Catalog No.
Product Name
Application
Product Information
Citations
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Brigatinib-PROTAC Degrader
SIAIS117 is a potent Brigatinib-PROTAC degrader that targets the ALK protein, specifically effective against the ALK G1202R point mutation. By utilizing a VHL-1 conjugation, SIAIS117 exhibits significant capability to induce protein degradation, leading to inhibited growth of SR and H2228 cancer cell lines. This compound holds potential for applications in anti-proliferative research, particularly in small cell lung cancer contexts. -
ALK Inhibitor
Con B-1 is a potent and selective inhibitor of anaplastic lymphoma kinase (ALK), exhibiting low toxicity towards normal cells. This compound effectively modulates ALK activity, making it valuable for research into ALK-driven cancers. It is suitable for use in studies related to targeted therapies and evaluation of cancer cell proliferation and survival pathways. -
ALK Inhibitor
(E)-Belizatinib is a potent and selective anaplastic lymphoma kinase (ALK) inhibitor, exhibiting an enzymatic IC50 of 0.005 μM and a cellular IC50 of 0.048 μM. Demonstrating over 61-fold selectivity for ALK over JAK2, SRC, and IGF1R, (E)-Belizatinib possesses favorable pharmacokinetic properties in both rats and dogs. This compound is valuable for research focused on ALK-driven cancers, offering significant potential for therapeutic development in this area. -
ALK5 Inhibitor
ALK5-IN-79 is a selective ALK5 inhibitor that interferes with TGF-β1/SMAD signaling pathways, exhibiting significant anticancer activity. This compound reduces extracellular matrix production and collagen deposition, making it pertinent for studies focused on fibrosis and cancer progression. ALK5-IN-79 demonstrates favorable pharmacokinetic properties and good in vivo tolerance, supporting its potential as a therapeutic agent in various research applications. -
Anaplastic lymphoma kinase (ALK) Inhibitor
KRCA-0713 is a potent inhibitor of anaplastic lymphoma kinase (ALK), demonstrating robust anti-ALK activity in both enzyme and cell-based assays. This compound effectively suppresses ALK-driven tumor growth, as evidenced by studies conducted in H3122 xenograft models. KRCA-0713 serves as a valuable tool for researchers investigating ALK-related oncogenesis and therapeutic responses in cancer treatment. -
ALK Inhibitor
ALK5-IN-26 is a potent inhibitor of Activin receptor-like kinase 5 (ALK5), exhibiting an IC50 value of ≤10 nM. This compound is valuable for research applications investigating the role of ALK5 in cancer progression and related pathways. Its high specificity and efficacy make it a useful tool for elucidating the mechanistic underpinnings of tumor biology. -
ALK Inhibitor
WZH-15-125 is a potent anaplastic lymphoma kinase (ALK) inhibitor, showing significant activity against compound ALK mutations that contribute to drug resistance. With an IC50 of 101.7 nM, it effectively targets the G1202R/L1196M mutation, which demonstrates resistance to Lorlatinib. WZH-15-125 serves as a valuable ligand for PROTAC synthesis, specifically for the development of PROTAC WZH-17-002. This compound is particularly relevant for research in non-small cell lung cancer, offering new avenues for therapeutic exploration. -
ALK inhibitor
ALK-IN-13 is a selective inhibitor of anaplastic lymphoma kinase (ALK), targeting key pathways involved in oncogenesis. This compound exhibits potent anti-tumor activity, making it valuable for research focused on ALK-driven cancers, including non-small cell lung cancer. Its mechanism of action allows for detailed studies of ALK signaling and the development of targeted therapeutic strategies. -
ALK Degrader
PROTAC ALK degrader-1 is a potent ALK degrader utilizing the proteolysis-targeting chimera (PROTAC) mechanism, exhibiting a DC50 of 26 nM in H3122 EML4-ALK cells. This compound enables selective degradation of ALK, thereby offering potential therapeutic benefits for ALK-driven cancers. Additionally, PROTAC ALK degrader-1 serves as a precursor for synthesizing PROTAC ALK degrader-2, which may possess enhanced bioavailability for further research applications. -
ALK Inhibitor
F6524-1593 is an ALK inhibitor that demonstrates significant inhibitory activity against A549 and HepG-2 cell lines, with IC50 values of 161.1 μM and 91.03 μM, respectively. This compound is valuable for research involving ALK-related malignancies, including non-small cell lung cancer, lymphoma, and neuroblastoma. Its ability to selectively target ALK makes it a potential tool for understanding and developing treatments for these cancers. -
ALK PROTAC Degrader
PROTAC ALK degrader-5 is a targeted degrader composed of a small molecule that selectively degrades anaplastic lymphoma kinase (ALK). It demonstrates potent inhibitory activity against EML4-ALK and NPM-ALK, with IC50 values of 27.4 nM and 116.5 nM, respectively. This compound exhibits significant anti-proliferative effects against ALK-driven cancer cell lines, including H3122 and Karpas 299, and effectively inhibits ALK and STAT3 phosphorylation. PROTAC ALK degrader-5 is a valuable tool for investigating ALK-driven malignancies, particularly in the context of human non-small cell lung cancer and anaplastic large cell lymphoma research. -
ALK Inhibitor
ALK-IN-21 is a potent inhibitor of the anaplastic lymphoma kinase (ALK), specifically targeting the ALKG1202R mutation. It demonstrates exceptional enzymatic inhibitory potency, with IC50 values of 4.59 nM for ALKWT, 2.07 nM for ALKL1196M, and 5.95 nM for ALKG1202R. This compound effectively inhibits the proliferation of ALK-positive Karpas299 and H2228 cell lines, exhibiting IC50 values of 0.07 μM. ALK-IN-21 is essential for research on anaplastic large cell lymphoma and related ALK-driven malignancies. -
ALK PROTAC Degrader
TD-004 is a highly effective ALK PROTAC degrader, demonstrating potent anti-ALK inhibitory activity with an IC50 of 0.11 µM. This compound selectively hampers the proliferation of ALK-positive cancer cell lines, SU-DHL-1 and H3122, with IC50 values of 0.058 µM and 0.28 µM, respectively. TD-004 induces the degradation of ALK fusion proteins, including NPM-ALK and EML4-ALK, through the recruitment of the VHL E3 ligase and the proteasome pathway. Its significant tumor growth inhibition and favorable safety profile in vivo make TD-004 a valuable tool for researching anaplastic large cell lymphoma and non-small cell lung cancer. -
ALK Inhibitor
ALK5-IN-29 is a selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating potent inhibitory activity with an IC50 value of ≤10 nM. This compound has been shown to effectively inhibit tumor growth, making it a valuable tool for research in proliferative diseases, including cancer. Its specificity for ALK5 allows for targeted studies examining the role of this kinase in various biological processes and therapeutic interventions. -
ALK ligand-Linker Conjugate
ALK ligand-Linker Conjugate 1 is designed to facilitate the synthesis of PROTAC ALK degrader-4, targeting the Anaplastic Lymphoma Kinase (ALK) pathway. This compound serves as a vital component in developing protein-targeting chimeras for therapeutic applications in cancer research. Its efficient linkage promotes effective degradation of ALK, making it a valuable tool for studies focused on modulating oncogenic signaling pathways. -
ALK Inhibitor
Dirozalkib is a potent ALK inhibitor with an IC50 value of 0.9 nM. It demonstrates significant anti-proliferative activity in cancer cell lines, including NCI-H3122, Karpas-299, and NCI-H2228, with IC50 values of 130.4, 0.71, and 15.11 nM, respectively. Dirozalkib also possesses favorable pharmacokinetic properties, with a bioavailability of 30% to 50%, making it a valuable tool for research in cancer therapeutics. -
ALK Inhibitor
TL13-110 is a selective ALK inhibitor that demonstrates an IC50 of 0.34 nM. This compound serves as a negative control for TL13-112 while exhibiting minimal interaction with cellular ALK degradation. TL13-110 is suitable for research applications focused on the exploration of ALK-related pathways and therapeutic strategies in oncology. -
ALK2 Inhibitor
CDD-2789 is a highly selective small-molecule inhibitor of Activin receptor type 1 (ALK2, or ACVR1), which targets the SMAD1/5 signaling pathway. By effectively blocking ALK2/ALK1-mediated phosphorylation events triggered by BMP and activin A, CDD-2789 demonstrates a potent inhibitory effect with an IC50 of 0.54 µM in the NanoBRET cellular model. This compound is invaluable for research into ALK2-associated diseases, such as diffuse intrinsic pontine glioma (DIPG), ependymoma, endometrial cancer, melanoma, non-small cell lung cancer, colorectal cancer, and pancreatic cancer. -
ALK Inhibitor
KRCA-0377 is an orally active inhibitor of anaplastic lymphoma kinase (ALK) that demonstrates potent activity with an IC50 of 0.001 μM against the wild-type enzyme, and ≤0.01 μM for mutant forms. This compound exhibits significant cytotoxic effects against cancer cells and effectively inhibits tumor growth in xenograft mouse models. KRCA-0377 is suitable for research applications focusing on ALK-positive non-small-cell lung cancer. -
ALK/EGFR Inhibitor
ALK/EGFR-IN-2 is a potent dual inhibitor targeting anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR). This compound induces apoptosis and causes G0/G1 cell cycle arrest in cancer cells, contributing to its efficacy. It demonstrates significant inhibition of cell proliferation in H1975, PC9, and Baf3-EML4-ALK cancer cell lines, with IC50 values of 0.0034, 0.0065, and 0.0018 μM, respectively. ALK/EGFR-IN-2 is valuable for research focused on cancer therapeutics and pathway analysis. -
ALK Inhibitor
ALK-IN-12 is a potent and orally bioavailable inhibitor of Anaplastic Lymphoma Kinase (ALK), exhibiting an IC50 of 0.18 nM. In addition to its action on ALK, it also inhibits Insulin-like Growth Factor 1 Receptor (IGF1R) and Insulin Receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. The compound demonstrates significant antitumor activity, making it a valuable tool for cancer research focused on ALK-driven malignancies and cellular signaling pathways involving IGF1R and InsR. -
ALK Inhibitor
ALK5-IN-30 is a potent inhibitor targeting ALK5 and TGFβ-R1, demonstrating IC50 values of less than 10 nM for both proteins. This compound is invaluable for research applications involving modulation of the TGF-β signaling pathway, which plays a critical role in cellular processes such as proliferation, differentiation, and immune response. Its high affinity and selectivity make it an essential tool for studies focused on cancer, fibrosis, and other diseases influenced by ALK signaling. -
ALK5 Inhibitor
J-1048 is a selective inhibitor of activin receptor-like kinase 5 (ALK5). It effectively inhibits TGF-β/Smad signaling, thereby reducing TAA-induced liver fibrosis in murine models. This compound is valuable for studying the roles of TGF-β signaling in fibrotic diseases and for evaluating therapeutic strategies targeting liver fibrosis. -
ALKBH5 Inhibitor
DDO-02267 is a selective covalent inhibitor of ALKBH5, demonstrating an IC50 value of 0.49 μM. This compound enhances N6-methyladenosine (m6A) levels and modulates the ALKBH5-AXL signaling pathway. DDO-02267 serves as an important tool for elucidating the biological functions of mRNA demethylase in various research contexts. -
ALK Ligand
ALK ligand-1 is a specific ligand for Anaplastic Lymphoma Kinase (ALK). It serves as a critical component in the synthesis of PROTAC ALK degrader-4, facilitating targeted protein degradation. This compound is valuable for research applications aimed at studying ALK-mediated pathways and developing novel therapeutic strategies in oncology. -
ALK Inhibitor
ALK-IN-9 is a highly potent inhibitor of anaplastic lymphoma kinase (ALK), demonstrating exceptional efficacy in inhibiting cell proliferation with IC50 values of less than 0.2 nM across multiple cell line models, including Ba/F3-EML4-ALK and KG-1 (OP2-FGFR1). This compound is particularly valuable in research applications focused on targeting ALK-driven cancers and exploring the role of ALK in various signaling pathways. Its robust biological activity makes it a critical tool for studying therapeutic resistance and drug development strategies in oncology. -
ALK5 Inhibitor
PF-03671148 is a selective inhibitor of ALK5, a receptor kinase involved in TGFβ signaling. This compound effectively attenuates TGFβ-induced fibrotic gene expression in fibroblasts, making it a promising candidate for research on fibrosis and related conditions. PF-03671148 may hold significant potential for therapeutic applications aimed at preventing dermal scarring and modulating fibrotic responses in various tissues. -
ALK2 Inhibitor
LDN-193688 is a selective inhibitor of ALK2, exhibiting IC₅₀ values of 104, 18, 235, 1530, and 1080 nM against ALK1, ALK2, ALK3, ALK4, and ALK5, respectively. This compound effectively inhibits bone morphogenetic protein 4 (BMP4)-induced phosphorylation of SMAD1/5/8, with an IC₅₀ of 2.6 μM. LDN-193688 is utilized in research focused on the BMP signaling pathway and its role in various biological processes, including development and disease. -
ALK/ROS1 Inhibitor
ALK/ROS1-IN-4 is a selective dual inhibitor targeting the anaplastic lymphoma kinase (ALK) and ROS1 kinases. This compound exhibits potent inhibitory activity against both kinases, making it a valuable tool for studying signaling pathways involved in certain cancers. ALK/ROS1-IN-4 is primarily used in research applications focused on cancer biology and therapeutic development for ALK- and ROS1-positive malignancies. -
ALK Inhibitor
CEP-28122 mesylate hydrochloride is a selective, orally active inhibitor of the anaplastic lymphoma kinase (ALK) with a reported IC50 of 1.9 nM. Exhibiting significant antitumor activity, it is effective in experimental models of ALK-positive malignancies, including anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma. Its favorable pharmacodynamic and pharmacokinetic properties make it a valuable tool for research into ALK-driven cancers. -
ALK inhibitor
Alectinib analog is a selective inhibitor of Anaplastic Lymphoma Kinase (ALK), specifically designed to overcome resistance via gating mutations. This compound shows low micromolar IC50 values, indicating potent antiproliferative and cytotoxic effects against cancer cells. Its efficacy is linked to enhanced stability and the release of active components. Additionally, Alectinib analog has been demonstrated to inhibit vascular septal dimensions in an in vivo zebrafish model, highlighting its potential for therapeutic applications in cancer research. -
c-Kit/PDGFR Inhibitor
Labuxtinib is a potent dual inhibitor of c-Kit and PDGFR, effectively blocking cell proliferation driven by c-Kit or PDGFR signaling pathways. This compound is suitable for research applications targeting mast cell-associated diseases, respiratory conditions, inflammatory disorders, fibrosis, and metabolic diseases. Its dual mechanism of action makes Labuxtinib a valuable tool for investigating the molecular underpinnings of these diseases and potential therapeutic strategies. -
VEGFR/PDGFα/c-Kit Inhibitor
Telatinib mesylate is a potent, orally active inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit, exhibiting IC50 values of 6 nM, 4 nM, 15 nM, and 1 nM respectively. This compound effectively impedes angiogenesis and tumor cell proliferation, making it a valuable tool in cancer research. Its selective targeting of key signaling pathways has potential applications in studying tumor microenvironments and in developing therapeutic strategies for various malignancies. -
c-KIT/PDGFR/RET Inhibitor
KBP-7018 is a selective tyrosine kinase inhibitor targeting c-KIT, PDGFR, and RET. It demonstrates potent inhibition with IC50 values of 10 nM for c-KIT, 7.6 nM for PDGFR, and 25 nM for RET. This compound is valuable for investigating the molecular mechanisms and potential treatments related to idiopathic pulmonary fibrosis. -
c-KIT/PDGFR/RET Inhibitor
KBP-7018 hydrochloride is a selective inhibitor of tyrosine kinases, specifically targeting c-KIT, PDGFR, and RET. It exhibits significant inhibitory potency, with IC50 values of 10 nM, 7.6 nM, and 25 nM, respectively. This compound is utilized in research focused on idiopathic pulmonary fibrosis, facilitating investigations into pathways associated with this condition. -
FLuc Inhibitor
GW694590A is an inhibitor targeting firefly luciferase (Fluc) that enhances the stability of the MYC protein, subsequently increasing its endogenous levels. This compound also inhibits receptor tyrosine kinases, demonstrating significant reductions in DDR2, KIT, and PDGFRα activity at 1 μM. GW694590A serves as a versatile protein kinase inhibitor, influencing both ATP-dependent and -independent luciferase systems, making it valuable for studies in cellular signaling and gene expression regulation. -
VEGFR Inhibitor
Tafetinib analogue 1 is a selective inhibitor of the vascular endothelial growth factor receptor (VEGFR). This compound exhibits potent anti-angiogenic activity, making it a valuable tool for investigating the role of VEGFR in tumor growth and metastasis. Tafetinib analogue 1 is applicable in cancer research, particularly in studies focusing on therapeutic strategies targeting the VEGF signaling pathway. -
Apoptotic, antiproliferative and antiangiogenic agent
2-Methoxyestradiol is an apoptotic, antiproliferative and antiangiogenic agent. Induces p53-induced apoptosis via two pathways: activation of p38 and NF-κB; and activation of JNK and AP-1 leading to Bcl-2 phosphorylation. -
HER2 inhibitor
Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA. -
EGFR inhibitor
AST-6 is a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, inhibits tumor growth both in vitro and in vivo -
c-Met inhibitor
BMS-794833 is a potent ATP competitive inhibitor to Met and VEGFR-2 with IC50 of 1.7 and 15 nmol. -
VEGFR inhibitor
Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling. -
RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively. -
EGFR inhibitor
Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway. -
EGFR, PKA,PKC inhibitor
Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.
