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Catalog No.
Product Name
Application
Product Information
Citations
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ASK1 Inhibitor
ASK1-IN-2 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), demonstrating a potent inhibitory activity with an IC50 of 32.8 nM. This compound is valuable for research applications related to ulcerative colitis, as it modulates inflammatory pathways mediated by ASK1. Its orally active nature makes it suitable for in vivo studies aimed at exploring the therapeutic potential in gastrointestinal diseases. -
Survivin Dimerization Inhibitor
LQZ-7F is a potent survivin dimerization inhibitor that promotes spontaneous apoptosis in prostate cancer cells. It demonstrates dose-dependent cytotoxicity against PC-3 and C4-2 cell lines, with IC50 values of 2.99 µM and 2.47 µM, respectively. Additionally, LQZ-7F exhibits synergistic effects when combined with Docetaxel, making it valuable for research into therapeutic strategies targeting survivin in cancer treatment. -
MDM2-p53 Interaction Inhibitor
MI-1061 TFA is a potent inhibitor of the MDM2-p53 interaction, exhibiting an IC50 of 4.4 nM and a Ki of 0.16 nM. This orally bioavailable and chemically stable compound effectively activates p53, leading to apoptosis in SJSA-1 xenograft tumor tissues in murine models. MI-1061 TFA demonstrates significant anti-tumor activity, making it a valuable tool for cancer research focused on the modulation of the p53 signaling pathway. -
Mdm2-MdmX Inhibitor
MMRi64 is a selective inhibitor of the Mdm2-MdmX protein interactions. This compound downregulates Mdm2 and MdmX levels in leukemia cells, leading to increased accumulation of p53 and activation of the apoptotic pathways associated with p53. MMRi64 is a valuable tool for cancer research, particularly in the study of leukemias and lymphomas, where modulation of the p53 signaling axis is critical. -
p53-MDM2 Inhibitor
DS-5272 is an orally active inhibitor of the p53-MDM2 interaction, demonstrating an IC50 of 20 nM. This compound effectively inhibits the proliferation of SJSA-1 cells (wildtype p53, IC50 = 0.17 μM) as well as DLD-1 cells (mutant p53). DS-5272 induces cell cycle arrest and promotes apoptosis in SJSA-1 cells, while also exhibiting antitumor efficacy in vivo in mouse models. This makes DS-5272 a valuable tool for research in cancer therapeutics targeting the p53 pathway. -
MDM2-NFAT1 Inhibitor
MA242 free base is a targeted inhibitor of MDM2 and NFAT1, effectively disrupting their interaction. By binding with high affinity, MA242 promotes degradation of both proteins and suppresses NFAT1-mediated transcription of MDM2. This compound has demonstrated the ability to induce apoptosis in pancreatic cancer cell lines, providing a valuable tool for research in cancer biology and therapeutic applications, particularly in contexts where p53 is either mutated or absent. -
ASK1 Inhibitor
ASK1-IN-4 is a selective inhibitor of Apoptosis Signal-regulating Kinase 1 (ASK1), demonstrating an IC50 of 0.2 μM. This compound effectively interacts with the ATP-binding site of ASK1, leading to the modulation of apoptotic signaling pathways. ASK1-IN-4 is primarily utilized in research focused on apoptosis regulation, oxidative stress response, and related therapeutic investigations. -
Survivin Inhibitor
FL118, a potent survivin inhibitor, is a synthetic analogue of camptothecin (10,11-(Methylenedioxy)-20(S)-camptothecin). It functions by binding to the oncoprotein DDX5 (p68), leading to its dephosphorylation and degradation. FL118 is instrumental for cancer research, providing valuable insights into therapeutic strategies targeting survivin-related pathways. -
PKD/PIM2 Inhibitor
CRT0066101 is a potent and orally active inhibitor of Protein Kinase D (PKD) with IC50 values of 1 nM, 2.5 nM, and 2 nM for PKD1, PKD2, and PKD3, respectively. Additionally, it serves as an effective PIM2 inhibitor with an IC50 of approximately 135.7 nM. This compound exhibits notable anti-inflammatory activity demonstrated in LPS-induced lung injury models in mice, as well as anticancer effects, making it a valuable tool for research in cancer and inflammation-related studies. -
MDM2 Inhibitor
D-CopA3 functions as an MDM2 inhibitor, promoting the activation of the p53 signaling pathway. It demonstrates significant cytotoxicity against colorectal cancer cell lines HCT-116, LoVo, and RKO, with an IC50 ranging from 15 to 18 μM, and induces JNK/Beclin-1-mediated autophagy. Additionally, D-CopA3 reduces the expression of the cell cycle inhibitor p21Cip1/Waf1, enhances mucosal barrier function, and exhibits anti-inflammatory properties in models of acute enteritis and chronic colitis. Furthermore, it has shown anti-tumor efficacy in HCT-116 mouse xenograft models. -
ROCK Inhibitor
3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine is a selective inhibitor of Rho-associated protein kinase (ROCK), exhibiting IC50 values of 0.092 μM for PKC-α, 0.26 μM for ROCK, and 0.77 μM for ASK1. This compound demonstrates significant cytotoxic activity against human prostate cancer PC-3 cells, with an IC50 value of 0.16 μM. Its efficacy in inhibiting kinase activity makes it a valuable tool for research in cancer therapeutics and related signaling pathways. -
Caspase-3/Caspase-7 Inhibitor
Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7, targeting the proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site. This compound is crucial for studying apoptosis and cellular signaling mechanisms by selectively modulating caspase activity. Its application extends to research areas involving cell death regulation and disease models where caspase-mediated pathways play a pivotal role. -
Glutathione Peroxidase Inhibitor
4-Methylesculetin is a coumarin derivative that functions as a potent inhibitor of glutathione peroxidase. This compound exhibits significant antioxidant and anti-inflammatory properties, effectively inhibiting myeloperoxidase activity. In research applications, 4-Methylesculetin demonstrates the ability to attenuate bone resorption by downregulating elevated levels of bone-related exoglycosidases, cathepsin D, and tartrate-resistant acid phosphatases. Additionally, it reduces the expression of pro-inflammatory markers such as TNF-α, IL-1β, IL-6, COX-2, and PGE2, making it a valuable tool for studying inflammatory diseases. -
ASK1 Inhibitor
Selonsertib hydrochloride is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1). This compound exerts anti-inflammatory, anti-tumor, and anti-fibrotic effects by blocking the phosphorylation and activation of ASK1 through its binding to the catalytic kinase domain. It also attenuates the production of inflammatory cytokines and decreases the expression of fibrosis-related genes, thereby inhibiting excessive apoptosis and limiting cell proliferation. These properties make selonsertib hydrochloride a valuable tool for research in inflammation and fibrotic diseases. -
ASK1 Inhibitor
ASK1-IN-3 is a selective inhibitor of the apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 33.8 nM. This compound demonstrates significant apoptotic induction in HepG2 cancer cells and exhibits effective cell cycle arrest. Its ability to modulate the activity of several cell cycle regulating kinases renders ASK1-IN-3 valuable for research applications related to cancer therapy and cell cycle regulation studies. -
PKD Inhibitor
CRT0066101 trihydrochloride is a potent inhibitor of Protein Kinase D (PKD), exhibiting IC50 values of 1 nM, 2.5 nM, and 2 nM against PKD1, PKD2, and PKD3, respectively. In addition to its PKD-inhibitory properties, it also targets PIM2 with an IC50 of approximately 135.7 nM. This compound demonstrates significant anti-inflammatory effects in lipopolysaccharide (LPS)-induced lung injury models in mice and exhibits potential anticancer activity, making it a valuable reagent for research in oncology and inflammation. -
MDM2/4 Inhibitor
MDM2/4-p53-IN-2 is a potent dual inhibitor of MDM2 and MDM4, functioning as an activator of p53. With IC50 values of 70.7 nM and 81.4 nM for the MDM2-p53 and MDM4-p53 complexes, respectively, this compound effectively regulates the cell cycle and induces apoptosis. It demonstrates significant anticancer activity, making it a valuable tool for research focused on cancer therapeutics and the modulation of p53 signaling pathways. -
ASK1 Inhibitor
ASK1-IN-5 is a selective inhibitor of apoptosis signal-regulated kinase 1 (ASK1). This compound plays a crucial role in regulating cellular stress responses and apoptosis, making it valuable in the investigation of autoimmune and neurodegenerative diseases. Its application in research can help elucidate the mechanisms underlying these conditions and potentially guide therapeutic development. -
p53-MDM2 Inhibitor
p53-MDM2-IN-6 is a selective inhibitor of the p53-MDM2 interaction, demonstrating an IC50 of 11.08 µg/mL. This compound effectively induces cell cycle arrest in the S phase and promotes both early and late apoptosis in HT29 colorectal cancer cell lines, with an IC50 of 10.44 µg/mL. Its ability to elevate p53 levels while decreasing GST enzyme expression highlights its potential as a valuable tool for investigating therapeutic strategies in colorectal cancer research. -
p53-MDM2 Inhibitor
p53-MDM2-IN-5 is a potent inhibitor of the p53-MDM2 interaction. This compound induces apoptosis, promotes autophagy, and causes DNA damage in cells, contributing to its anti-tumor efficacy. Additionally, p53-MDM2-IN-5 effectively induces cell cycle arrest at both the S and G2/M phases, making it a valuable tool for cancer research applications focused on therapeutic strategies targeting the p53 pathway. -
MDM2-p53 Interaction Inhibitor
MI-773 TFA is a selective inhibitor of the MDM2-p53 interaction, demonstrating a Ki of 0.88 nM for MDM2. By disrupting the MDM2-TP53 interaction, MI-773 TFA effectively activates the p53 tumor suppressor pathway, leading to apoptotic cell death. This compound has shown significant anticancer activity, inducing tumor regression in xenograft models of adenoid cystic carcinoma and exhibiting therapeutic potential in neuroblastoma. MI-773 TFA serves as a valuable tool for research focused on p53-related cancer therapies. -
MDM2/MDMX Inhibitor
MDMX/MDM2-IN-2 is a potent dual inhibitor of the p53-MDM2/MDMX interaction, exhibiting inhibition constants (Kis) of 0.23 µM for MDM2 and 2.45 µM for MDMX. This compound effectively disrupts the binding of p53 to MDM2 and MDMX, thereby restoring p53's function, which leads to cell cycle arrest and apoptosis. Additionally, MDMX/MDM2-IN-2 demonstrates inhibition of cell migration and invasion, highlighting its potential for therapeutic applications in cancer research. Its antitumor activity makes it a valuable tool for studying tumor biology and exploring novel cancer treatment strategies. -
NF-κB p65 Inhibitor, Apoptosis Inducer
N-Desmethyldauricine is an inhibitor of NF-κB p65 with significant apoptotic effects. It effectively reduces p65 protein expression, induces apoptosis, and arrests the cell cycle at the G0/G1 phase. Additionally, N-Desmethyldauricine attenuates intercellular adhesion and inhibits the growth of 3D spheroids derived from triple-negative breast cancer. This compound is useful for research involving triple-negative breast cancer dynamics and therapeutic strategies. -
p53 Inhibitor
YL-1-9 is a potent inhibitor of p53 degradation mediated by MDM2, achieved through its strong binding to critical hydrophobic pockets within the MDM2 protein. This compound effectively induces cell cycle arrest and promotes apoptosis, particularly in breast cancer cells. YL-1-9 is valuable for research into p53-targeted therapies and the mechanisms of cancer cell proliferation and survival. -
GP130 D1 domain inhibitor
(R)-JAK2/STAT3-IN-1 is a selective inhibitor of the GP130 D1 domain, primarily targeting the JAK2/STAT3 signaling pathway. This compound demonstrates significant anti-tumor activity by inhibiting the phosphorylation of JAK2 and STAT3, thereby impairing tumor cell viability and migration while promoting apoptosis. With an affinity of 3.8 μM for GP130, (R)-JAK2/STAT3-IN-1 serves as a valuable tool for research into cancer biology and therapeutic interventions. -
ASK Inhibitor
ASK1-IN-6 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 7 nM in biochemical assays and 25 nM in cellular assays. This compound demonstrates potent anti-inflammatory properties and penetrates the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases, including Alzheimer's disease. Its specificity and efficacy position ASK1-IN-6 as a potential candidate for therapeutic exploration in related research applications. -
RET/BRAF/S6K/Src Inhibitor
AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases. -
RET/BRAF/S6K/Src Inhibitor
AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models. -
p53 DNA-binding inhibitor
NSC194598 is a p53 DNA-binding inhibitor that effectively disrupts the interaction between p53 and DNA, exhibiting an IC50 value of 180 nM for in vitro studies and a range of 2-40 μM for in vivo applications. This compound has been shown to interfere with the transcriptional activation of the mutated RET gene in human medullary thyroid carcinoma TT cells. NSC194598 is utilized in research investigating acute toxicity effects on normal tissues due to radiation and chemotherapy. -
RET Inhibitor
RET-IN-4 is a potent and selective RET inhibitor that demonstrates oral bioavailability, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM against wild-type RET, RET V804M, and RET M918T variants, respectively. This compound exhibits improved selectivity against kinases such as JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 is primarily utilized in cancer research, highlighting its potential for therapeutic applications in RET-driven malignancies. -
RET Inhibitor
RET-IN-14 is a highly selective RET inhibitor that demonstrates potent inhibition with IC50 values of less than 0.51 nM for wild-type RET and varying nanomolar activity against RET mutations (G810R and V804M) as well as BTK and its C481S mutant. Its exceptional efficacy positions RET-IN-14 as a valuable tool for investigating RET-driven tumors and exploring therapeutic strategies in cancer research. -
c-KIT/PDGFR/RET Inhibitor
KBP-7018 is a selective tyrosine kinase inhibitor targeting c-KIT, PDGFR, and RET. It demonstrates potent inhibition with IC50 values of 10 nM for c-KIT, 7.6 nM for PDGFR, and 25 nM for RET. This compound is valuable for investigating the molecular mechanisms and potential treatments related to idiopathic pulmonary fibrosis. -
c-KIT/PDGFR/RET Inhibitor
KBP-7018 hydrochloride is a selective inhibitor of tyrosine kinases, specifically targeting c-KIT, PDGFR, and RET. It exhibits significant inhibitory potency, with IC50 values of 10 nM, 7.6 nM, and 25 nM, respectively. This compound is utilized in research focused on idiopathic pulmonary fibrosis, facilitating investigations into pathways associated with this condition. -
ASK1 Inhibitor
CS17919 is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of 22.52 nM. This compound demonstrates significant anti-inflammatory and antifibrotic effects, making it a valuable tool for investigating metabolic-related kidney and liver diseases. Its oral bioavailability enhances its utility in preclinical studies aimed at understanding ASK1's role in disease mechanisms and potential therapeutic interventions. -
ASK1 Inhibitor
DDO3711 is a specific inhibitor of apoptosis signal-regulated kinase 1 (ASK1), exhibiting an IC50 of 164.1 nM while displaying minimal inhibition of ASK2 (IC50 > 20 μM). This compound functions by dephosphorylating phosphorylated ASK1 at threonine 838 through recruitment of the phosphatase PP5. DDO3711 demonstrates significant ASK1-dependent antiproliferative effects and shows promise in studies related to cancer by targeting abnormally phosphorylated oncoproteins. -
ASK1 Inhibitor
JT21-25 is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of 5.1 nM. This compound plays a crucial role in inhibiting apoptotic signaling pathways, making it valuable for research focused on cellular stress responses and apoptosis. JT21-25 is utilized in studies investigating the modulation of ASK1 activity in various disease models, particularly those related to neurodegenerative disorders and cancer. -
PPT1 Inhibitor
Ezurpimtrostat (hydrochloride) is a potent and selective PPT1 inhibitor with multiple biological activities. It disrupts lysosomal function, modulates autophagy, and induces apoptosis, making it a valuable tool in cancer research and immunology. This compound has demonstrated efficacy in reducing inflammatory markers such as IFN-α and CRP, as well as in lowering viral loads of SARS-CoV-2. Ezurpimtrostat is suitable for investigating conditions such as systemic lupus erythematosus, hepatocellular carcinoma, fibrosis, and other related disorders. -
Mdm2 E3 Ligase Inhibitor
MEL24 is an inhibitor of the Mdm2 E3 ligase, which plays a critical role in regulating p53 protein levels. This compound significantly reduces cell survival and enhances sensitivity to DNA-damaging agents in a p53-dependent manner. MEL24 is primarily utilized in antitumor research, contributing to studies aimed at understanding and overcoming resistance in cancer therapies. -
MDM2 E3 Ligase Inhibitor
MEL23 is an MDM2 E3 ligase inhibitor that specifically targets the E3 ligase activity of the MDM2-MDMX complex. This compound effectively inhibits the ubiquitination of MDM2 and p53, leading to decreased viability in cells expressing wild-type p53. Additionally, MEL23 stabilizes MDM2 through a mechanism that does not involve p53 transcription, making it a valuable tool for research into cancer biology and therapeutic strategies targeting the p53 pathway. -
SLC7A11 Inhibitor, GPX4 Inhibitor
Anti-NSCLC agent-2 (compound 6o) functions as a dual inhibitor of SLC7A11 and GPX4, key regulators of ferroptosis. By disrupting redox homeostasis and depleting glutathione levels, this compound facilitates the accumulation of lipid peroxides, leading to the induction of ferroptosis in non-small cell lung cancer (NSCLC) cells. Anti-NSCLC agent-2 is a valuable tool for research focused on understanding and targeting non-small cell lung cancer mechanisms.
