Catalog No.
Product Name
Application
Product Information
Citations
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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-FMS(CSF-IR)/c-Kitdual Inhibitor
Vimseltinib is a selective dual inhibitor of c-FMS (CSF-IR) and c-Kit, demonstrating IC50 values of less than 0.01 μM and 0.1-1 μM, respectively. This compound exhibits robust biological activity, making it a valuable tool for investigating signaling pathways involved in hematopoiesis and various pathologies such as cancer and inflammatory diseases. The oral bioavailability of Vimseltinib enhances its potential for in vivo studies and therapeutic applications. -
c-kit Inhibitor
Bezuclastinib is a highly selective inhibitor of the c-kit tyrosine kinase, demonstrating potent activity against the KIT D816V mutation. This compound is valuable for researching nonadvanced systemic mastocytosis (NonAdvSM) and provides insight into the underlying mechanisms of this condition. Its oral bioavailability makes it a convenient option for in vivo studies targeting c-kit dysregulation. -
CSF1R Inhibitor
Pimicotinib is a selective and orally active inhibitor of the Colony Stimulating Factor 1 Receptor (CSF1R), with an IC50 value of 19.48 nM as determined by the inhibition of ADP production. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research applications aimed at understanding tumor microenvironment interactions and immune modulation. Researchers can utilize Pimicotinib to explore CSF1R-mediated signaling in cancer biology and potential therapeutic strategies. -
Tyrosine Kinase Inhibitor
Elenestinib is a selective orally active tyrosine kinase inhibitor, demonstrating a potent inhibitory effect on the KIT D816V mutant with an IC50 value of 6 nM. Its mechanism of action is primarily focused on inhibiting aberrant signaling pathways associated with systemic mastocytosis. Due to its limited ability to cross the blood-brain barrier, Elenestinib is particularly applicable in the investigation of hematologic disorders related to mast cell proliferation and activity. -
c-Kit Inhibitor
c-Kit-IN-5 is a potent c-Kit inhibitor, demonstrating IC50 values of 22 nM in kinase assays and 16 nM in cellular assays. This compound exhibits over 200-fold selectivity for c-Kit compared to other kinases, such as KDR, p38, Lck, and Src. Due to its favorable pharmacokinetic properties, c-Kit-IN-5 is well-suited for research applications exploring c-Kit-related signaling pathways and their implications in various diseases, including cancer. -
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. -
Tyrosine Kinase Inhibitor
Elenestinib phosphate is an orally active tyrosine kinase inhibitor that selectively targets the KIT D816V mutation, exhibiting an IC50 of 0.2 nM. This compound's targeted inhibition is particularly relevant for studying systemic mastocytosis, as it provides insights into the role of mutated KIT in this condition. Notably, elenestinib phosphate has limited capacity to penetrate the blood-brain barrier, making it suitable for investigating its effects in peripheral tissues. -
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 Inhibitor
c-Kit-IN-7 is a potent c-Kit inhibitor that demonstrates an IC50 of ≤10 nM. It effectively inhibits cell proliferation in GIST430 and BaF3 mutant cell lines, with IC50 values of ≤100 nM. This compound is crucial for research focused on cancers driven by c-KIT kinase mutations, providing valuable insights into therapeutic strategies targeting this pathway. -
CSF1R Inhibitor
Pimicotinib hydrochloride is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF1R), demonstrating an IC50 value of 19.48 nM in inhibiting ADP production. This compound exhibits notable anti-tumor activity, making it a valuable tool for research in cancer biology and immunotherapy. Its specificity for CSF1R provides insights into the modulation of macrophage activity in the tumor microenvironment. -
FMS/KIT Inhibitor
PLX647 dihydrochloride is a potent and selective dual inhibitor of FMS and KIT kinases, exhibiting IC50 values of 28 nM and 16 nM, respectively. This compound demonstrates high selectivity for FMS and KIT over a broad spectrum of 400 kinases at a concentration of 1 μM, with minimal activity against FLT3 and KDR (IC50s of 91 nM and 130 nM, respectively). PLX647 dihydrochloride is valuable for research applications focused on hematopoietic and oncogenic signaling pathways. -
c-kit Inhibitor
c-Kit-IN-14 is a selective inhibitor of the c-Kit kinase, effectively blocking its phosphorylation with an IC50 of 0.4 nM for pKIT. It demonstrates potent activity against Exon 11 c-Kit mutations, also with an IC50 of 0.4 nM. This compound is primarily utilized in research related to mast cell-mediated disorders, including urticaria, providing insights into therapeutic strategies targeting c-Kit signaling pathways. -
c-kit Inhibitor
c-Kit-IN-13 is a highly selective c-kit kinase inhibitor that effectively blocks the autophosphorylation of wild-type c-kit, demonstrating an IC50 of 0.3 nM for pKIT and 0.9 nM for Exon 11 KIT. This compound is particularly useful in researching mast cell-mediated conditions, including urticaria, providing insights into the role of c-kit in these pathologies. Its potent inhibitory activity makes it a valuable tool for studies focused on targeted therapies in hematological cancers and related disorders. -
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. -
Kit Inhibitor
APcK110 is a potent inhibitor of the Kit receptor tyrosine kinase, with applications in the study of acute myeloid leukemia (AML). This compound has been shown to induce apoptosis in AML cells, offering valuable insights into therapeutic strategies for targeting this malignancy. Researchers can utilize APcK110 to explore mechanisms of resistance, cell signaling pathways, and potential combination therapies in AML treatment. -
c-Kit Inhibitor
KI-328 is a selective inhibitor of the c-Kit kinase, specifically designed to target various mutant forms associated with acute myeloid leukemia (AML). It demonstrates effective inhibition of both wild-type and certain mutant KIT-expressing cell lines, although it shows diminished activity against the D816V-KIT variant. Comparative analyses with other potent KIT inhibitors indicate varying degrees of efficacy across different mutant forms, highlighting the necessity for targeted assessments in clinical applications. KI-328 provides a valuable tool for research focused on the biological mechanisms of KIT mutations and their implications in leukemia therapies. -
c-Kit Inhibitor
c-Kit-IN-11 is a selective inhibitor of c-Kit, exhibiting an IC50 of 76 nM in Mo7e cells. This compound is valuable in research related to inflammatory conditions such as asthma, as well as in the study of malignant cancers. Its targeted inhibition of c-Kit makes it a useful tool for investigating the underlying mechanisms of these diseases and potential therapeutic strategies. -
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. -
c-Kit Inhibitor
c-Kit-IN-8 is a selective inhibitor of the c-Kit kinase, demonstrating high efficacy with an IC50 greater than 1 μM for uKIT kinase. It effectively reduces the proliferation of cancer cells, including GIST430 and BaF3 cell lines, with an IC50 of over 0.1 μM. This compound is valuable for research in cancer biology, particularly in studies focusing on c-Kit-related signaling pathways and therapeutic resistance in oncogenesis. -
c-Kit Inhibitor
c-Kit-IN-10 is a selective inhibitor of the c-Kit receptor tyrosine kinase, which plays a critical role in hematopoiesis, cell signaling, and tumorigenesis. This compound demonstrates potent anti-proliferative activity against c-Kit-dependent cancers and has potential applications in the study of inflammatory conditions such as asthma. Researchers may utilize c-Kit-IN-10 to investigate its therapeutic effect on disease models characterized by aberrant c-Kit signaling. -
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. -
EGFR Inhibitor
Afatinib N-Oxide is an oxidative degradation product of Afatinib dimaleate, an irreversible inhibitor of the epidermal growth factor receptor (EGFR) family. This compound serves as a valuable tool for characterizing the stability and degradation pathways of Afatinib in chemical research. It may also aid in understanding the mechanistic effects of EGFR inhibition in various biological contexts. -
Endogenous Metabolite
PF-05387252 is a potent and selective inhibitor of IRAK4, effectively targeting endogenous Toll-like receptor (TLR) signaling pathways. This compound exhibits significant anti-inflammatory activity in experimental models, suggesting potential therapeutic applications in conditions such as psoriasis. While PF-05387252 has demonstrated efficacy in reducing inflammation in animal studies, its effectiveness in clinical settings for psoriasis has yet to be established. -
HPK1 Inhibitor
HPK1-IN-7 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1, MAP4K1) with an IC50 of 2.6 nM, demonstrating excellent selectivity among kinases. It exhibits some selectivity against IRAK4 and GLK, with IC50 values of 59 nM and 140 nM, respectively. This compound has shown significant efficacy in the MC38 syngeneic tumor model, particularly when used in combination with anti-PD1 therapy, highlighting its potential in immuno-oncology research. -
Endogenous Metabolite
IRAK4-IN-29 is a selective inhibitor of the interleukin-1 receptor-associated kinase 4 (IRAK4), demonstrating low nanomolar activity. This compound effectively disrupts TLR-mediated signaling pathways and exhibits significant inhibition of cytokine production in response to LPS and R848 stimulation. In vivo studies reveal that IRAK4-IN-29 can suppress LPS-induced TNFα, mirroring the phenotype observed in IRAK4 gene-deficient mice. Furthermore, IRAK4-IN-29 possesses favorable medicinal chemistry characteristics, including microsomal stability and solubility, indicating its potential for clinical applications in inflammatory diseases. -
HER2 Inhibitor
JBJ-08-178-01 is a selective tyrosine kinase inhibitor targeting mutant forms of the human epidermal growth factor receptor 2 (HER2). It demonstrates significant antitumor activity by reducing both the kinase activity and protein levels of HER2 through the induction of proteasomal degradation. This compound holds potential for research applications in non-small-cell lung cancer, providing insights into therapeutic mechanisms against HER2-driven malignancies.
