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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR Inhibitor
Gefitinib hydrochloride is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR. -
VEGFR/EGFR inhibitor
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. -
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. -
PIM-1 Inhibitor
PIM-1 inhibitor 2 is a potent Pim-1 kinase inhibitor (Ki = 91 nM). -
Pim-1 Kinase Inhibitor
TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM). -
EGFR inhibitor
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. -
EGFR inhibitor
AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR). It binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. -
STAT3 inhibitor
Corylifol A is a phenolic compounds isolated from Psoralea corylifolia; inhibits IL-6-induced STAT3 activation and phosphorylation(IC50=0.8 uM). -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib is a potent multi-targeted kinase inhibitor that primarily targets c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This orally active compound demonstrates significant antitumor activity in human gastric cancer cells and xenograft models. Famitinib also induces apoptosis, making it a valuable tool for research in cancer therapeutics and signaling pathways. -
PIM Kinase Inhibitor
PIM-447 dihydrochloride is a potent and selective pan-PIM kinase inhibitor targeting PIM1, PIM2, and PIM3 with Ki values of 6, 18, and 9 pM, respectively. This compound exhibits significant antimyeloma activity and protective effects on bone tissue. PIM-447 dihydrochloride also induces apoptosis, making it a valuable tool for research into cancer therapies and bone disease studies. -
Stat5a/b Inhibitor
IST5-002 is a selective inhibitor of Stat5a and Stat5b, with IC50 values of 1.5 μM and 3.5 μM, respectively. This compound effectively disrupts the transcriptional activity of Stat5 proteins, inducing apoptosis in prostate cancer and chronic myeloid leukemia (CML) cells. IST5-002 is suitable for research applications focused on understanding the role of Stat5 in cancer progression and therapeutic targeting in prostate cancer and CML. -
STAT3 Inhibitor
Danvatirsen is an antisense oligonucleotide that specifically inhibits STAT3, a transcription factor involved in cell survival and proliferation. This compound reduces cell viability and promotes apoptosis in leukemia cell lines, while downregulating the expression of endogenous STAT3 and its downstream target genes. Additionally, Danvatirsen effectively diminishes proliferation and tumorigenicity in models of neuroblastoma and lymphoma. In vivo studies demonstrate its capacity to inhibit tumor growth rates in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen is applicable in research focused on lymphoma, myelodysplastic syndrome, acute myeloid leukemia, and neuroblastoma. -
STAT3 Inhibitor
HP590 is a potent, orally active inhibitor of STAT3, demonstrating an IC50 of 27.8 nM for STAT3 luciferase activity and 24.7 nM for ATP inhibition. This compound exhibits significant anti-proliferative effects on gastric cancer cells and effectively induces apoptosis. HP590 serves as a valuable research tool for investigating the role of STAT3 in cancer biology and potential therapeutic interventions. -
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. -
STAT3 Signal Inhibitor
STAT3-IN-12 is a potent inhibitor of the STAT3 signaling pathway, effectively blocking IL-6 induced JAK/STAT3 activation. This compound exhibits significant anti-cancer activity by inhibiting cell growth, reducing migration, promoting apoptosis, and inducing cell cycle arrest. STAT3-IN-12 is particularly relevant for research applications in cancers such as hepatocellular carcinoma (HCC) and esophageal carcinoma. -
STAT3 Phosphorylation Inhibitor
Tetramethylcurcumin is a selective inhibitor of STAT3 phosphorylation, targeting Janus kinase 2 and the Src homology-2 domain of STAT3. This compound demonstrates significant anti-inflammatory and anti-cancer properties, making it a valuable tool for research into cancer biology and inflammatory pathways. Its ability to modulate key signaling events provides insight into therapeutic strategies for diseases driven by aberrant STAT3 activity. -
GBP1:PIM1 Interaction Inhibitor
NSC756093 is a GBP1:PIM1 interaction inhibitor with a binding affinity of 38 nM. This compound demonstrates significant biological activity by suppressing cell proliferation, reducing migration, inducing G1 phase cell-cycle arrest, and promoting apoptosis in ovarian cancer cells. Additionally, NSC756093 decreases proteasomal activity and leads to the accumulation of ubiquitinated proteins, thereby inhibiting tumor progression and lung metastasis in murine ovarian cancer xenograft models. Furthermore, it enhances sensitivity of prostate cancer cells to Docetaxel and sensitizes GBP1-overexpressing ovarian cancer cells to Paclitaxel, making it a valuable reagent for research in prostate and ovarian cancer. -
STAT3 Inhibitor
STAT3-IN-11 is a selective inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3), specifically targeting the phosphorylation at Tyr705. This compound downregulates the phosphorylation of downstream genes such as Survivin and Mcl-1, while leaving upstream tyrosine kinases like Src and JAK2 unaffected. By inducing apoptosis in cancer cells, STAT3-IN-11 presents potential as a valuable tool for research in cancer therapeutics and the development of effective STAT3 inhibitors. -
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. -
STAT3-SH2 Domain Inhibitor
STAT3-SH2 Domain Inhibitor 1 specifically targets the Src Homology 2 (SH2) domain of STAT3, exhibiting a Kd value of 1.57 μM. This compound effectively inhibits STAT3 signaling and transcriptional activation, leading to apoptosis in gastric cancer cells. It serves as a valuable tool for researching mechanisms of cancer progression and potential therapeutic strategies targeting the STAT3 pathway. -
STAT3 Inhibitor
8-Epixanthatin is a STAT3 inhibitor derived from Xanthium chinese Mill. It effectively inhibits STAT3 activation, leading to the induction of apoptosis in cancer cells. This compound demonstrates notable anti-tumor activity, making it a valuable tool for research applications focused on cancer biology and therapeutic development. -
STAT3 Inhibitor
WB436B is a selective inhibitor of STAT3, targeting STAT3-Tyr705 phosphorylation and modulating the expression of downstream STAT3 target genes. This compound exhibits significant cytotoxicity against pancreatic cancer cells while promoting apoptosis. In preclinical mouse models, WB436B has been shown to suppress tumor growth and metastasis, leading to an extended survival rate in tumor-bearing subjects. This makes WB436B a valuable tool for research in cancer biology and therapeutic development. -
STAT3 Inhibitor
HJC0416 hydrochloride is a potent inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3) that exhibits enhanced anticancer properties compared to Stattic. This compound has demonstrated significant biological activity against breast cancer, making it a promising candidate for cancer research applications. Its oral bioavailability and efficacy highlight its potential as a valuable tool for investigating STAT3-related pathways in oncology. -
EGFR Inhibitor
EGFR-IN-86 is a potent EGFR inhibitor, exhibiting an IC50 of 1.5 nM. It demonstrates significant biological activity against glioblastoma by inducing apoptosis and causing cell cycle arrest in the G2/M phase in U87 cells. This compound serves as a valuable tool for research focused on targeting EGFR in cancer therapy. -
STAT3 Inhibitor
SC99 is a selective inhibitor of the STAT3 pathway, exerting its effects through the inhibition of JAK2. By binding to the ATP-binding pocket of JAK2, SC99 effectively prevents the phosphorylation of both JAK2 and STAT3, while sparing other kinases linked to STAT3 signaling. SC99 demonstrates significant biological activity, including the inhibition of platelet activation and aggregation, as well as potent anti-myeloma and anti-thrombotic effects, making it a valuable tool for research in cancer and cardiovascular studies. -
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. -
STAT3 Inhibitor
LLL3 is a potent STAT3 inhibitor that effectively impedes the dimerization and phosphorylation of STAT3, thereby blocking its translocation into the nucleus. This mechanism leads to reduced expression of STAT3-dependent genes, including those encoding Bcl-xL and cyclin D1. Moreover, LLL3 has been shown to induce growth inhibition and apoptosis in human breast cancer and rhabdomyosarcoma cells through the activation of the caspase pathway. This reagent is valuable for investigating cancers associated with persistent STAT3 activation. -
STAT5b Inhibitor
Pomstafib-2 is a potent and selective inhibitor of STAT5b, a transcription factor involved in various signaling pathways. This compound reduces the expression of phosphorylated STAT5b (pSTAT5b) and promotes apoptotic processes in cells. Pomstafib-2 is valuable for studying STAT5b-related biological functions and developing therapies targeting STAT5b-driven malignancies. -
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.
