Catalog No.
Product Name
Application
Product Information
Citations
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TrxR/EGFR Inhibitor
TrxR/EGFR-IN-1 is a potent inhibitor targeting both Thioredoxin Reductase (TrxR) and Epidermal Growth Factor Receptor (EGFR). This compound demonstrates significant anti-proliferative effects against Gefitinib-sensitive and resistant lung cancer cells, facilitating apoptosis and tumor cell death. TrxR/EGFR-IN-1 promotes GPX4 protein degradation via autophagolysosomal and proteasomal pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it a valuable tool for studying mechanisms underlying Gefitinib-resistant lung cancer. -
ErbB-2/EGFR Inhibitor
Lapatinib tosylate is a potent inhibitor targeting the ErbB-2 and EGFR tyrosine kinase domains. With IC50 values of 10.2 nM for EGFR and 9.8 nM for ErbB-2, it effectively blocks signaling pathways associated with cell proliferation and survival. This compound is primarily utilized in cancer research and therapeutic studies, particularly for conditions driven by aberrant ErbB signaling. -
STAT3 Inhibitor
W1131 is a potent inhibitor of signal transducer and activator of transcription 3 (STAT3), which plays a critical role in oncogenic processes. By inducing ferroptosis, W1131 effectively suppresses cancer progression in various models, including gastric cancer subcutaneous xenografts, organoids, and patient-derived xenografts (PDX). Additionally, W1131 enhances chemosensitivity of cancer cells to 5-fluorouracil (5-FU), while modulating cell cycle dynamics, DNA damage response, and oxidative phosphorylation via the IL6-JAK-STAT3 and ferroptosis pathways. This compound is valuable for research into cancer biology and therapeutic resistance. -
PIM-3 Inhibitor
M-110 is a selective, ATP-competitive inhibitor of PIM kinases, prominently targeting PIM-3 with an IC50 of 47 nM. This compound exhibits inhibitory activity against PIM-1 and PIM-2 with IC50 values around 2.5 μM. M-110 has demonstrated efficacy in curtailing the proliferation of prostate cancer cell lines, exhibiting IC50 values ranging from 0.6 to 0.9 μM. This makes M-110 a valuable tool for studying PIM kinase signaling pathways and their role in cancer biology. -
Pim-2 Inhibitor
HJ-PI01, a potent Pim-2 inhibitor, effectively induces apoptosis and autophagic cell death in cancer cells. This compound demonstrates significant anti-tumor activity in vivo, notably inhibiting tumor growth in MDA-MB-231 xenograft mouse models. HJ-PI01 serves as a valuable tool for cancer research, facilitating investigations into the therapeutic implications of Pim-2 inhibition. -
PIM Inhibitor
Uzansertib is a potent, orally active pan-PIM kinase inhibitor that operates through ATP-competitive mechanisms, exhibiting IC50 values of 0.24 nM, 30 nM, and 0.12 nM for PIM1, PIM2, and PIM3, respectively. This compound demonstrates significant anti-proliferative activity across a range of hematologic tumor cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Researchers can utilize Uzansertib to explore the roles of PIM kinases in tumorigenesis and potential treatment strategies. -
Pim-1/2 Kinase Inhibitor
Pim-1/2 kinase inhibitor 1 is a selective inhibitor of Pim-1 and Pim-2 kinases, targeting their phosphorylation activity. This compound effectively disrupts the phosphorylation of key substrates, including 4E-BP1 and p27Kip1, which are crucial for cell cycle regulation and protein synthesis. Pim-1/2 kinase inhibitor 1 is primarily utilized in cancer research, particularly in studies focusing on the mechanisms underlying prostate cancer progression. -
PIM Inhibitor
AZD1897 is a potent inhibitor of PIM1, PIM2, and PIM3 kinases, demonstrating IC50 values of less than 3 nM for each target. This compound exhibits significant anticancer activity, particularly in acute myeloid leukemia (AML) cells, where it shows a synergistic effect when used in combination with Capivasertib. The mechanism of action involves the inhibition of critical cellular pathways, including mTOR and MCL1, making AZD1897 a valuable tool for cancer research. -
Pim Inhibitor
K00135 is a potent and selective inhibitor of PIM kinases, primarily targeting PIM1, PIM2, and PIM3. This compound demonstrates significant inhibition of cell survival and clonogenic growth in acute leukemia cells. Additionally, K00135 effectively reduces the phosphorylation of downstream targets of the PIM signaling pathway, making it a valuable tool for cancer research focusing on PIM kinase-related mechanisms. -
Pim/DAPK3 Inhibitor
HS56 is an ATP-competitive dual inhibitor of Pim kinases and DAPK3, demonstrating Ki values of 0.26 μM for DAPK3, 0.208 μM for Pim-3, and over 100 μM for Pim-2 and Pim-1. This compound effectively inhibits LC20 phosphorylation and smooth muscle contraction, leading to a reduction in blood pressure in spontaneously hypertensive mouse models. HS56 is suitable for research investigating the mechanisms and potential treatments for hypertension. -
Pim-1 Kinase Inhibitor
Pim-1 Kinase Inhibitor 13 is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 of 4.41 μM. This compound is instrumental in the study of immunological processes and cancer biology, providing valuable insights into Pim-1's role in cell survival and proliferation. Its application in research may facilitate the development of targeted therapies for malignancies associated with aberrant Pim-1 activity. -
Pim Inhibitor
DHPCC-9 is a selective inhibitor of Pim kinase, a critical regulator of cell survival and proliferation. This compound demonstrates potent biological activity in modulating cancer cell growth and has significant implications for cancer research, particularly in the investigation of therapeutic strategies targeting the Pim signaling pathway. Researchers can utilize DHPCC-9 to explore its effects on cellular responses and potential applications in developing anti-cancer therapies. -
Pim Inhibitor
R8-T198wt is a cell-permeable peptide that functions as a Pim-1 kinase inhibitor. By targeting the carboxyl-terminal region of p27Kip1, it exhibits significant anti-tumor activity. This reagent is ideal for research applications involving cancer biology and cellular signaling pathways associated with cell cycle regulation and apoptosis. -
Pan-PIM Inhibitor
GDC-0570 is a potent and selective pan-PIM inhibitor designed for oral administration. It exhibits pronounced antitumor activity and has shown synergistic effects when combined with Sotorasib in models of acquired KRAS-resistant non-small cell lung cancer (NSCLC). This compound serves as a valuable tool for investigating the role of PIM kinases in cancer biology and therapeutic resistance. -
PIM-1 Inhibitor
PIM1-IN-7 is a potent inhibitor of the PIM-1 kinase, exhibiting an IC50 of 0.67 μM. This compound demonstrates significant cytotoxicity against HCT-116 and MCF-7 cancer cell lines, with IC50 values of 42.9 μM and 7.68 μM, respectively. Its ability to selectively inhibit PIM-1 makes it a valuable tool for investigating the role of this kinase in cancer biology and for exploring potential therapeutic strategies. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 5 is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 value of 0.61 μM. This compound demonstrates significant cytotoxicity across various cancer cell lines, including HepG2, MCF-7, PC3, and HCT-116, with IC50 values ranging from 6.95 to 20.19 μM. It serves as a valuable tool for researching the modulation of Pim-1 in cancer biology and therapeutic applications. -
PIM Inhibitor
FD1024 is a potent PIM inhibitor with IC50 values of 1.96 nM, 38.9 nM, and 4.17 nM for PIM1, PIM2, and PIM3, respectively. This compound exhibits strong antiproliferative activity against various acute myeloid leukemia (AML) cell lines, showing effective concentrations of 0.16 μM, 0.12 μM, 1.05 μM, and 1.39 μM for EOL-1, MV-4-11, KG-1, and MOLM-16 cells. Additionally, FD1024 demonstrates significant antitumor efficacy in in vivo mouse models, making it a valuable tool for research into AML therapeutic strategies. -
PIM-1 Inhibitor
PIM1-IN-6 is a potent inhibitor of Pim-1 kinase, exhibiting an IC50 of 0.60 μM. This compound demonstrates significant cytotoxic activity in HCT-116 and MCF-7 cancer cell lines, with IC50 values of 1.51 μM and 15.2 μM, respectively. PIM1-IN-6 holds promise for research applications in cancer biology, particularly in studies aimed at elucidating the role of Pim-1 in tumor proliferation and survival. -
Pim-1 Kinase Inhibitor
10-DEBC is a selective inhibitor of Pim-1 kinase, demonstrating potent inhibitory activity with an IC50 of 1.28 μM. This compound plays a critical role in regulating cell proliferation and survival, making it a valuable tool for research in cancer biology and therapeutic interventions. Its specificity for Pim-1 kinase supports its use in studies exploring signal transduction pathways and the development of targeted cancer therapies. -
PIM1 Inhibitor
PIM1-IN-4 is a selective inhibitor of PIM1 kinase, demonstrating potent activity in blocking PIM1-mediated signaling. In addition to PIM1, PIM1-IN-4 exhibits significant inhibition of several other kinases, including SGK-1, PKA, CaMK-1, GSK3β, and MSK1. This compound is valuable for investigating its role in cancer biology and therapeutic strategies targeting PIM1-related pathways. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 3 (Compound H5) is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 of 35.13 nM. This compound effectively modulates the activity of Pim-1, a serine/threonine kinase involved in cell growth and survival signaling pathways. It is valuable for studying the role of Pim-1 in cancer and other diseases where its dysregulation is implicated. -
Pim Inhibitor
MNK/PIM-IN-1 is a dual inhibitor targeting MNK and PIM kinases, showcasing a favorable pharmacokinetic profile. This reagent exhibits significant antitumor activity and is applicable in studying the roles of MNK and PIM signaling pathways in cancer biology. It is an essential tool for researchers investigating the mechanisms of cell proliferation and survival in various malignancies. -
PIM1 Inhibitor
NMS-P645 is a potent PIM1 inhibitor that exhibits anti-proliferative activity, particularly when used in combination with GDC-0941 in both TMPRSS2/ERG positive and negative prostate cancer cells. By reversing PIM1-induced pro-survival signals, NMS-P645 contributes valuable insights into the mechanisms underlying prostate cancer resistance and cell survival. This compound is suitable for research applications focused on prostate cancer treatment and the exploration of PIM1 signaling pathways. -
Pim-1 Kinase Inhibitor
Pim-1 kinase inhibitor 4 is a potent inhibitor of Pim-1 kinase, with an inhibitory concentration (IC50) of 17.01 nM. This compound exhibits antioxidant activity and inhibits DPPH, contributing to its biological profile. Additionally, Pim-1 kinase inhibitor 4 induces apoptosis in PC-3 prostate cancer cells, demonstrating an IC50 of 16 nM for growth inhibition. This reagent is valuable for research focused on prostate cancer and cellular apoptosis mechanisms. -
Pim-2 Inhibitor
PIM-IN-2 is a potent inhibitor of Pim-2 kinases, exhibiting an IC50 of 25 nM. This compound has demonstrated significant antiapoptotic properties and promotes cell survival, making it a valuable tool in cancer research. Its elevated expression in various human tumors positions PIM-IN-2 as a relevant reagent for studies on tumor biology and therapeutic strategies targeting the Pim kinase pathway. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 6 is a selective inhibitor of Pim-1 kinase, demonstrating an IC50 value of 0.46 μM. This compound exhibits significant cytotoxic activity against various cancer cell lines, making it a valuable tool for cancer research. Its ability to target and inhibit Pim-1 kinase contributes to its potential applications in investigating therapeutic strategies for malignancies. -
Pim Inhibitor
PIM-IN-4 is a potent inhibitor of Pim kinases, exhibiting Ki values of 2 nM, 3 nM, and 0.5 nM for Pim-1, Pim-2, and Pim-3, respectively. By inhibiting the phosphorylation of the pro-apoptotic protein Bad, PIM-IN-4 effectively induces apoptosis in leukemic cells. This compound is valuable for research into leukemia and related signaling pathways, contributing to the understanding of therapeutic strategies in hematological malignancies. -
PIM-1/PIM-2 Inhibitor
Pim-1/2 kinase inhibitor 2 is a selective competitive inhibitor of PIM-1 and PIM-2 kinases, with IC50 values of 1.31 μM and 0.67 μM, respectively. This compound exhibits low cytotoxicity in normal human lung fibroblast Wi-38 cells while demonstrating potent anticancer activity against various cancer cell lines, including myeloid leukemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2). It serves as a valuable tool for studying the therapeutic potential of PIM inhibition in cancer research. -
JAK3 Inhibitor
JAK3-IN-13 is a selective and orally bioavailable inhibitor of JAK3, exhibiting IC50 values of 4728, 2039, 8, and 365 nM against NK1, JNK2, JNK3, and Tyk2, respectively. This compound demonstrates significant antiproliferative effects and induces cell cycle arrest in the G0/G1 phase. JAK3-IN-13 is particularly relevant for research applications focused on tumor biology and the modulation of immune responses. -
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. -
EPAC1 Activator, STAT3 Modulator
DM243 is an EPAC1 activator and STAT3 modulator known for its ability to increase GTP-bound Rap1 levels specifically in EPAC1-expressing cells, while exhibiting no effects on EPAC2 or PKA. This compound effectively reduces IL-6/IL-6Rα-induced STAT3 phosphorylation in endothelial cells and suppresses TGF-β1-mediated fibroblast-to-myofibroblast transition, leading to decreased levels of α-smooth muscle actin and Collagen I in lung fibroblasts. Additionally, DM243 demonstrates minimal cytotoxicity in normal human lung fibroblasts, making it a valuable tool for studies related to fibrosis and inflammation. -
JAK/STAT Inhibitor
Phenylpyropene C is a JAK/STAT pathway inhibitor known to effectively inhibit interferon-gamma (IFN-γ) mediated expression of reporter genes, with an IC50 range of 5.4 to 10.8 μM. Additionally, it serves as an inhibitor of acyl-CoA, exhibiting an IC50 of 16.0 μM. This compound is valuable for research applications focusing on the modulation of immune responses and the exploration of cytokine signaling pathways. -
STAT6 Modulator
Medrysone, also known as 6α-Methyl-11β-hydroxyprogesterone, functions as a STAT6 modulator with significant implications for macrophage polarization. This compound enhances IL-4-induced STAT6 activation, leading to increased expression of M2 macrophage markers and elevated secretion of pro-angiogenic factors such as VEGF and CCL2. Additionally, Medrysone promotes the migratory capacity of M2-like macrophages towards endothelial cells, thereby facilitating tissue repair processes. Its efficacy in regulating macrophage polarization makes it a valuable tool for research on corneal injury and wound healing applications. -
EPAC1 Activator, STAT3 Phosphorylation Inhibitor
DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor. It effectively increases Rap1-GTP levels through selective activation of EPAC1, without affecting EPAC2 or PKA. DM245 mitigates IL-6/IL-6Rα-mediated STAT3 phosphorylation in endothelial cells and inhibits the TGF-β1-induced transition of fibroblasts to myofibroblasts, leading to decreased levels of αSMA and Collagen I. Importantly, DM245 shows minimal cytotoxicity in normal human lung fibroblasts, indicating a high safety profile for extended exposure. -
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. -
STAT3 Ligand
STAT3-IN-26 is a selective ligand for the transcription factor STAT3, a critical regulator of cell growth and survival. This compound is instrumental in the synthesis of PROTACs (Proteolysis-targeting chimeras) aimed at inducing the degradation of STAT3. It is particularly relevant for research into targeted cancer therapies and studies on cellular signaling pathways involving STAT3. -
STAT3 PROTAC Degrader
PROTAC STAT3 degrader-3 (S3D1) targets the STAT3 protein through a PROTAC-mediated degradation mechanism. This compound exhibits potent anticancer activity by facilitating the ubiquitination and subsequent proteasomal degradation of STAT3, a key oncogenic transcription factor. It is primarily applied in research focused on cancer biology, particularly in studies investigating the therapeutic potential of targeting the STAT3 signaling pathway. -
EGFR PARP Dual-targeting PROTAC Molecule
DP-C-4 is a Cereblon-based dual-targeting PROTAC molecule designed for the concurrent degradation of epidermal growth factor receptor (EGFR) and poly (ADP-ribose) polymerase (PARP). This compound demonstrates significant biological activity by promoting the targeted destruction of these proteins, which can be crucial in cancer research and therapeutic applications. DP-C-4 may facilitate studies investigating the interplay between EGFR and PARP pathways, potentially leading to new insights in oncology and the development of innovative treatment strategies. -
JAK3/TEC Family Kinase Inhibitor
Plodicitinib is an inhibitor of Janus tyrosine kinase 3 (JAK3) and TEC family kinases. This compound exhibits significant anti-inflammatory activity, making it valuable for research in inflammation-related disorders. It is applicable in studies exploring the modulation of immune responses and potential therapeutic interventions in autoimmune diseases. -
ErbB-2/EGFR Tyrosine Kinase Inhibitor
GW583340 is an orally bioavailable inhibitor targeting the ErbB-2 and EGFR tyrosine kinases. It demonstrates significant antitumor activity in xenograft models characterized by overexpression of EGFR or ErbB-2, making it a valuable tool for investigating therapeutic strategies. GW583340 is particularly relevant for research focused on head and neck cancer, breast cancer, and gastric cancer. -
EGFR T790M/L858R/ACK1 Inhibitor
EGFR/ACK1-IN-1 is a potent inhibitor targeting the EGFR T790M/L858R mutation and ACK1, with IC50 values of 23 nM and 263 nM, respectively. This dual inhibition effectively disrupts cell proliferation and demonstrates significant antitumor activity. It is a valuable reagent for research applications focused on cancer biology and therapeutic development for EGFR mutant-driven tumors. -
EphB4, VEGFR-2 and PDGFR-β Inhibitor
JI-101 hydrochloride is an orally active inhibitor targeting EphB4, VEGFR-2, and PDGFR-β, effectively modulating angiogenesis signaling pathways associated with tumor vasculature. This compound demonstrates significant anti-cancer activity, inhibiting multiple stages of tumor angiogenesis and showing efficacy against various cancer cell lines and xenografts. With rapid oral absorption and extensive tissue distribution, preferential uptake occurs in the lungs, while elimination primarily occurs via feces. JI-101 hydrochloride can be utilized in research studies focused on ovarian cancer and other solid tumors, providing valuable insights into angiogenesis and cancer treatment mechanisms. -
AKT1/SRC/STAT3/EGFR Binder
(+)−Theta-cypermethrin is a stereoisomer of cypermethrin that functions as a selective binder to AKT1, SRC, STAT3, and epidermal growth factor receptor (EGFR). This compound is known to penetrate the blood-brain barrier, leading to alterations in the amplitude of delayed rectifier potassium channel currents and significant shifts in the activation and inactivation curves at elevated concentrations. Additionally, (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons and is associated with chronic respiratory system damage and neurotoxicity. It serves as a valuable tool for research into signal transduction pathways and neuropharmacology. -
EGFR Ligand
Cyclo[K(N3)larllt] is a cyclic peptide that specifically targets the epidermal growth factor receptor (EGFR) with a Kd value of 5.09 μM and demonstrates selectivity for related proteins HER2 and HER3. This compound exhibits no cytotoxicity and does not inhibit the growth of EGFR-overexpressing cancer cells. Cyclo[K(N3)larllt] is ideal for use as a ligand in EGFR-targeted fluorescent conjugates, facilitating the detection of tumors with elevated EGFR levels. Its applications extend to research focused on colorectal cancer and related pathologies. -
NUAK1 Inhibitor
NUAK1-IN-3 is a selective inhibitor of NUAK1 with a high potency, exhibiting an IC50 of 0.49 nM. It also demonstrates inhibitory activity against NUAK2 and JAK3 with IC50 values of 265 nM and 225 nM, respectively. This compound disrupts the NUAK1-MYPT1 signaling pathway, leading to reduced MYPT1 phosphorylation and inhibition of proliferation, migration, and invasion in triple-negative breast cancer cells. Additionally, NUAK1-IN-3 counteracts TGF-β1-induced epithelial-mesenchymal transition effects by modulating critical markers such as Snail, N-cadherin, and E-cadherin. It holds potential for exploring therapeutic strategies for triple-negative breast cancer. -
JAK1 Inhibitor
YYSW001 is a selective Janus kinase 1 (JAK1) inhibitor with an IC50 of 6 nM, demonstrating significant efficacy in blocking JAK1-mediated phosphorylation of STAT6 as well as IL-6-induced phosphorylation of STAT3. This compound effectively suppresses pro-inflammatory cytokine levels, reduces paw swelling, and lowers clinical arthritis scores, thereby alleviating joint damage and diminishing bone loss. YYSW001 is particularly valuable for research related to rheumatoid arthritis and inflammation-related disorders. -
STAT3 Inhibitor
YN11 is a selective inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3) with a Kd of 11.9 μM. By directly binding to the SH2 domain, YN11 effectively inhibits the phosphorylation of STAT3, leading to decreased expression of downstream target proteins. This compound has demonstrated significant biological activity, inducing cell cycle arrest and promoting apoptosis in prostate cancer cells, while also inhibiting cell invasion and migration. In vivo studies indicate that YN11 suppresses tumor growth in prostate cancer xenograft models without causing significant body weight loss or histopathological changes in major organs, making it a valuable tool for research in prostate cancer therapy. -
JAK3 Inhibitor
JAK3-IN-20 is a selective and orally active JAK3 inhibitor, demonstrating an IC50 of 0.7473 nM. By covalently binding to JAK3 Cys909 and outcompeting ATP at the catalytic site, JAK3-IN-20 effectively blocks JAK-STAT pathway activation. This compound exhibits anti-tumor properties by inhibiting migration, proliferation, and growth of Bortezomib-resistant cancer cells, as well as inducing dose-dependent apoptosis. JAK3-IN-20 is a valuable tool for researching Bortezomib-resistant multiple myeloma. -
EGFR Inhibitor
ZW-49 is a potent orally active pan-EGFR inhibitor, demonstrating IC50 values ranging from 0.03 to 1.5 nM. This compound selectively targets various EGFR mutations while sparing wild-type EGFR and other familial targets, effectively blocking the ATP-binding pocket and a conserved hydrophobic subpocket without causing steric conflicts with PACC mutation P loops. ZW-49 exhibits significant anti-proliferative activity by inhibiting cancer cell proliferation, inducing G0/G1 phase cell-cycle arrest, and promoting apoptosis, making it a valuable reagent for cancer research, particularly in non-small cell lung cancer models. -
EGFR Inhibitor
Rinumafusp alfa is a human monoclonal antibody that specifically inhibits the epidermal growth factor receptor (EGFR) by targeting ERBB3/HER3. This compound demonstrates potential in blocking tumor cell signaling pathways, thereby impeding tumor growth and progression. It is primarily utilized in research applications focused on cancer biology and therapeutic development targeting EGFR-related pathways.
