Catalog No.
Product Name
Application
Product Information
Citations
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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. -
ALK/MET inhibitor
Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. - 2-Keto Crizotinib (PF-06260182) is an active lactam metabolite of crizotinib.
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antagonist of the TGFbeta family type I receptors, Alk5 and/or Alk4
BIO-013077-01, Novel potent antagonist of the TGFbeta family type I receptors, Alk5 and/or Alk4. -
ALK5 inhibitor
TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. -
PROTAC ALK Degrader
TL13-12 is a selective PROTAC degrader targeting anaplastic lymphoma kinase (ALK), exhibiting an IC50 of 0.69 nM for ALK inhibition. In addition to its primary action, TL13-12 induces degradation of several other kinases, including Aurora A (IC50 = 13.5 nM), FER (IC50 = 5.74 nM), PTK2 (IC50 = 18.4 nM), and RPS6KA1 (IC50 = 65 nM). This compound is designed through the conjugation of TAE684 and the Cereblon ligand derived from Pomalidomide, making it a valuable tool for studying kinase biology and developing targeted therapies. -
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. -
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. -
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. -
ALK/EGFR Degrader
SIAIS164018 is a PROTAC-based degrader targeting ALK and EGFR, demonstrating IC50 values of 2.5 nM and 6.6 nM against ALK and ALK G1202R, respectively. This compound exhibits potent inhibitory effects on cancer cell migration and invasion, induces G1 cell cycle arrest, and promotes apoptosis. SIAIS164018 is a valuable tool for research applications investigating targeted degradation mechanisms in oncology. -
ALK/ROS1 Inhibitor
Lorlatinib acetate is a selective and orally active inhibitor targeting ROS1 and ALK pathways. This compound exhibits potent anticancer activity with Kis of less than 0.025 nM for ROS1 and less than 0.07 nM for wild-type ALK, establishing it as a promising therapeutic candidate for ALK-driven cancers. Additionally, Lorlatinib acetate effectively inhibits ALK phosphorylation, demonstrated by IC50 values ranging from 15-43 nM for ALKL1196 and varying efficacy against multiple resistant mutations, making it a valuable tool for cancer research and drug discovery. -
ALK/EGFR Inhibitor
ALK/EGFR-IN-1 is a potent dual inhibitor targeting ALK and EGFR, effectively blocking their phosphorylation. This compound demonstrates high inhibitory activity against EGFR L858R T790M mutants in H1975 cells, with an IC50 of 4.3 nM, and EML4-ALK in BaF3 cells, with an IC50 of 3.6 nM. ALK/EGFR-IN-1 is particularly valuable for research in non-small cell lung cancer (NSCLC) and provides insights into the mechanisms of resistance in targeted therapies. -
ALKBH5 Inhibitor
DDO-2728 is a selective inhibitor of AlkB homologue 5 (ALKBH5), demonstrating an IC50 of 2.97 μM. This compound enhances the levels of N6 methyladenosine (m6A) modifications, leading to increased cell apoptosis and cell cycle arrest. DDO-2728 has shown efficacy in suppressing tumor growth in the MV4 11 xenograft model, highlighting its potential application in cancer research and therapeutic strategies targeting ALKBH5. -
ALK Inhibitor
Neladalkib is a potent oral selective inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 2.8 nM. This compound induces apoptotic cell death and demonstrates anti-tumor activity, making it a valuable tool for cancer research. Neladalkib is particularly relevant in studies focused on ALK-driven malignancies and therapeutic resistance mechanisms. - 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.
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ALK/ROS1 inhibitor
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC). -
BMP receptor agonist
SY-LB-35 is a potent agonist of bone morphogenetic protein (BMP) receptors, capable of activating both canonical and non-canonical signaling pathways. In the C2C12 myoblast cell line, SY-LB-35 significantly enhances cell proliferation and viability, promoting cell cycle progression by increasing the proportion of cells in the S and G2/M phases. Mechanistically, it activates the canonical Smad pathway as well as non-canonical PI3K/Akt, ERK, p38, and JNK signaling cascades. These properties make SY-LB-35 a valuable tool for studying BMP-related cellular processes and a potential therapeutic candidate for tissue regeneration and muscle repair. -
PROTAC ALK/EGFR degrader
SIAIS164018 hydrochloride is a PROTAC-based dual degrader targeting ALK and EGFR, with IC₅₀ values of 2.5 nM for ALK and 6.6 nM for the ALK G1202R mutant. It effectively suppresses cancer cell migration and invasion, induces G1 phase cell cycle arrest, and promotes apoptosis, making it a promising candidate for targeted cancer therapy research. -
PROTAC ALK Degrader
TL13-112 is a potent and selective PROTAC degrader targeting ALK, with an IC₅₀ of 0.14 nM for ALK inhibition. In addition to ALK, TL13-112 also induces degradation of Aurora A (IC₅₀: 8550 nM), FER (42.4 nM), PTK2 (25.4 nM), and RPS6KA1 (677 nM), supporting its utility in kinase signaling and cancer research. -
ALK Inhibitor
ALK/PI3K/AKT-IN-1 is a selective ALK inhibitor that demonstrates significant anti-proliferative effects on A549, H1975, and PC9 cancer cell lines with IC50 values of 0.44, 0.83, and 1.51 μM, respectively. This compound induces cell cycle arrest at the G1 phase by enhancing p21 and p27 expression while inhibiting CDK2 and phosphorylated Rb activity. Additionally, ALK/PI3K/AKT-IN-1 disrupts the ALK/PI3K/AKT signaling pathway, leading to mitochondrial membrane depolarization and apoptosis in A549 cells. It also effectively inhibits spheroid formation and growth in A549 cells, making it a valuable tool for cancer research. -
ALK Inhibitor
ALK-IN-31 is an orally active inhibitor of anaplastic lymphoma kinase (ALK), with an IC50 of 1135 nM. This compound demonstrates significant antiproliferative activity against H2228 lung cancer cells, showing an IC50 of 1.35 μM. ALK-IN-31 induces apoptosis and halts cell cycle progression in the G0/G1 phase by modulating mitochondrial function. Furthermore, it attenuates tumor growth by downregulating p-AKT and p-mTOR within the PI3K-AKT-mTOR signaling pathway, making it a valuable tool for research in non-small cell lung cancer (NSCLC). -
EML4-ALK PROTAC Degrader
Gly-PEG3-BA is an EML4-ALK PROTAC degrader that targets the EML4-ALK fusion protein. This compound exhibits a DC50 of 0.50 μM for EML4-ALK in H3122 cells and a DC50 of 20.15 μM for EGFR mutant (L858R/T790M) levels in H1975 cells. Gly-PEG3-BA demonstrates notable antiproliferative effects, with IC50 values of 0.84 μM against H3122 cells and 20.74 μM against H1975 cells. It is a valuable tool for research in non-small cell lung cancer. -
EML4-ALK/EGFR PROTAC Degrader
Lys-PEG3-BA is a novel EML4-ALK/EGFR PROTAC degrader that influences target proteins through the ubiquitin-proteasome pathway. With DC50 values of 1.32 μM against H3122 (EML4-ALK) cells and 19.66 μM for H1975 (EGFR-L858R/T790M) cells, it effectively inhibits cell proliferation. This compound serves as a valuable tool for research into non-small cell lung cancer and the mechanisms underlying targeted protein degradation. -
EGFR/ALK Inhibitor
DA-0157 is a selective inhibitor of the epidermal growth factor receptor (EGFR) and anaplastic lymphoma kinase (ALK), designed to address drug-resistant mutations, specifically EGFR C797S and ALK mutations in non-small cell lung cancer (NSCLC) models. It demonstrates potent antiproliferative activity in cells bearing EGFR Del19/T790M/C797S (IC50 = 6.9 nM), as well as in various ALK mutant forms, including Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM). Additionally, DA-0157 has been shown to inhibit CYP2D6 with an IC50 of 5.26 μM, and exhibits promising antitumor efficacy in preclinical mouse models, making it a valuable tool for cancer research. -
ALK Inhibitor
TSR-011-isomer is a potent anaplastic lymphoma kinase (ALK) inhibitor with an IC50 of 6 nM. This compound demonstrates significant biological activity by undergoing metabolic hydrolysis and NADPH-dependent metabolism, facilitating its clearance in biological systems. TSR-011-isomer is suitable for research focused on ALK-driven cancers, making it a valuable tool for studies in cancer biology and targeted therapy development. -
ALK Degrader
ALK-IN-35 is an ALK degrader that selectively inhibits ALK kinase activity with an IC50 of 0.74 nM. This compound increases the solvent-accessible surface area of hydrophobic residues around the ALK binding pocket, leading to a partially unfolded conformation that promotes proteasomal degradation of ALK. ALK-IN-35 has demonstrated potent anti-proliferative effects on cancer cells and is a valuable tool for research focused on non-small cell lung cancer. -
ALK Inhibitor
XMU-MP-5 is a selective inhibitor of anaplastic lymphoma kinase (ALK), demonstrating potent inhibitory activity against ALK-mutated Ba/F3 cells with IC50 values ranging from 4 to 50 nM. This compound induces apoptosis specifically in EML4-ALK Ba/F3 cells and has shown notable antitumor efficacy in murine models. XMU-MP-5 serves as a valuable tool in cancer research, particularly in studies focused on ALK-driven malignancies. -
ALK Inhibitor
Ceritinib mesylate is a selective ALK tyrosine kinase inhibitor that functions through ATP-competitive mechanisms, exhibiting an IC50 of 200 pM. In addition to its activity against ALK, Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D, with IC50 values of 8 nM, 7 nM, and 23 nM, respectively. This compound demonstrates significant antitumor potency, making it a valuable tool for research in cancer biology and targeted therapies. -
ALK4/5/7 Inhibitor
A 83-01 sodium is a selective inhibitor of the transforming growth factor-beta (TGF-β) type I receptors ALK4, ALK5, and ALK7. With IC50 values of 12 nM, 45 nM, and 7.5 nM, it effectively blocks transcriptional activity induced by these kinases. This compound is valuable for research applications focused on TGF-β signaling pathways and regulation of cellular processes such as proliferation, differentiation, and epithelial-mesenchymal transition. -
ALK2 Inhibitor
M4K-2009 is a potent inhibitor of ALK2, exhibiting an IC50 value of 13 nM, and is capable of penetrating the blood-brain barrier. In addition to its primary activity against ALK2, M4K-2009 demonstrates efficacy against the hERG potassium channel. This compound is valuable for research in the areas of bone morphogenetic protein signaling and related therapeutic applications. -
ALK Molecular Glue Degrader
TRI-611 is an orally active molecular glue degrader that targets the anaplastic lymphoma kinase (ALK). It forms a ternary complex with the substrate receptor CRBN, leading to polyubiquitination and subsequent degradation of ALK, including resistant fusion proteins. TRI-611 effectively inhibits ALK-mediated downstream signaling and exhibits anti-proliferative effects in ALK-positive cancer cells. Preclinical studies demonstrate its capability to induce regression of ALK-positive non-small cell lung cancer tumors, making it a valuable tool for research into TKI-refractory tumors and central nervous system metastases.
