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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. -
Glutathione Peroxidase Inhibitor
4-Aminobenzohydrazide is a potent inhibitor of glutathione peroxidase, demonstrated to induce oxidative stress in neutrophils, with an IC50 value of 43.6 μM for reactive oxygen species (ROS) generation. This compound serves as a valuable tool for investigating oxidative stress-related mechanisms and has applications in subacute stroke research. Its ability to irreversibly inhibit myeloperoxidase further reinforces its utility in studying inflammatory processes and cellular responses. -
GPX4 Inhibitor
GPX4-IN-4 is a selective inhibitor of glutathione peroxidase 4 (GPX4). This compound demonstrates significant efficacy in disrupting GPX4 activity, leading to increased oxidative stress and cellular apoptosis. GPX4-IN-4 is particularly relevant for cancer research, as it can help elucidate the role of GPX4 in tumor growth and survival, providing insights for potential therapeutic strategies. -
GPX4-Inhibitor Affinity Probe
ML162-yne is a selective GPX4-inhibitor affinity probe that utilizes click chemistry for targeted interactions. Featuring an alkyne functional group, this reagent can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), enabling efficient conjugation with azide-containing molecules. This capability makes ML162-yne valuable for studying the role of GPX4 in various biological processes and for developing novel therapeutic strategies. -
Glutathione Peroxidase Inhibitor
Sorbifolin is a flavone glucoside that functions as a potent inhibitor of glutathione peroxidase. It exhibits myeloperoxidase inhibitory activity with an IC50 value of 19.2 nM, along with significant radical scavenging properties. Due to its ability to modulate oxidative stress-related pathways, Sorbifolin is valuable for research applications focusing on inflammatory diseases and redox homeostasis. -
GPX4 Inhibitor
GPX4-IN-15 is a specific inhibitor of GPX4, demonstrating a 19.8% inhibition at a concentration of 1 μM. This compound effectively inhibits the proliferation of various cancer cell lines, including MDA-MB-468, BT-549, and MDA-MB-231, with IC50 values of 0.86 μM, 0.96 μM, and 0.48 μM, respectively. GPX4-IN-15 is a valuable tool for researchers investigating the role of GPX4 in cancer biology and therapeutic resistance. -
GPX4 Inhibitor
GPX4-IN-17 is a selective inhibitor of GPX4, demonstrating potent cytotoxicity with an IC50 of 0.3 nM and high binding affinity (KD = 20.4 nM). This compound effectively inhibits tumor growth in xenograft models while exhibiting minimal cytotoxic effects on normal tissues. GPX4-IN-17 is a valuable tool for enhancing cancer chemotherapy and addressing tumor resistance, making it a significant reagent for antitumor research applications. -
GPX4 Inhibitor
GPX4-IN-1 is a potent inhibitor of glutathione peroxidase 4 (GPX4), a critical enzyme involved in cellular redox regulation. This compound exhibits significant antiproliferative activity, making it a valuable tool in cancer research. GPX4-IN-1 can be utilized to investigate mechanisms of cancer cell survival and sensitivity to oxidative stress, providing insights into targeted therapies for malignancies. -
STIM1-TFR1 Protein Complex Inhibitor
STIM1-TFR1-IN-1 is an inhibitor of the STIM1-transferrin receptor 1 (TFR1) protein complex, exhibiting a binding affinity (Kd) of 2.18 μM to the STIM1-CD protein. This compound effectively disrupts the STIM1-TFR1 interaction, thereby decreasing TFR1-mediated iron uptake while inhibiting ferroptosis, lipid peroxidation, and reactive oxygen species (ROS) production. STIM1-TFR1-IN-1 also enhances glutathione peroxidase 4 (GPX4) activity and improves the glutathione/oxidized glutathione ratio, promoting neuroprotective effects and mitigating brain injury. This reagent is particularly relevant for studies focusing on intracerebral hemorrhage. -
GPX4 Inhibitor
GPX4-IN-8 is a selective inhibitor of Glutathione Peroxidase 4 (GPX4), a key enzyme involved in cellular redox homeostasis. This compound exhibits significant antiproliferative activity, making it a valuable tool for research focusing on oxidative stress, ferroptosis, and cancer biology. GPX4-IN-8 can effectively facilitate investigations into the role of GPX4 in various disease models and therapeutic contexts. -
GPX4 Inhibitor
LOC1886 is a covalent inhibitor targeting glutathione peroxidase 4 (GPX4), crucial for regulating oxidative stress within cells. It exhibits robust biological activity that aids in the investigation of ferroptosis and related cell death pathways. This compound is particularly useful for research applications focused on cancer biology, neurodegenerative diseases, and the study of oxidative damage mechanisms. -
Survivin Inhibitor
MX107 is a selective survivin inhibitor known for its potent efficacy in suppressing the proliferation of triple-negative breast cancer (TNBC) cells. By inducing the degradation of survivin and inhibitor-of-apoptosis proteins (IAPs), MX107 effectively inhibits nuclear factor κB (NF-κB) activation in response to DNA damage. This compound enhances the tumoricidal effects of genotoxic treatments when used in conjunction with chemotherapeutic agents, making it a valuable tool in cancer research and therapy development. -
MDM2/XIAP Inhibitor
MDM2/XIAP-IN-1 is a potent inhibitor of both MDM2 and XIAP, exhibiting significant anti-cancer activity with an IC50 value of 0.3 μM. This compound is suitable for use in cancer research, facilitating studies aimed at dissecting the role of MDM2 and XIAP in tumor progression and survival. Its dual-targeting mechanism allows for exploration of therapeutic strategies that may enhance apoptosis in cancer cells. -
RIPK2 Inhibitor
CSLP43 is a selective inhibitor of RIPK2, demonstrating an IC50 of 19.9 nM against human RIPK2. By binding to the ATP-binding pocket of RIPK2, CSLP43 disrupts its interaction with the BIR2 domain of XIAP and cIAP1, effectively inhibiting RIPK2 ubiquitination and regulating NOD1- and NOD2-dependent inflammatory signaling pathways, as well as NF-κB activation. This compound is particularly relevant for research investigating Crohn's disease, Blau syndrome, early-onset sarcoidosis, and early-onset inflammatory bowel disease, due to its selectivity for the NOD1/NOD2 signaling pathway without affecting RIPK1 or RIPK3 activity. -
p53 Inhibitor
Pifithrin-α, p-Nitro, Cyclic is a potent p53 inhibitor that acts by blocking posttranscriptional activity of the p53 protein. This compound exhibits enhanced neuroprotective effects, demonstrating superior activity compared to traditional Pifithrin-α, particularly in cortical neurons exposed to Etoposide, with an ED50 of 30 nM. Importantly, Pifithrin-α, p-Nitro, Cyclic does not inhibit phosphorylation of p53 at the S15 residue, making it a valuable tool in studies of p53-related signaling pathways and neuroprotection research. -
MDM2 Inhibitor
SP-141 is a selective inhibitor of MDM2, a protein that regulates the p53 tumor suppressor pathway. By promoting MDM2 auto-ubiquitination and subsequent degradation, SP-141 enhances p53 activity, which can lead to increased cell cycle arrest and apoptosis. This compound is a valuable tool for investigating therapeutic strategies in pancreatic and breast cancer research. -
p53-Snail Binding Inhibitor
GN25 is a selective inhibitor of the p53-Snail protein interaction, which plays a critical role in tumorigenesis. This compound exhibits antitumor activity by disrupting the binding of these proteins, potentially leading to the restoration of p53 tumor suppressor function. GN25 is suited for research applications aimed at exploring p53 signaling pathways and evaluating therapeutic strategies for cancer treatment. -
MDM2-p53 Inhibitor
MDM2-p53-IN-16 is an inhibitor of the MDM2-p53 complex, demonstrating an IC50 value of 4.3 nM for the dissociation of the human p53/MDM2 interaction. By reactivating p53, it promotes apoptosis and cell-cycle arrest in Glioblastoma Multiforme (GBM) cells. This compound is suitable for use in cancer research, particularly in studies targeting p53 signaling pathways and therapeutic strategies for GBM. -
CDK2/MDM2 Inhibitor
CDK2/MDM2-IN-1 is a potent dual inhibitor targeting both CDK2 and MDM2, exhibiting an IC50 value of 2.60 nM for CDK2. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to simultaneously inhibit key regulatory proteins positions it as a promising candidate for studies focused on cell cycle regulation and apoptosis. -
MDM-2/p53 Inhibitor
MX69-102 is an MDM-2/p53 inhibitor that promotes the degradation of MDM2, leading to the activation of the tumor suppressor p53 and subsequent apoptosis in cancer cells. This compound demonstrates significant efficacy in inhibiting xenografted human acute lymphoblastic leukemia (ALL) characterized by MDM2 overexpression in SCID mice, making it a valuable tool for cancer research and therapeutic development targeting the MDM2/p53 pathway. -
MDM-2/p53 Inhibitor
Siremadlin (R Enantiomer) is a highly specific inhibitor of the MDM-2/p53 interaction. This compound exhibits potent biological activity in disrupting the MDM-2-mediated degradation of p53, thereby promoting p53-dependent tumor suppression. Siremadlin is valuable for research applications in cancer therapy, particularly in studies focused on restoring p53 function in tumor cells. -
MDM2/MDMX Inhibitor
ATSP-7041 is a selective dual inhibitor of MDM2 and MDMX, designed to reactivate the p53 tumor suppressor pathway. This compound demonstrates significant biological activity in p53-positive cancers, providing a potential therapeutic strategy for tumorigenesis associated with p53 pathway dysregulation. Research applications include studying the regulation of cancer cell apoptosis and the effects of p53 reactivation on tumor growth dynamics. -
p53 Inhibitor
NSC405640 is a potent inhibitor of the MDM2-p53 interaction, targeting the regulation of the p53 tumor suppressor protein. This compound effectively rescues structural mutations in p53, allowing for the restoration of its function. NSC405640 selectively inhibits the growth of cell lines expressing wild-type p53, making it a valuable tool for studying p53-related pathways and potential therapeutic applications in cancer research. -
HDM2-p53 Inhibitor
MK-4688 is a potent inhibitor of the HDM2-p53 protein-protein interaction. By disrupting this interaction, MK-4688 plays a crucial role in restoring p53 function, which is often compromised in cancer cells. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating p53 restoration and its implications in tumor suppression. -
MDM2 Inhibitor
Milademetan tosylate is a potent inhibitor of MDM2, functioning through the restoration of p53 activity by disrupting the p53-MDM2 interaction. This compound effectively arrests the cell cycle in the G1 phase and induces apoptosis, demonstrating significant anticancer activity. Milademetan tosylate shows promise in research related to Merkel cell carcinoma (MCC) and other malignancies involving dysfunctional p53 signaling. -
MDM2-p53 Inhibitor
AM-7209 is a potent and selective inhibitor of the MDM2-p53 interaction, exhibiting a dissociation constant (Kd) of 38 pM. It demonstrates significant inhibitory efficacy in the MDM2-amplified SJSA-1 osteosarcoma cell line with an IC50 of 1.6 nM. AM-7209 is primarily utilized in cancer research for its antitumor properties, specifically in studies aimed at reactivating p53 function in malignancies where MDM2 is overexpressed. -
MDM2-p53 Inhibitor
ISA 27 is a small-molecule inhibitor of the MDM2-p53 protein-protein interaction. It effectively inhibits MDM2-mediated ubiquitination and degradation of p53, thereby stabilizing p53 levels. This compound is valuable for research on p53-mutant solid tumors, including thyroid and breast cancers, and offers a potential therapeutic strategy for targeting aberrant p53 signaling pathways. -
MDM2 Inhibitor
MDM2-IN-21 is a potent inhibitor of the MDM2 protein, which plays a critical role in the regulation of the p53 tumor suppressor pathway. By disrupting the MDM2-p53 interaction, MDM2-IN-21 activates p53-dependent signaling, leading to enhanced apoptosis and cell cycle arrest in cancer cells. This compound is widely utilized in cancer research to explore therapeutic strategies targeting MDM2 and to investigate its role in tumorigenesis and cellular responses to stress. -
MDM2/MDM4 Inhibitor
RDR03871 is a potent dual inhibitor of MDM2 and MDM4, demonstrating IC50 values of 35.4 nM and 10.4 nM for the MDM2-p53 and MDM4-p53 interactions, respectively. This compound plays a significant role in cancer research by modulating p53 pathways, thus offering a potential therapeutic avenue for tumors with dysregulated MDM2/MDM4 signaling. RDR03871 is suitable for studies focused on the restoration of p53 function in malignancies. -
MDM2-p53 Inhibitor
MI-888 TFA is a potent MDM2-p53 interaction inhibitor with a Ki of 0.44 nM, demonstrating notable efficacy in disrupting the MDM2-p53 complex. This compound exhibits rapid, complete, and sustained tumor regression in xenograft mouse models, making it a valuable tool in cancer research. MI-888 TFA is suitable for studies investigating the modulation of p53 pathways and its potential therapeutic applications in oncology. -
MDM-2/p53 Interaction Inhibitor
UNP-6457 is a potent inhibitor of the MDM2/p53 interaction, exhibiting an IC50 value of 8.9 nM. This compound plays a crucial role in disrupting oncogenic pathways by stabilizing the p53 tumor suppressor protein, leading to enhanced apoptosis in cancer cells. UNP-6457 is primarily utilized in cancer research to investigate the modulation of p53 activity and evaluate potential therapeutic strategies targeting the MDM2/p53 axis. -
MDM2-p53 Inhibitor
BI-0282 is a potent inhibitor of the MDM2-p53 interaction. This compound disrupts the negative regulation of the p53 tumor suppressor by MDM2, thereby enhancing p53-mediated transcriptional activity. BI-0282 is primarily used in research applications focused on cancer therapy, specifically in studies aimed at restoring p53 function in tumor cells. Its ability to stabilize p53 makes it a valuable tool for exploring therapeutic strategies targeting MDM2 in various malignancies. -
p53-MDM2 Inhibitor
RO 2468 is a potent and selective inhibitor of the p53-MDM2 interaction, designed for oral administration. This compound exhibits significant anti-proliferative activity, effectively reducing cell growth in SJSA1 osteosarcoma models while demonstrating minimal toxicity. RO 2468 is utilized in research focused on tumor suppression and the modulation of p53 signaling pathways. -
MDM2 Inhibitor
MI-888 is a potent, orally active MDM2 inhibitor with a Ki of 0.44 nM, specifically designed to disrupt the MDM2-p53 interaction. This regulatory inhibition is critical for reactivating p53 signaling pathways, promoting apoptosis in cancer cells. With favorable pharmacokinetic properties, MI-888 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development. -
NF-κB Inhibitor/p53 Activator
CBLC100 is an NF-κB inhibitor and a p53 activator that exhibits potent anticancer properties. By targeting FACT, CBLC100 induces cytotoxicity through both p53-dependent apoptotic and non-apoptotic pathways. This compound is particularly relevant for research applications centered on cancers, including fibrosarcoma, making it a valuable tool for studying tumorigenesis and therapeutic responses. -
MDM2 Inhibitor
SP-141 hydrochloride is a selective inhibitor of MDM2, a key negative regulator of the tumor suppressor p53. By promoting MDM2 auto-ubiquitination and subsequent degradation, SP-141 enhances p53 activity, which can induce apoptosis in cancer cells. This compound is primarily utilized in research focused on pancreatic and breast cancer, providing insights into MDM2-related pathways and potential therapeutic strategies. -
MDM2/4 Dual Inhibitor
YL93 is a MDM2/4 dual inhibitor, exhibiting Ki values of 0.64 μM for MDM4 and 1.1 nM for MDM2. This compound effectively induces cell-cycle arrest and promotes apoptosis in p53-dependent contexts. YL93 is valuable for research applications focused on cancer biology and the modulation of p53 signaling pathways. -
MDM2/4-p53 Inhibitor
MDM2/4-p53-IN-1 is an effective inhibitor of both MDM2-p53 and MDM4-p53 interactions, exhibiting IC50 values of 35.9 nM and 57.4 nM, respectively. This compound demonstrates significant antiproliferative activity, making it a valuable tool for cancer research and therapeutic studies targeting p53 pathways. Its ability to modulate p53 activity positions it as a promising candidate for investigations into tumorigenesis and potential cancer treatments. -
MDM2/XIAP Inhibitor
MDM2/XIAP-IN-2 is a dual inhibitor targeting murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP). This compound promotes the degradation of MDM2 and interferes with XIAP mRNA translation, effectively hindering the proliferation of cancer cells. Notably, MDM2/XIAP-IN-2 demonstrates potent activity against the acute lymphoblastic leukemia cell line EU-1, with an IC50 value of 0.3 μM, making it a valuable tool for cancer research. -
MDM2 inhibitor
RG7112D is a potent MDM2 inhibitor that demonstrates IC50 values of 11 nM for MDM2-p53 and >10,000 nM for VHL-HIF1α, as assessed by HTRF assays. This compound is designed as a bi-functional molecule, YX-02-030, through an amide bond with VHL-Amine, enhancing its activity as a MDM2-PROTAC. RG7112D effectively stabilizes MDM2 protein and elevates p53 protein levels, making it a valuable tool for research in cancer biology and therapeutic applications targeting the p53 pathway.

