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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. -
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. -
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. -
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. -
Survivin Inhibitor
Isonanangenine B is a selective inhibitor of survivin, exhibiting an IC50 of 1.6 µM. It effectively obstructs the interaction of critical transcription factors, including Stat3 and NF-κB, with the survivin promoter. This compound holds potential for advancing cancer research, particularly in elucidating the mechanisms of survivin modulation in tumorigenesis. -
ASK1 Inhibitor
ASK1-IN-10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of less than 200 nM. In addition to its primary mechanism, ASK1-IN-10 exhibits inhibitory activity against hERG potassium channels. This compound serves as a valuable tool for investigating the role of ASK1 in inflammation-related research and its potential therapeutic implications. -
ASK1 Inhibitor
ASK1-IN-8 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM. This compound demonstrates significant hepatoprotective effects in experimental models, notably reducing plasma alanine transaminase (ALT) levels in acetaminophen-induced liver injury. ASK1-IN-8 is suitable for research applications focused on liver pathologies and the modulation of apoptosis signaling pathways. -
ASK1 Inhibitor
ASK1-IN-9 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of less than 200 nM. This compound is primarily utilized in research focused on inflammation pathways, offering insights into the role of ASK1 in cellular stress responses and programmed cell death. Its potent inhibitory effects make it a valuable tool for exploring therapeutic strategies in related diseases. -
ASK1 Inhibitor
ASK1-IN-7 is an inhibitor specifically targeting Apoptosis signal-regulating kinase 1 (ASK1). This compound is derived from a recognized ASK1 inhibitor scaffold and exhibits significant potential in modulating the ASK1 signaling pathway. Its biological activity supports research into cell stress responses, inflammation, neurodegenerative disorders, and cardiovascular diseases. ASK1-IN-7 serves as a valuable tool for understanding the role of ASK1 in various pathophysiological processes. -
DAPK1/ZIPK Inhibitor
HS38 is a selective ATP-competitive inhibitor targeting death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also known as DAPK3), with Kds of 300 nM and 280 nM, respectively. Additionally, HS38 demonstrates inhibitory activity against PIM3 with an IC50 of 200 nM. This compound is valuable for research into smooth muscle-related disorders, aiding in the understanding of the underlying molecular mechanisms and potential therapeutic pathways. -
DAPK3 Inhibitor
HS148 is a selective inhibitor of Death-associated protein kinase 3 (DAPK3) with a Ki value of 119 nM. This compound effectively modulates DAPK3 activity, making it a valuable tool for studying its role in apoptosis and various signaling pathways. HS148 is suitable for applications in cancer research and investigations into neurodegenerative conditions where DAPK3 is implicated. -
DAPK1 Inhibitor
DAPK1-IN-1 is a selective inhibitor of death-associated protein kinase 1 (DAPK1) with a Kd value of 0.63 μM. This compound exhibits potential in modulating DAPK1 activity, making it a valuable tool for investigating pathways involved in neurodegenerative diseases, particularly Alzheimer’s disease. Researchers can utilize DAPK1-IN-1 to explore its effects on cell death and survival mechanisms in various cellular contexts. -
DAPK Inhibitor
CK156 is a selective inhibitor of death-associated protein kinase (DAPK), exhibiting an IC50 of 182 nM in the DRAK1 NanoBRET assay. Additionally, it shows inhibition of CK2a1 and CK2a2 at concentrations of 34 μM and 39 μM, respectively. This compound is valuable for investigating autoimmune and inflammatory diseases, providing insights into the regulation of cell death and survival pathways. -
DAPK3 Inhibitor
HS94 is a selective inhibitor of DAPK3 (Death-associated protein kinase 3), a serine/threonine kinase involved in various cellular processes, including apoptosis and inflammation. This compound has demonstrated significant biological activity by modulating DAPK3 signaling pathways, making it a valuable tool in hypertension research. Investigating HS94's effects may provide insights into the molecular mechanisms underlying cardiovascular diseases and potential therapeutic approaches. -
DAPK Inhibitor
DAPK-IN-2 is an inhibitor of Death-Associated Protein Kinase (DAPK), a key regulator involved in apoptosis and autophagy. This compound exhibits potential anti-apoptotic properties and is relevant in the study of cerebral infarction and ischemic diseases. Researchers can utilize DAPK-IN-2 to investigate the role of DAPK in cell death pathways and evaluate therapeutic approaches for neuroprotective strategies.

