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Catalog No.
Product Name
Application
Product Information
Citations
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HDAC inhibitor
MC1742 is a potent pan-HDAC inhibitor with broad activity across multiple HDAC isoforms, exhibiting IC₅₀ values of 0.1 μM (HDAC1), 0.11 μM (HDAC2), 0.02 μM (HDAC3), 0.007 μM (HDAC6), 0.61 μM (HDAC8), 0.04 μM (HDAC10), and 0.1 μM (HDAC11). It effectively increases acetylation of histone H3 and α-tubulin, markers of HDAC inhibition. MC1742 inhibits the growth of cancer stem cells (CSCs), and induces growth arrest, apoptosis, and differentiation, particularly in sarcoma CSC models, making it a promising candidate for targeting therapy-resistant cancer cell populations. -
HDAC6 inhibitor
SelSA is a selective and orally active histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 56.9 nM. It also inhibits ERK1/2 phosphorylation, contributing to its anticancer effects. SelSA suppresses the proliferation of breast cancer and hepatocellular carcinoma cells with IC₅₀ values ranging from 0.58 to 2.6 μM, inhibits migration and invasion of Huh7 cells, and induces apoptosis. In vivo, SelSA demonstrates significant antitumor activity, supporting its potential as a therapeutic agent for solid tumors. -
HDAC inhibitor
KH16 is a potent histone deacetylase (HDAC) inhibitor with low nanomolar activity, selectively targeting class I HDACs—HDAC1, HDAC2, and HDAC3—with IC₅₀ values ranging from 6 to 34 nM. It effectively induces apoptosis and exhibits broad-spectrum antitumor activity across cancer cells with diverse gene expression profiles, making it a promising candidate for epigenetic cancer therapy research. -
ErbB2 inhibitor
AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease. -
NF-κB p65 Inhibitor
Licochalcone D is a naturally occurring flavonoid primarily found in the root of *Glycyrrhiza uralensis* (Chinese licorice). It functions as a potent and orally active inhibitor of the NF-κB p65 subunit, a key regulator of inflammation and cancer-related signaling pathways. Licochalcone D exhibits broad pharmacological properties, including antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for research in inflammation-related diseases and oncology. -
HDAC6 inhibitor
AES-350 is a potent and orally bioavailable histone deacetylase 6 (HDAC6) inhibitor, with an IC₅₀ of 0.0244 μM and a Kᵢ of 0.035 μM. It also exhibits inhibitory activity against HDAC3 and HDAC8, with IC₅₀ values of 0.187 μM and 0.245 μM, respectively. AES-350 induces apoptosis in acute myeloid leukemia (AML) cells through HDAC inhibition, making it a promising compound for AML research and the development of epigenetic-based cancer therapies. -
POLA1-HDAC11 Inhibitor
GEM144 is a potent and orally bioavailable dual inhibitor of DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It promotes p53 acetylation, induces p21 activation, and triggers G1/S cell cycle arrest followed by apoptosis. GEM144 exhibits significant antitumor efficacy in human orthotopic malignant pleural mesothelioma xenograft models, highlighting its potential as a targeted therapeutic agent for aggressive thoracic malignancies. -
POLA1/HDAC 11 Inhibitor
MIR002 is a potent, orally bioavailable dual inhibitor targeting DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It induces p53 acetylation, upregulates p21 expression, and triggers G1/S cell cycle arrest followed by apoptosis. MIR002 demonstrates significant antitumor efficacy in vivo, highlighting its potential as a therapeutic agent for cancers driven by POLA1 and HDAC11 dysregulation. -
TAK1 inhibitor
HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA). -
Casein Kinase inhibitor
BTX-A51 (Casein Kinase Inhibitor A51) is a potent, orally bioavailable inhibitor of casein kinase 1α (CK1α). It effectively induces apoptosis in leukemia cells and demonstrates strong anti-leukemic activity in preclinical models, making it a promising therapeutic candidate for hematologic malignancies. -
SUV39H1 methyltransferase inhibitor
F5446 (Compound 1) is a selective small-molecule inhibitor of the histone methyltransferase SUV39H1. By reducing H3K9 trimethylation (H3K9me3) at the Fas promoter, F5446 upregulates Fas expression and enhances the sensitivity of colorectal carcinoma cells to Fas ligand (FasL)-induced apoptosis in vitro. In vivo, F5446 effectively suppresses the growth of human colorectal tumor xenografts, highlighting its potential as an epigenetic therapeutic agent in cancer treatment. -
ASK1 Inhibitor
ASK1-IN-11 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of less than 200 nM. This compound also demonstrates inhibitory effects on TNF-α, MYLK/MLCK kinases, and hERG potassium channels. The primary research applications of ASK1-IN-11 include investigations into inflammation-related pathways. -
ASK1 Inhibitor
TC ASK 10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of 14 nM. This compound demonstrates minimal inhibitory activity against a range of other kinases, with ASK2 being the only exception, showing an IC50 of 0.51 μM. TC ASK 10 is valuable for research applications focused on apoptosis regulation and cellular stress response pathways. -
Granzyme B/Caspase-8 Inhibitor
Ac-IETD-CHO is a potent, reversible inhibitor of granzyme B and caspase-8. By blocking these proteases, Ac-IETD-CHO effectively inhibits Fas-mediated apoptotic cell death, as well as preventing hemorrhage and liver failure. This compound is valuable for research in apoptosis, immune response, and the modulation of cytotoxic T lymphocyte-induced cell death. -
MDM2 Inhibitor
Milademetan tosylate hydrate is a selective, orally active inhibitor of MDM2, primarily utilized in research focused on acute myeloid leukemia (AML) and solid tumors. This compound induces G1 cell cycle arrest, promotes cellular senescence, and triggers apoptosis, making it a valuable tool for studying the therapeutic potential in cancer treatment and the underlying mechanisms of tumor biology. -
Mdm2-MdmX RING Domain Inhibitor
MMRi6 is an Mdm2-MdmX RING domain inhibitor that disrupts the RING-RING interaction between Mdm2 and MdmX. This compound effectively inhibits MdmX-stimulated Mdm2 autoubiquitination and Mdm2-MdmX-mediated polyubiquitination of p53 in vitro, while sparing NEDD4-1 autoubiquitination. MMRi6 promotes stabilization and accumulation of p53, leading to PARP cleavage in wild-type p53 Emu-myc lymphoma cells. It demonstrates growth inhibition of wild-type p53 and p53-null Emu-myc lymphoma cells with IC50 values of approximately 0.5 μM and 3 μM, respectively, making it a valuable tool for studying leukemia and lymphoma. -
PKD Inhibitor
BPKDi is a potent inhibitor of Protein Kinase D (PKD), targeting PKD1, PKD2, and PKD3 with IC50 values of 1 nM, 9 nM, and 1 nM, respectively. This compound effectively disrupts signal-dependent phosphorylation and nuclear export of class IIa histone deacetylases (HDACs) in cardiomyocytes, consequently attenuating cellular hypertrophy. BPKDi serves as a valuable tool for investigating the role of PKD in cardiovascular research and therapeutic interventions. -
GPX4 Inhibitor
GPX4-IN-11 is a potent inhibitor of GPX4, demonstrating a KD of 45.7 μM. This compound is significant in the study of ferroptosis, enabling researchers to investigate the mechanisms underlying oxidative stress and cell death. Its utility in various biological assays contributes to the understanding of GPX4's role in disease processes and potential therapeutic approaches. -
GPX4 Inhibitor
GPX4-IN-13 is a potent inhibitor of GPX4, targeting its role in cellular antioxidant defense mechanisms. This compound exhibits significant anticancer activity by promoting ferroptosis and reducing proliferation in thyroid cancer cells. It demonstrates inhibitory effects on the growth of various thyroid cancer cell lines, with IC50 values of 8.39 μM for N-thy-ori-3-1, 10.28 μM for MDA-T32, and 8.18 μM for MDA-T41. GPX4-IN-13 is instrumental for research in cancer biology and therapeutic development targeting GPX4-dependent pathways. -
GPX4 Inhibitor
GPX4-IN-12 is a non-covalent inhibitor of Glutathione Peroxidase 4 (GPX4), primarily targeting this enzyme to induce ferroptosis. This compound effectively inhibits cell proliferation in HT1080 cells, making it a valuable tool for studying the mechanisms of ferroptosis and its implications in cancer research. GPX4-IN-12 is suitable for investigations into oxidative stress and related pathways within various biological contexts. -
GPX4 Inhibitor
GPX4-IN-21 is a selective inhibitor of glutathione peroxidase 4 (GPX4), a key regulator in cellular redox homeostasis. This compound effectively induces ferroptosis by downregulating ferroptosis-related proteins, including SLC7A11, SLC11A2, and GPX4, leading to increased levels of reactive oxygen species (ROS) and malondialdehyde (MDA). GPX4-IN-21 demonstrates significant anti-proliferative activity and is useful for investigating therapeutic strategies in cancer research, particularly in models of melanoma. -
GPX4 Inhibitor
NPD4928 is a potent GPX4 inhibitor that enhances RSL3-dependent ferroptosis through its unique mechanism of action. By binding to ferroptosis suppressor protein 1 (FSP1), NPD4928 effectively inhibits its enzymatic activity, thereby promoting ferroptotic cell death. This compound is valuable for research applications focused on studying ferroptosis pathways and identifying potential therapeutic targets in cancer and neurodegenerative diseases. -
GPX4 Inhibitor
GPX4-IN-6 is a covalent inhibitor of GPX4, exhibiting an IC50 of 0.13 μM. This compound effectively induces ferroptosis, making it a valuable tool for studying mechanisms related to triple-negative breast cancer (TNBC). Its role in modulating oxidative stress pathways presents significant implications for cancer research and therapeutic development. -
GPX4 Inhibitor
JKE-1716 is a potent and selective inhibitor of glutathione peroxidase 4 (GPX4). It induces ferroptosis through the covalent modification of GPX4, making it a valuable tool for studying iron-dependent cell death mechanisms. This compound is applicable in research focusing on cancer biology, neurodegenerative diseases, and oxidative stress-related studies. -
GPX4 Inhibitor
RSL3-NH2 is a selective inhibitor of GPX4, a crucial regulator of lipid peroxidation and ferroptosis. By promoting ferroptosis in cancer cells, RSL3-NH2 serves as an effective tool for studying cell death pathways and cancer metabolism. Additionally, this compound can be utilized as a cytotoxic payload in the development of antibody-drug conjugates (ADCs), enhancing targeted therapeutic strategies in cancer research. -
GPX4 Inhibitor
GPX4-IN-9 is a selective inhibitor of glutathione peroxidase 4 (GPX4), effectively promoting ferroptosis under both in vitro and in vivo conditions. This compound demonstrates significant cytotoxic effects on pancreatic cancer cells, making it a valuable tool for cancer research. Its mechanisms of action offer insights into the role of GPX4 in cancer cell survival and potential therapeutic strategies targeting ferroptosis. -
GPX4 Inhibitor
GPX4-IN-19 is a potent inhibitor of GPX4, exhibiting an IC50 of 0.311 μM through covalent binding to the Sec 46 site. This compound demonstrates significant anti-proliferative effects with a high selectivity for inducing ferroptosis, characterized by intracellular Fe2+ accumulation and elevated levels of lipid peroxides (LPOs) and reactive oxygen species (ROS). GPX4-IN-19 is particularly relevant for research in Triple-Negative Breast Cancer (TNBC), as it induces ferroptosis and subsequent DNA damage. -
GPX4 Inhibitor
JKE-1674 is a potent inhibitor of glutathione peroxidase 4 (GPX4), functioning through modulation of cellular redox status. This orally active compound, an analog of ML-210 with a structural modification to the nitroisoxazole ring, demonstrates strong cytotoxicity against LOX-IMVI cells, akin to that of ML-210. Notably, cell viability is restored upon treatment with ferroptosis inhibitors, underscoring its utility in studying ferroptotic cell death pathways and oxidative stress in various biological contexts. -
GPX4 Inhibitor
GPX4-IN-3 is a selective inhibitor of glutathione peroxidase 4 (GPX4), serving as a potent inducer of ferroptosis. At a concentration of 1 μM, GPX4-IN-3 demonstrates 71.7% inhibition of GPX4 activity. This compound is valuable for research applications focused on oxidative stress, cell death mechanisms, and potential therapeutic strategies against various cancers and neurodegenerative diseases. -
GPX4 Inhibitor
GPX4-IN-5 is a potent covalent inhibitor of GPX4, exhibiting an IC50 of 0.12 μM. This compound induces ferroptosis, demonstrating significant anti-tumor activity. GPX4-IN-5 is particularly relevant for research applications focused on triple-negative breast cancer (TNBC). -
MDM2-MDM4 Inhibitor
MMRi62 is an MDM2-MDM4 inhibitor that promotes ferroptosis by targeting negative regulators of the tumor suppressor p53. It exhibits P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induces autophagy. MMRi62 augments reactive oxygen species levels and triggers lysosomal degradation of ferritin heavy chain (FTH1), while also facilitating the proteasomal degradation of mutant p53. Moreover, MMRi62 demonstrates efficacy in vivo by inhibiting orthotopic xenograft models of PDAC characterized by frequent KRAS and TP53 mutations, supporting its potential in cancer research applications. -
MDM-2/p53 MDM2 Inhibitor
CTX1 is a selective inhibitor of MDM2, designed to alleviate HdmX-mediated repression of the tumor suppressor protein p53. This compound demonstrates significant anti-cancer activity, particularly in mouse models of acute myeloid leukemia (AML). CTX1 is utilized in research focused on cancer therapeutics and the modulation of p53 pathways. -
MDM-2/p53 MDM2 Inhibitor
p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a selective inhibitor of the interaction between the tumor suppressor protein p53 and its negative regulator MDM2. This compound enhances p53 activity, highlighting its potential as an anticancer agent by promoting apoptosis in p53-deficient tumors. It is valuable for research applications focused on cancer therapy, cell cycle regulation, and the molecular mechanisms of tumorigenesis. -
p53-MDM2/X Inhibitor
p53-MDM2-IN-4 is a potent inhibitor of the p53-MDM2/X protein interaction, displaying a Ki value of 3.079 μM. This compound effectively disrupts the MDM2-mediated inhibition of p53, promoting the stabilization and activation of the tumor suppressor protein. p53-MDM2-IN-4 holds significant potential in anti-tumor research and therapeutic development targeting cancer's reliance on the p53 pathway. -
p53-MDM2/X Inhibitor
p53-MDM2-IN-1 is an inhibitor of the p53-MDM2/X protein interaction, exhibiting a Ki value of 23.35 µM. This compound is valuable for anti-tumor research, as it disrupts the interaction between p53 and MDM2/X, potentially restoring p53 function in cancer cells. Its application can enhance the understanding of tumor biology and contribute to the development of novel therapeutic strategies targeting this pathway. -
MDM-2/p53 MDM2 Inhibitor
NVP-CGM097 sulfate is a selective inhibitor of the MDM2-p53 interaction, demonstrating an IC50 of 1.7±0.1 nM for human MDM2. This compound effectively disrupts the MDM2-mediated suppression of p53, leading to the activation of p53-dependent pathways. NVP-CGM097 sulfate is utilized in research focused on cancer therapeutics and the modulation of tumor suppressor activities. -
p53 Ubiquitination Inhibitor
Hdm2 E3 ligase inhibitor 1 is a reversible inhibitor targeting the Hdm2 E3 ubiquitin ligase, which regulates the ubiquitination of the p53 tumor suppressor protein. With an IC50 value of 12.7 μM, this compound effectively inhibits the transfer of ubiquitin from preligated Ub-Ubc4 to p53, resulting in the stabilization of p53 protein levels within tumor cells. Its role in preventing p53 ubiquitination positions Hdm2 E3 ligase inhibitor 1 as a valuable tool for research in cancer biology and therapeutic development. -
p53-MDM2 Binding Inhibitor
NU-8231 is a potent inhibitor of the p53-MDM2 interaction, exhibiting an IC50 range of 5.3-200 μM. This compound is instrumental in cancer research, facilitating studies on the restoration of p53 function and the modulation of apoptotic pathways. Its ability to disrupt the p53-MDM2 binding offers potential insights into therapeutic strategies targeting p53-mediated tumor suppression. -
MDM2 Inhibitor
AM-6761 is a highly potent inhibitor of MDM2, exhibiting an IC50 of 0.1 nM. This compound is crucial for studies on cancer biology, particularly in understanding the regulatory mechanisms of p53 and its interactions with MDM2. AM-6761 is primarily used in cancer research to evaluate potential therapeutic strategies targeting MDM2-mediated pathways. -
MDM-2/p53 MDM2 Inhibitor
AM-8735 is a selective inhibitor of the MDM2 protein, targeting its interaction with the p53 tumor suppressor. It exhibits potent activity with an IC50 of 25 nM, making it a valuable tool for cancer research. This compound is utilized in studies investigating the reactivation of p53 in tumor models, offering potential insights into therapeutic strategies for p53-deficient cancers. -
PERK Inhibitor
AMG PERK 44 is a highly selective inhibitor of the protein kinase PERK, exhibiting an IC50 of 6 nM. It demonstrates significant selectivity, being 1000-fold more potent than GCN2 (IC50 = 7300 nM) and 160-fold more selective over B-Raf (IC50 > 1000 nM). This compound has been shown to induce autophagy, making it a valuable tool for research into cellular stress responses and related metabolic pathways. -
ASK1 Inhibitor
ASK1-IN-1 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with a cell IC50 of 138 nM and a biochemical IC50 of 21 nM. This compound is designed to penetrate the central nervous system (CNS) and is suitable for use in research investigating the roles of ASK1 in cellular apoptosis and neurodegenerative disorders. Its inhibitory activity makes it a valuable tool for exploring therapeutic strategies targeting ASK1-related pathways. -
ASK Inhibitor
MSC 2032964A is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 96 nM. This compound is shown to preserve visual responses in experimental autoimmune encephalomyelitis (EAE) mouse models and has significant efficacy in reducing neuroinflammation. Its application in research includes studies on neurodegenerative conditions and the modulation of inflammatory pathways. -
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. -
RIPK1 inhibitor
RIPK1-IN-36 is a potent inhibitor of receptor-interacting protein kinase 1 (RIPK1) with an EC50 of less than 25 nM. This compound is valuable for investigating the role of RIPK1 in various pathological conditions, including inflammatory diseases and neurodegenerative disorders. Researchers can utilize RIPK1-IN-36 to explore the therapeutic potential of targeting RIPK1 signaling pathways in relevant biological models. -
Survivin Inhibitor
LQZ-7I is a potent inhibitor of survivin, specifically targeting its dimerization. By disrupting survivin interactions, LQZ-7I effectively induces cell death and decreases cancer cell viability. This compound demonstrates significant anti-tumor activity in xenograft models, contributing to reduced tumor growth and survivin depletion within tumor tissues, making it valuable for cancer research applications. -
Survivin and Op18 Inhibitor
GDP366 is a dual inhibitor of survivin and Op18, effectively targeting these proteins to impede cancer cell proliferation. This compound demonstrates significant cell growth inhibition, promotes cellular senescence, and induces mitotic catastrophe in human cancer cells. Its mechanism of action makes GDP366 valuable for research related to cancer biology and therapeutic strategies. -
Survivin Inhibitor
LLP-3 is a potent inhibitor of Survivin, targeting the interaction between Survivin and Ran in cancer cells. This compound demonstrates significant potential in the study of Glioblastoma multiforme (GBM), aiding in the understanding of cancer cell viability and proliferation. LLP-3 provides valuable insights into therapeutic strategies aimed at disrupting key survival pathways in tumors. -
Survivin Inhibitor
AQIM-I is a potent inhibitor of survivin, effectively reducing its expression and colony formation in cancer cells. This compound induces reactive oxygen species (ROS) production, leading to apoptosis, cell cycle arrest, DNA damage, and autophagy. AQIM-I demonstrates significant efficacy against non-small cell lung cancer cells A549, exhibiting an IC50 value of 9 nM, making it a valuable tool for investigating survivin-related pathways in cancer research. -
Survivin Inhibitor
MX106 is a potent inhibitor of survivin, a protein that plays a critical role in inhibiting apoptosis. This compound demonstrates significant anti-proliferative activity against human melanoma, epidermoid carcinoma, and colon cancer cell lines. Additionally, MX106 effectively targets multidrug-resistant cell lines that overexpress P-glycoprotein, making it a valuable tool for cancer research and the development of novel therapeutic strategies.
