tool for research in pain mechanisms and the therapeutic targeting of JAK pathways. -
HDAC/JAK/BRD4 Inhibitor
HDAC/JAK/BRD4-IN-1 is a potent inhibitor targeting histone deacetylases (HDAC), Janus kinases (JAK), and bromodomain-containing protein 4 (BRD4). This compound demonstrates significant anti-proliferative effects and promotes apoptosis in MDA-MB-231 breast cancer cells. Additionally, HDAC/JAK/BRD4-IN-1 exhibits promising anticancer activity in vivo, making it a valuable tool for research in cancer therapeutics and the study of epigenetic and signaling pathways. -
JAK2/FLT3 Inhibitor
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. -
JAK1 Inhibitor
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. -
Aurora/JAK Inhibitor
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. -
JAK2/3 Inhibitor
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. -
JAK2 Inhibitor
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. -
STAT3/JAK Inhibitor
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. -
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. -
JAK2 Signal Activator
Coumermycin A1 is a JAK2 signal activator that functions by inhibiting DNA gyrase, leading to the inhibition of bacterial cell division. This compound exhibits notable anti-orthopoxvirus activity, making it valuable for research applications related to bacterial infections and viral pathogenesis. Additionally, its role in modulating JAK2 signaling pathways may provide insights into therapeutic interventions for diseases involving dysregulated signaling. -
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. -
α7 nAchR/JAK2/STAT3 Agonist
α7 nAchR-JAK2-STAT3 agonist 1 is a selective agonist targeting the α7 nicotinic acetylcholine receptor, modulating the JAK2-STAT3 signaling pathway. It demonstrates significant anti-inflammatory activity by inhibiting the expression of inducible nitric oxide synthase (iNOS), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) in murine RAW264.7 macrophages, with an IC50 of 0.32 μM for nitric oxide production. Additionally, it effectively suppresses lipopolysaccharide (LPS)-induced nitric oxide release, NF-κB activation, and related cytokine production. This compound is valuable for studying sepsis and inflammatory responses. -
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. -
JAK2 JH2 Binder
JAK2 JH2 binder-1 is a potent and selective inhibitor targeting the JAK2 JH2 domain, exhibiting a Kd of 37.1 nM. This compound holds significant promise for research into myeloproliferative neoplasms, offering insights into the mechanisms of JAK2-mediated signaling pathways and potential therapeutic interventions. -
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.
