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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR Inhibitor
Cucurbitacin IIa is a potent EGFR inhibitor with an IC50 of 1.455 nM, demonstrating effective modulation of the EGFR signaling pathway. This compound induces caspase-3-dependent apoptosis, downregulates survivin expression, and enhances autophagy, while disrupting the actin cytoskeleton and arresting the cell cycle at the G2/M phase. Additionally, Cucurbitacin IIa exhibits anti-inflammatory properties, making it a valuable tool for research into inflammation-related diseases, depression, and various cancers, including non-small cell lung cancer. -
RIPK2/ALK2 Inhibitor
OD36 hydrochloride is a potent inhibitor of receptor-interacting protein kinase 2 (RIPK2) and an effective modulator of activin receptor-like kinase 2 (ALK2), exhibiting an IC50 of 5.3 nM against RIPK2. This macrocyclic compound demonstrates strong binding affinity for the ALK2 kinase ATP pocket, with a Kd of 37 nM. OD36 hydrochloride is suitable for research applications focused on signaling pathways involving RIPK2 and ALK2, relevant in studying various diseases, including inflammation and cancer. -
FLT3 Inhibitor
AKN-028 is a potent inhibitor of FMS-like receptor tyrosine kinase 3 (FLT3), demonstrating an IC50 value of 6 nM and effectively inhibiting FLT3 autophosphorylation. This orally active compound elicits a dose-dependent cytotoxic effect, with a mean IC50 of 1 μM. AKN-028 promotes apoptosis through the activation of caspase 3, making it particularly relevant for research on acute myeloid leukemia (AML) and related hematological malignancies. -
BCR-ABL Inhibitor
VS1150 is a BCR-ABL inhibitor that induces inhibitory phosphorylation at the Y253 site, effectively disrupting oncogenic BCR-ABL signaling with an EC50 of 69 nM. This compound not only targets the BCR-ABL fusion protein but also demonstrates inhibitory effects on other oncogenic ABL fusions and drug-resistant mutants, such as T315I. VS1150 is suitable for research applications related to chronic myeloid leukemia (CML) and other cancers driven by ABL fusions. -
RIPK2/ALK2 Inhibitor
OD36 is a selective inhibitor of RIPK2 with an IC50 of 5.3 nM, demonstrating potent binding affinity to the ATP pocket of the ALK2 kinase, with a KD of 37 nM. This macrocyclic compound exhibits specific ALK2-directed activity, making it a valuable tool for investigating the roles of these kinases in various biological pathways. Research applications include the exploration of inflammatory signaling and potential therapeutic interventions in related diseases. -
RIPK2/ALK2 Inhibitor
RIPK2-IN-1 is a selective inhibitor targeting RIPK2 and ALK2, with an IC50 of 51 nM and 5 nM, respectively. This compound demonstrates substantial efficacy in modulating RIPK2/NOD2 pathways, exhibiting an IC50 of 390 nM in cellular assays. RIPK2-IN-1 is suitable for research applications investigating pathways related to inflammation and immune response mechanisms. -
ALKBH5 Inhibitor
ALKBH5-IN-5 is a selective inhibitor of ALKBH5 with an IC50 of 0.62 μM and a Kd of 804 nM. This compound disrupts the interaction between ALKBH5 and its substrates, m6A-RNA and 6mA-DNA, leading to enhanced differentiation and apoptosis in cancer cells, as well as G2-M phase arrest. Notably, ALKBH5-IN-5 reduces the protein levels of TACC3 and MYC while increasing cleaved caspase-3 levels, demonstrating significant antiproliferative effects. Furthermore, it exhibits antitumor activity in xenograft mouse models and is relevant for research into acute myeloid leukemia. -
RAF-1/HIF-1α Inhibitor
MO-2097 is a selective RAF-1 and HIF-1α inhibitor that induces the destabilization of RAF-1, resulting in decreased levels of epithelial-mesenchymal transition (EMT) transcription factors and mesenchymal markers. Additionally, MO-2097 effectively inhibits HIF-1α protein expression mediated by hnRNPA2B1 in hypoxic conditions. This compound promotes the generation of mitochondrial reactive oxygen species (ROS), contributing to apoptosis in malignant cells. MO-2097 demonstrates significant potential in suppressing colorectal cancer metastasis by targeting the RAF/MEK/ERK signaling pathway and has shown efficacy in reducing tumor growth in HCT116 cell xenograft mouse models, thus serving as a valuable tool for colorectal cancer research. -
HIF2α Inhibitor
HIF-2α-IN-17 is a selective inhibitor of hypoxia-inducible factor 2α (HIF2α) that targets the PAS-B domain, effectively disrupting its interaction with the molecular chaperone Hsp70. This interference promotes the proteasomal degradation of HIF2α, leading to significant antitumor activity and the induction of apoptosis in cancer cells. HIF-2α-IN-17 is primarily utilized in research focused on malignancies such as clear cell renal cell carcinoma. -
FLT3 Inhibitor
AKN-028 TFA is a potent and orally active inhibitor of FMS-like receptor tyrosine kinase 3 (FLT3), exhibiting an IC50 value of 6 nM. This compound effectively inhibits FLT3 autophosphorylation and elicits a dose-dependent cytotoxic response with a mean IC50 of 1 μM. Additionally, AKN-028 TFA induces apoptosis through the activation of caspase 3. It is a valuable tool for research in acute myeloid leukemia (AML). -
ALK Inhibitor
ALK-IN-26 is a selective inhibitor of the anaplastic lymphoma kinase (ALK) with an IC50 value of 7.0 μM for ALK tyrosine kinase. This compound exhibits favorable pharmacokinetic properties and demonstrates permeability across the blood-brain barrier. ALK-IN-26 has been shown to induce apoptosis, autophagy, and necrosis, making it a valuable tool in the study of glioblastoma and related malignancies. -
FAK Inhibitor
PND-1186 hydrochloride is a potent and selective inhibitor of Focal Adhesion Kinase (FAK) with an IC50 value of 1.5 nM. This reversible inhibitor has been shown to promote apoptosis in tumor cells, making it a valuable tool in cancer research. PND-1186 hydrochloride is applicable in investigations aimed at understanding FAK's role in tumor progression and therapeutic resistance. -
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. -
FLT3 Inhibitor
Quizartinib dihydrochloride is a potent and selective second-generation type II FLT3 tyrosine kinase inhibitor. Demonstrating a Kd of 1.6 nM, it effectively inhibits autophosphorylation of both wild-type FLT3 and FLT3-ITD in MV4-11 cells, with IC50 values of 4.2 nM and 1.1 nM, respectively. This compound is also suitable for the development of PROTAC FLT3 degraders when linked to the VHL ligand, and it has been shown to induce apoptosis in target cells. -
Pan-FLT3/Pan-BTK Inhibitor
Luxeptinib is a first-in-class, non-covalent pan-FLT3 and pan-BTK inhibitor that exhibits potent oral activity. This compound effectively induces cell cycle arrest, apoptosis, or autophagy in acute myeloid leukemia cells, making it a significant tool for cancer research. Its dual-targeting mechanism positions Luxeptinib as a potential therapeutic candidate in the treatment of hematological malignancies. -
Syk Inhibitor
BAY 61-3606 hydrochloride is a highly selective Syk inhibitor that acts in an ATP-competitive manner with a Ki of 7.5 nM and an IC50 of 10 nM. It effectively reduces ERK1/2 and Akt phosphorylation in neuroblastoma cells and significantly decreases Syk phosphorylation in K-rn cell lysates. Additionally, BAY 61-3606 hydrochloride enhances TRAIL-induced apoptosis in breast cancer cells by downregulating Mcl-1, making it a valuable tool for investigating Syk-related pathways in cancer research. -
ALK/FAK/ROS1 Multikinase Inhibitor
APG-2449 is an orally active inhibitor targeting BCL-2 and multikinase pathways, specifically ALK, FAK, and ROS1. It demonstrates potent antitumor activity by reducing cell viability and enhancing apoptosis in acute myeloid leukemia cells in vitro. APG-2449 effectively decreases the activation of FAK and its downstream signaling effectors. This compound is suitable for research applications in various malignancies, including mesothelioma, non-small cell lung cancer, ovarian cancer, and other hematologic and solid tumors. -
p210Bcr-Abl Kinase Inhibitor
PD180970 is a potent ATP-competitive inhibitor of the p210Bcr-Abl kinase, exhibiting an IC50 of 5 nM for the inhibition of its autophosphorylation. Additionally, it inhibits Src and KIT kinases with IC50 values of 0.8 nM and 50 nM, respectively. PD180970 effectively induces apoptosis in K562 leukemic cells, making it a valuable reagent for research on chronic myelogenous leukemia. -
ALKBH5 Inhibitor
W23-1006 is a selective and covalent inhibitor of ALKBH5, targeting the C200 residue with an IC50 of 3.848 μM. This compound exhibits approximately 30-fold and 8-fold greater inhibitory activity against ALKBH5 compared to FTO and ALKBH3, respectively. W23-1006 is particularly valuable for research applications focusing on triple-negative breast cancer (TNBC), enabling studies on the role of ALKBH5 in tumor biology and potential therapeutic strategies. -
FAK Inhibitor
YH-306 is a selective FAK (Focal Adhesion Kinase) inhibitor that exhibits potent antitumor activity. It effectively suppresses colorectal tumor growth and metastasis by inhibiting key signaling pathways, leading to significant reductions in the migration and invasion of colorectal cancer cells. YH-306 also induces apoptosis and inhibits the proliferation of cancer cells by disrupting the activation of FAK, c-Src, paxillin, and downstream effectors such as PI3K and Rac1, while downregulating MMP2 and MMP9 expression. Additionally, this compound impedes actin polymerization mediated by the Arp2/3 complex, contributing to its antitumor effects. -
FAK Inhibitor
GSK-2256098 hydrochloride is a selective inhibitor of focal adhesion kinase (FAK), known for its antiangiogenic and antineoplastic properties. By targeting FAK, it effectively disrupts tumor cell growth through the modulation of key cellular processes, including adhesion, migration, proliferation, and survival. This compound is valuable for researchers investigating the mechanisms of cancer progression and the development of potential therapeutic strategies. -
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. -
p210bcr/abl Inhibitor
Adaphostin, a potent inhibitor of the p210bcr/abl fusion protein (IC50 = 14 μM), exhibits significant anti-leukemic activity. It induces apoptosis in T-lymphoblastic leukemia cell lines, with IC50 values ranging from 17 to 216 nM. This compound demonstrates selective efficacy against both chronic and acute myeloid leukemia cells and increases reactive oxygen species (ROS) levels in chronic lymphocytic leukemia (CLL) B cells, making it valuable for research in leukemia therapeutics and cellular pathways related to oxidative stress. -
Bcr-Abl Inhibitor
HG-7-85-01 is a type II ATP competitive inhibitor that targets Bcr-Abl, including its T315I mutant, as well as PDGFRα, Kit, and Src kinases. It demonstrates potent inhibition with IC50 values of 3 nM for T315I Bcr-Abl, 20 nM for KDR, and 30 nM for RET, while showing minimal activity against other kinases (IC50 > 2 μM). HG-7-85-01 effectively inhibits cell proliferation through the induction of apoptosis and the suppression of cell-cycle progression, making it a valuable tool for research in cancer biology. -
Syk Inhibitor
PRT062607 acetate is a potent Syk inhibitor with an IC50 of 1 nM, designed for oral administration. This compound effectively inhibits inflammatory pathways and induces apoptosis, demonstrating significant antitumor activity in tumor xenograft mouse models. It serves as a valuable tool in cancer research and the study of Syk-mediated signaling. -
FAK Inhibitor
FAK-IN-2 is a potent inhibitor of focal adhesion kinase (FAK), exhibiting a reported IC50 of 35 nM. This compound effectively covalently modifies and inhibits the autophosphorylation of FAK, leading to significant inhibition of tumor cell migration and clonal formation. Additionally, FAK-IN-2 induces apoptosis in cancer cells, highlighting its potential utility in oncological research and therapeutic applications targeting FAK signaling pathways. -
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. -
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. -
Btk Inhibitor
LFM-A13 is a selective Bruton's tyrosine kinase (BTK) inhibitor known for its capacity to inhibit JAK2 and PLK. With IC50 values of 2.5 μM for recombinant BTK, 10 μM for JAK2, and 61 μM for PLK3, LFM-A13 exhibits significant antiproliferative and anticancer properties. This compound is valuable for research applications focused on cancer biology and therapeutic interventions targeting BTK and related signaling pathways. -
SYK Inhibitor
GSK2646264 is a potent and selective inhibitor of spleen tyrosine kinase (SYK), exhibiting a pIC50 value of 7.1. This compound also shows inhibitory activity against several other kinases, including LCK, LRRK2, GSK3β, JAK2, VEGFR2, and Aurora kinases, with varying pIC50 values. Due to its ability to penetrate the epidermis and dermis, GSK2646264 is potentially valuable for research applications in dermatological conditions and immune responses. -
JAK2/FLT3 Inhibitor
Pacritinib hydrochloride is a selective inhibitor targeting JAK2 and FLT3, demonstrating inhibitory potency against wild-type JAK2 (IC50=23 nM), the JAK2V617F mutant (IC50=19 nM), and FLT3 (IC50=22 nM) as well as the FLT3D835Y mutant (IC50=6 nM). This compound is primarily utilized in research related to acute myeloid leukemia (AML) and myelofibrosis (MF), making it a valuable tool for studying these hematological malignancies and the associated signaling pathways. -
SYK/JAK Inhibitor
Gusacitinib hydrochloride is a potent dual inhibitor of SYK and JAK kinases, demonstrating IC50 values of 5 nM, 46 nM, 4 nM, 11 nM, and 8 nM for SYK, JAK1, JAK2, JAK3, and TYK2, respectively. This compound effectively suppresses critical inflammatory pathways linked to the pathogenesis of atopic dermatitis. Gusacitinib hydrochloride is suitable for research applications involving chronic hand eczema and various cancers, including basal cell carcinoma. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-3 is a selective inhibitor of Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). Targeting both JAK3 and BTK can provide synergistic effects beneficial for the therapeutic intervention of autoimmune diseases. This compound is suitable for research applications focused on elucidating the roles of JAK3 and BTK in various disease mechanisms, facilitating the development of novel treatment strategies. -
JAK2/FLT3 Inhibitor
SB1578 is a selective inhibitor of JAK2 and FLT3, exhibiting IC50 values of 46 nM and 60 nM, respectively. This compound demonstrates high selectivity for other kinase targets, making it a valuable tool for research. SB1578 is particularly useful in studying non-oncological indications, such as rheumatoid arthritis, offering insights into potential therapeutic applications in inflammatory diseases. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-7 is a potent inhibitor targeting Janus kinase 3 (JAK3) and Bruton’s tyrosine kinase (BTK), demonstrating IC50 values of 2 nM and 14 nM, respectively. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for investigating the underlying mechanisms of rheumatoid arthritis. Its efficacy in modulating inflammatory pathways highlights its potential in related therapeutic research applications. -
CDK2/JAK2/FLT3 Inhibitor
Zotiraciclib hydrochloride is a novel small molecule inhibitor targeting cyclin-dependent kinase 2 (CDK2), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase 3 (FLT3). This reagent demonstrates anti-tumor activity by downregulating the Myc oncogene through CDK9 inhibition, contributing to reduced tumor growth. Zotiraciclib hydrochloride is particularly relevant for research into cancers capable of crossing the blood-brain barrier, and elevated levels of the MCL-1 protein may indicate its potential as a prognostic marker and therapeutic target in cancer studies. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-2 is a potent dual inhibitor of Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). By simultaneously targeting the BTK/JAK3 signaling pathway, this compound demonstrates synergistic effects that may enhance therapeutic outcomes in autoimmune diseases. JAK3/BTK-IN-2 is suitable for research applications focused on JAK3 and BTK-related pathologies, facilitating studies on their roles in immune regulation and disease progression. -
Multi-kinase Inhibitor
Debio 0617B is a multi-kinase inhibitor that targets key kinases involved in the regulation of STAT3/STAT5 signaling, including JAK, SRC, ABL, and class III/V receptor tyrosine kinases. This compound effectively reduces the maintenance and self-renewal of primary human acute myeloid leukemia (AML) CD34+ stem/progenitor cells. Additionally, Debio 0617B has demonstrated efficacy in preclinical models of STAT3-driven solid tumors, making it a valuable tool for cancer research and therapeutic development. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-5 is a potent dual inhibitor targeting Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). This compound effectively disrupts the BTK/JAK3 signaling pathway, demonstrating potential synergistic effects advantageous for the treatment of autoimmune diseases. JAK3/BTK-IN-5 is valuable for research into conditions related to JAK3 kinase and BTK, making it a crucial tool for studying the pathophysiology of these targets. -
FLT3 Inhibitor
JI6 is a potent and selective FLT3 inhibitor, exhibiting IC50 values of approximately 40 nM for FLT3-WT, 8 nM for FLT3-D835Y, and 4 nM for FLT3-D835H. Additionally, JI6 demonstrates inhibitory activity against JAK3 and c-Kit, with IC50 values of around 250 nM and 500 nM, respectively. This compound serves as a valuable tool for research applications focused on acute myeloid leukemia. -
BTK/JAK3 Inhibitor
JAK3/BTK-IN-6 is a potent dual inhibitor targeting Bruton's Tyrosine Kinase (BTK) and Janus Kinase 3 (JAK3), exhibiting IC50 values of 0.6 nM and 0.4 nM, respectively. This compound demonstrates excellent metabolic stability in human liver microsomes, making it suitable for in vitro studies. JAK3/BTK-IN-6 is valuable in research applications related to hematological disorders and immune system dysfunctions. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-4 is a potent inhibitor targeting both JAK3 and BTK kinases, which are critical in the modulation of immune responses involved in autoimmune diseases. By simultaneously inhibiting the BTK/JAK3 signaling pathway, JAK3/BTK-IN-4 demonstrates synergistic effects, making it a valuable tool for studying JAK3 and BTK-related pathologies. This compound is particularly relevant for research applications focused on therapeutic strategies for autoimmune disorders. -
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. -
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. -
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. -
FGFR3 Inhibitor
Dabogratinib is a selective inhibitor of FGFR3, displaying an IC50 of 11 nM. It demonstrates significant antitumor activity against urothelial carcinoma and various solid tumors by downregulating FGFR3 and ERK1/2 signaling pathways, leading to tumor growth inhibition and regression in FGFR3-altered xenograft models. Additionally, Dabogratinib enhances chondrocyte proliferation and differentiation, promotes endochondral bone formation, and improves craniofacial and spinal morphology. This compound is valuable for research into metastatic urothelial carcinoma, achondroplasia, and hypochondroplasia. -
FGFR2 Inhibitor
FGFR2-IN-2 is a selective inhibitor of fibroblast growth factor receptor 2 (FGFR2), demonstrating inhibitory potency with an IC50 value of 29 nM against FGFR2, and 389 nM and 758 nM for FGFR1 and FGFR3, respectively. This compound exhibits potential in the study of FGFR-related signaling pathways and can be utilized in research focused on cancer therapeutics, particularly in tumors with aberrant FGFR2 activity. -
FGFR Inhibitor
FIIN-1 is a selective, irreversible inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2, FGFR3, and FGFR4). It exhibits potent binding affinity, with Kd values of 2.8 nM for FGFR1, 6.9 nM for FGFR2, 5.4 nM for FGFR3, and 120 nM for FGFR4, alongside Kd values of 32 nM and 120 nM for Flt1 and Flt4, respectively. With biochemical IC50 values of 9.2 nM for FGFR1, 6.2 nM for FGFR2, 11.9 nM for FGFR3, and 189 nM for FGFR4, FIIN-1 is valuable for research applications focused on FGFR-related pathways in cancer and developmental biology. -
FGFR1 Inhibitor
FGFR1 inhibitor-10 is a potent FGFR1 inhibitor with an IC50 value of 28 nM. It effectively inhibits the phosphorylation of FGFR1, leading to significant anti-angiogenic, anti-invasive, and anti-tumor activities. This compound is valuable for research applications focused on understanding FGFR1 signaling pathways and developing therapies for cancers characterized by aberrant FGFR1 activity.
