Catalog No.
Product Name
Application
Product Information
Citations
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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
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. -
AK/STAT Signaling Inhibitor
AUH-6-96 is a potent JAK/STAT signaling inhibitor that effectively reduces Unpaired-induced transcriptional activity in Drosophila cells and inhibits tyrosine phosphorylation of STAT92E. It also suppresses both constitutive and IL-6-induced phosphorylation of STAT3 while decreasing levels of tyrosine-phosphorylated JAK3. Furthermore, AUH-6-96 induces apoptosis in cancer cells by downregulating anti-apoptotic genes downstream of STAT3, selectively reducing the viability of cancer cells with dysregulated JAK/STAT signaling. This compound is relevant for research pertaining to Hodgkin's lymphoma, breast cancer, and prostate cancer. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-2 is a dual-target inhibitor of Janus kinase (JAK) and histone deacetylase (HDAC), specifically inhibiting HDAC3/6 and JAK1/2 with nanomolar potency. This compound demonstrates proapoptotic activity by inhibiting histone deacetylation and STAT3 phosphorylation, contributing to its mechanism of action. JAK/HDAC-IN-2 exhibits significant antiproliferative effects in various hematological malignancies and solid tumors, making it a valuable tool for cancer research and therapeutic studies. -
JAK2/Bcr-Abl/FLT3 Inhibitor
LS-104 is a non-ATP-competitive inhibitor targeting JAK2, Bcr-Abl, and FLT3. It effectively induces apoptosis in JAK2V617F-positive cells while inhibiting JAK2 autophosphorylation and downstream signaling pathways. Additionally, LS-104 demonstrates significant cytotoxic effects and inhibits the proliferation of FLT3-expressing leukemic cells. This hydroxystyryl-acrylonitrile compound holds potential for research into myeloproliferative disorders and refractory or relapsed hematologic malignancies. -
JAK3 Inhibitor
PRN-371 is a potent and selective inhibitor of JAK3. By disrupting the JAK3-STAT signaling pathway, PRN-371 effectively suppresses the proliferation of natural killer and T-cell lymphoma cells, inducing apoptosis in these malignancies. This compound demonstrates significant antitumor activity and is applicable in the research of various cancer types, particularly hematological malignancies. -
JAK2 Inhibitor
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. -
JAK3 Inhibitor
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. -
Anticancer Agent
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. -
JAK2/STAT3 Inhibitor
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. -
FLT3/JAK2 Inhibitor
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. -
JAK2/STAT3 Inhibitor
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-Inhibitor
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. -
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. - 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.
