Catalog No.
Product Name
Application
Product Information
Citations
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EGFT/HER2 inhibitor
Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity. -
VEGFR-2 inhibitor
JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively. -
FAK and Pyk2 kinase inhibitor
PF-562271 hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively. -
BTK inhibitor
Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. -
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. -
EGFR inhibitor
Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). -
VEGFR2 inhibitor
ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM. -
dual inhibitor for c-Met and EGFR
Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. -
FGFR inhibitor
2,5-Dihydroxybenzoic acid is a derivative of benzoic and a powerful inhibitor of fibroblast growth factors. -
BTK inhibitor
BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM. -
IRAK4/FLT3 inhibitor
Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. -
Bcr-Abl1 inhibitor
Vodobatinib, also known as K-0706, is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity. -
PDGFR inhibitor
Seralutinibm, also known as PK-10571 and GB002, is a Inhaled Pdgfr Kinase Inhibitor. -
PDGFRα/PDGFRβ inhbitor
JNJ 10198409 is a potent platelet-derived growth factor receptor (PDGFR) inhibitor (IC50 values are 4.2 and 45 nM for PDGFRβ and PDGFRα, respectively). Also inhibits c-Abl, Lck, c-Src and Fyn kinases (IC50 values are 22, 100, 185 and 378 nM respectively). -
multi-kinase inhibitor
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl. -
SU-4313 is a small-molecule modulator of protein tyrosine kinases (PTKs). It inhibits multiple receptor tyrosine kinases with reported IC₅₀ values of 14.5 μM (PDGFR), 18.8 μM (FLK-1/VEGFR2), 11 μM (EGFR), 16.9 μM (HER2 kinase), and 8.0 μM (IGF-1R).
Through its multi-kinase inhibitory profile, SU-4313 modulates tyrosine kinase–mediated signal transduction pathways involved in the regulation of cell proliferation and growth. It is therefore commonly used as a research tool for investigating aberrant receptor tyrosine kinase signaling and proliferation-associated pathways.
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FLT3 inhibitor
5'-Fluoroindirubinoxime (5'-FIO, compound 13), an Indirubin derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
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PROTAC FAK Degrader
GSK215 is a potent and selective PROTAC degrader targeting focal adhesion kinase (FAK) via the VHL E3 ligase. With a pDC50 of 8.4, it induces rapid and sustained degradation of FAK, leading to significant modulation of FAK levels over time. This compound demonstrates an extended pharmacokinetic/pharmacodynamic disconnect, making it a valuable tool for research applications in cancer biology and signaling pathways associated with cell adhesion and migration. -
Smad3/HIF-α Dual Target PROTAC
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine functions as a dual-target PROTAC, effectively inducing ubiquitination and degradation of Smad3 while simultaneously enhancing HIF-α protein levels. This compound exhibits multi-pathway anti-fibrotic activity and renal protective properties, making it valuable for research on renal anemia. Additionally, it has potential applications in studying prostate cancer and other malignancies, contributing to a deeper understanding of cancer biology and treatment modalities. -
PROTAC Btk Degrader
SJF620 is a PROTAC that targets Bruton's tyrosine kinase (Btk) for degradation through its ligands for Cereblon (CRBN). With a DC50 of 7.9 nM, SJF620 effectively recruits CRBN, facilitating selective protein degradation. This compound is primarily utilized in research applications focused on Btk-related signaling pathways and therapeutic development for B-cell malignancies. -
PROTAC BCR-ABL Degrader
SIAIS178 is a potent and selective PROTAC BCR-ABL degrader that operates through the recruitment of Von Hippel-Lindau (VHL) E3 ubiquitin ligase, achieving an IC50 of 24 nM. This compound effectively induces degradation of the BCR-ABL protein, demonstrating significant anticancer activity. SIAIS178 is suitable for research applications focused on targeted protein degradation in cancer models. -
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. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
PROTAC BTK Degrader
NRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies. -
EGFR Degrader
MS154 is a novel E3 ligase cereblon-recruited degrader specifically targeting epidermal growth factor receptor (EGFR). It has demonstrated potent degradation of the EGFR L858R mutant in cancer cell lines with Kd values of 1.8 nM and 3.8 nM for wild-type and mutant EGFR, respectively. This selective degradation mechanism highlights its potential as an anticancer agent, particularly in lung cancer treatment. MS154 operates through an E3 ligase-dependent pathway, representing a promising therapeutic strategy for treating EGFR-driven malignancies. -
VEGFR-2 Inhibitor
VEGFR-2-IN-39 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), with an IC50 of 208.6 nM. This compound effectively inhibits the proliferation of EA.hy926 cells, a human umbilical vein endothelial cell line, in a concentration-dependent manner, exhibiting an IC50 of 38.65 µM. VEGFR-2-IN-39 has low toxicity, making it suitable for further research applications in angiogenesis and vascular biology. -
Iron Chelator
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19. -
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. -
HIF-1α inhibitor
PRLX-93936 dihydrochloride (Compound 16) is a small-molecule inhibitor of hypoxia-inducible factor 1α (HIF-1α) with demonstrated anticancer activity. It also suppresses signaling within the activated Ras pathway, thereby inhibiting tumor cell proliferation and survival. PRLX-93936 shows potential therapeutic relevance in the study of relapsed or refractory multiple myeloma and other Ras-driven malignancies, making it a useful compound for investigating hypoxia-related and oncogenic signaling mechanisms in cancer. -
BTK/GSPT1 Degrader
GBD-9 is a dual-action degrader that targets both BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). It acts as a PROTAC to promote BTK degradation and functions as a molecular glue to induce GSPT1 degradation. GBD-9 exhibits significant antiproliferative activity in cancer cells, making it a promising candidate for cancer research. -
PROTAC FGFR2 Degrader
LC-MB12 is an orally active PROTAC compound that targets FGFR2 degradation, with a DC₅₀ of 11.8 nM. It consists of the FGFR2 inhibitor BGJ398, a PROTAC linker, and a cereblon (CRBN) ligand. LC-MB12 effectively inhibits FGFR2 signaling in gastric cancer cells and exhibits antitumor activity. - ATWLPPR peptide is a biologically active heptapeptide and a specific antagonist of VEGFR2 (KDR/Flk-1). It binds to VEGFR2, completely blocking VEGF binding and thereby inhibiting VEGF-induced angiogenesis in vivo. ATWLPPR selectively inhibits human endothelial cell proliferation in vitro and fully suppresses VEGF-mediated angiogenesis in vivo.
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Kinases PROTAC/Nek9 Inhibitor
DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity.
