Catalog No.
Product Name
Application
Product Information
Citations
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SYK/JAK Inhibitor
SYK/JAK-IN-1 is a dual inhibitor targeting SYK and JAK2, exhibiting IC50 values of less than 5 nM for both kinases. This compound demonstrates significant anti-inflammatory and anti-proliferative activities, making it a valuable tool for research involving hematological malignancies and autoimmune disorders. Its potent inhibition profile allows for the exploration of signaling pathways associated with SYK and JAK2, facilitating studies in cancer biology and immunology. -
JAK1 Inhibitor
MMT3-72 is a selective inhibitor of Janus kinase 1 (JAK1), demonstrating effective modulation of the JAK-STAT signaling pathway. This compound significantly reduces phosphorylated STAT3 (p-STAT3) levels in models of dextran sulfate sodium (DSS)-induced colitis, highlighting its potential role in inflammatory bowel disease research. MMT3-72 serves as a valuable tool for studying JAK1-related signaling mechanisms and therapeutic interventions in related conditions. -
JAK1 Inhibitor
JAK1-IN-17 is a highly selective inhibitor of Janus kinase 1 (JAK1), exhibiting a Ki of 1.9 nM. This compound maintains effective potency in whole blood due to its low whole blood shift, making it a valuable tool for hematological studies. Additionally, JAK1-IN-17 is a nitrile-containing analogue that displays weak reversible inhibition of CYP3A4, demonstrated by an IC50 of 7.9 μM. Researchers can utilize JAK1-IN-17 in cancer research to explore the therapeutic potential of JAK1 inhibition in various malignancies. -
JAK3 Inhibitor
JAK3-IN-12 is a potent inhibitor of Janus kinase 3 (JAK3), exhibiting IC50 values of 9.5 nM, 18 nM, and 42 nM for JAK3, JAK1, and JAK2, respectively. This compound serves as a valuable tool for investigating the role of JAK3 in various biological processes, particularly in the context of autoimmune diseases such as rheumatoid arthritis. Its selective inhibition can facilitate understanding of JAK3's function and its potential as a therapeutic target in related research applications. -
JAK inhibitor
JAK kinase-IN-1 is a selective inhibitor of Janus kinase (JAK) family members, effectively targeting TYK2, JAK1, JAK2, and JAK3 with IC50 values of 4.2 nM, 32 nM, 27 nM, and 3473 nM, respectively. This compound demonstrates significant biological activity in modulating JAK-mediated signaling pathways, making it a valuable reagent for research on immune responses and inflammatory diseases. Its specificity and potency contribute to its utility in investigating the role of JAK kinases in various cellular processes and therapeutic applications. -
JAK1 Inhibitor
JAK1-IN-19 is a potent inhibitor of Janus kinase 1 (JAK1), demonstrating IC50 values of 0.02 nM for JAK1, 0.5 nM for JAK2, 91 nM for JAK3, and 0.2 nM for TYK2. This compound exhibits enhanced intrinsic clearance in both rat and human models. JAK1-IN-19 is applicable for research in atopic dermatitis and other autoimmune diseases, facilitating the investigation of JAK1 signaling pathways and their role in inflammatory responses. -
JAK1/2/3 Inhibitor
INCB16562 is a selective inhibitor targeting JAK1 and JAK2, with a notable preference for JAK1 over JAK3. It effectively inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3, thereby blocking the proliferation and survival of myeloma cells reliant on IL-6 for growth. Furthermore, INCB16562 demonstrates antitumor activity in vivo by reducing the growth of myeloma xenografts in murine models. This compound shows potential for advancing research in multiple myeloma therapies. -
JAK1/2 Inhibitor
JAK1/2-IN-2 is a highly selective inhibitor of the Janus kinase 1 and 2 (JAK1/2) pathways, demonstrating Ki values of 2 nM and 0.6 nM, respectively. This compound is instrumental in research focused on the modulation of cytokine signaling pathways and holds potential for therapeutic applications in autoimmune diseases and hematological malignancies. Its potent inhibition of JAK1/2 makes it a valuable tool for understanding the role of these kinases in various biological processes. -
JAK2 Inhibitor
Tkip is a selective inhibitor of JAK2, targeting the JAK2 autophosphorylation site. It effectively inhibits JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1, thereby reducing the antiviral effects of IFN-γ and downregulating MHC Class I molecule expression. Tkip is a valuable tool for investigating the IFN-γ signaling pathway and its implications in various biological processes. -
BET/JAK2/FLT3 Inhibitor
SG3-179 is a selective inhibitor of BET bromodomain proteins, with additional activity against JAK2 and FLT3. This compound effectively reduces HOXB13 protein expression, demonstrating potential relevance in the study of multiple myeloma (MM1.S). SG3-179 is a valuable tool for research involving epigenetic regulation and signaling pathways associated with hematological malignancies. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-1 is a potent dual inhibitor targeting JAK3 and BTK, key proteins implicated in autoimmune diseases. By simultaneously blocking the BTK/JAK3 signaling pathway, this compound demonstrates synergistic effects that could enhance therapeutic outcomes. JAK3/BTK-IN-1 is suitable for research into JAK3 kinase and BTK-related diseases, facilitating the exploration of innovative treatment strategies in immunology and related fields. -
JAK Inhibitor
Tyk2-IN-17 is a selective inhibitor of the Janus kinase 2 (TYK2). This compound effectively impedes the activity of TYK2, which is crucial in various signaling pathways associated with immune regulation and inflammation. Tyk2-IN-17 is primarily used in research focusing on autoimmune diseases, inflammatory disorders, and cancer biology, providing insights into therapeutic strategies for conditions mediated by aberrant JAK signaling. -
JAK Inhibitor
PF-1367550 is a pan-JAK inhibitor that selectively targets Janus kinase enzymes. It is demonstrated to reduce the release of pro-inflammatory cytokines CXCL9, CXCL10, and CXCL11 from primary airway epithelial cells. This compound is valuable for research in inflammatory diseases and the modulation of immune responses. -
JAK Inhibitor
CEE321 is a potent pan-JAK inhibitor that exhibits an IC50 value of 54 nM. It effectively inhibits key biomarkers associated with atopic dermatitis, making it a valuable tool for research in inflammatory skin conditions and related therapeutic studies. Its broad activity against various JAK isoforms facilitates investigations into the signaling pathways involved in immune responses. -
Aurora Kinase A/JAK2 Inhibitor
AJI-100 is a dual-target inhibitor that selectively inhibits Aurora kinase A and JAK2 with IC50 values of 12.7 nM and 18.5 nM, respectively. By directly blocking Aurora kinase A, AJI-100 disrupts T cell mitosis and cell polarity, while its inhibitory effect on JAK2 activation prevents STAT3 phosphorylation. This compound is valuable for research focused on modulating immune responses and has potential applications in the prevention of graft-versus-host disease (GVHD). -
JAK2-STAT5 Activator
Methionyl-methionine (Met-Met) functions as a JAK2-STAT5 activator, enhancing intracellular substrate availability. This compound has been shown to significantly promote the expression of α-s1 casein (αS1-CN) in mammary explants, mediated through the activation of JAK2-STAT5 and mTOR signaling pathways. Its role in modulating these critical pathways makes it a valuable tool for research in lactation biology and protein synthesis studies. -
JAK3 Inhibitor
CP-690550A is a selective inhibitor targeting Janus kinase 3 (JAK3), with notable efficacy against JAK2 as well. This compound exhibits significant immunosuppressive properties and is primarily utilized in research focused on autoimmune diseases and transplant rejection. Its ability to modulate cytokine signaling pathways makes it a valuable tool for studying immune response mechanisms. -
JAK2 Inhibitor
NMS-P953 is a potent orally active inhibitor of JAK2, exhibiting an IC50 of 0.008 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. It is particularly useful in studies focusing on JAK2-related signaling pathways and therapeutic applications in hematological malignancies. -
JAK2 Inhibitor
BVB808 is a selective JAK2 inhibitor, exhibiting approximately 10-fold selectivity for JAK2 over other JAK family members in vitro. This compound effectively inhibits JAK2 activity, leading to a reduction in STAT5 phosphorylation, which in turn disrupts JAK2-dependent cell proliferation and survival signaling pathways. BVB808 is utilized in cancer research, particularly in studies focusing on malignancies driven by JAK2 signaling dysregulation. -
JAK3/Syk Inhibitor
R-348 choline is a potent, orally active inhibitor of Janus kinase 3 (JAK3) and spleen tyrosine kinase (Syk). This compound effectively reduces the expression levels of pro-inflammatory cytokines, including interferon-gamma (IFN-γ), interleukin-6 (IL-6), and interleukin-10 (IL-10). R-348 choline is primarily utilized in research related to acute cardiac allograft rejection and other autoimmune conditions where JAK3 and Syk signaling play critical roles. -
JAK3 Inhibitor
JAK3-IN-19 is a selective inhibitor of Janus kinase 3 (JAK3), a critical component in cytokine signaling pathways. Inhibition of JAK3 has been shown to affect the proliferation and survival of cancer cells. This compound is valuable for research applications focused on understanding the role of JAK3 in various malignancies and exploring its potential as a therapeutic target in cancer treatment. -
JAK Inhibitor
(3S,4R)-Tofacitinib is a less active enantiomer of Tofacitinib, primarily targeting Janus kinase 3 (JAK3) as a potent inhibitor. It exhibits an IC50 of 1 nM, highlighting its potential for modulating immune responses and inflammatory processes. This compound is valuable for research in immunology and the development of therapies targeting JAK-mediated signaling pathways. -
JAK Inhibitor
AS2553627 is a selective JAK inhibitor, exhibiting IC50 values of 0.46 nM for JAK1, 0.30 nM for JAK2, 0.14 nM for JAK3, and 2.0 nM for TYK2. This compound effectively inhibits the proliferation of human and rat T cells in response to IL-2, with IC50 values of 2.4 nM and 4.3 nM, respectively. In preclinical studies, AS2553627 has demonstrated a capacity to mitigate cardiac allograft vasculopathy and fibrosis in rat heart transplant models, thereby improving survival rates and showing potential for use in preventing acute and chronic rejection in heart transplantation. -
JAKs Inhibitor
JAK-IN-34 is a potent inhibitor of Janus kinases (JAKs), demonstrating low nanomolar IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3, and 1.95 nM for TYK2. This compound effectively reduces joint swelling, indicating its potential application in inflammatory diseases and autoimmune disorders. Its favorable safety profile makes it a valuable tool for research focused on JAK signaling pathways and related therapeutic interventions. -
JAK Inhibitor
JAK3-IN-7 is a potent and selective inhibitor of Janus kinase 3 (JAK3) with an IC50 of less than 0.01 μM. This compound effectively modulates JAK3-mediated signaling pathways, which are critical for immune response and hematopoiesis. JAK3-IN-7 is valuable for research applications focused on autoimmune diseases, inflammatory disorders, and hematological malignancies. -
JAK inhibitor
LY2784544 is identified as being highly selective for JAK2-V617F and has advanced into human clinical trials for the treatment of several myeloproliferative disorders. -
JAK2/FLT3 inhibitor
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity. -
dual JAK1/TYK2 inhibitor
PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. -
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. -
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. - 6-Demethoxytangeretin is a flavonoid compound isolated from *Citrus reticulata* with demonstrated anti-inflammatory and anti-allergic properties. It inhibits IL-6 production and the expression of related genes in human mast cells by modulating the ALK and MAPK signaling pathways. Additionally, 6-Demethoxytangeretin enhances CRE-mediated transcription in hippocampal neurons, indicating potential neuroregulatory effects.
