Catalog No.
Product Name
Application
Product Information
Citations
-
p53-Y220C/PLK1 Modulator
p53-Y220C/PLK1 modulator-1 is a novel dual modulator targeting the p53-Y220C mutation and Polo-like kinase 1 (PLK1). This compound exhibits significant biological activity in cancer research, providing a potential therapeutic avenue for tumors harboring the p53-Y220C alteration. Its application in cellular and molecular studies can facilitate the exploration of p53-mediated pathways and PLK1 functionality in oncogenesis. -
p53 Y220C Mutant Stabilizer
Antitumor agent-202 is a stabilizer of the p53 Y220C mutant, specifically targeting the mutated protein to enhance its functional activity. This compound demonstrates a selective inhibitory effect on the proliferation of tumor cells harboring the p53 Y220C mutation. It serves as a valuable tool in the exploration of therapeutic strategies for cancers associated with this specific mutation, facilitating research into potential treatments and cellular mechanisms. -
Apoptosis Inducer
Kevetrin (3-Cyanopropyl carbamimidothioate; 4-Isothioureidobutyronitrile) is an apoptosis inducer that functions through both p53-dependent and p53-independent mechanisms. It activates and stabilizes the p53 protein in TP53 wild-type models by modulating MDM2 processing, leading to cell cycle arrest and apoptosis. Additionally, Kevetrin demonstrates enhanced efficacy in models with mutated TP53. This compound is valuable for research applications in various cancers, including acute myeloid leukemia and breast cancer. -
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. -
p53 Activator
AKT-100 is a p53 activator that functions as a reactivation agent, disrupting the proliferation of ovarian and endometrial cancer cells at low concentrations. This compound upregulates key cell cycle regulatory genes, including p21 and GADD45, and pro-apoptotic genes such as NOXA and DR5, while inhibiting DNA repair pathways. AKT-100 is an essential tool in cancer research, facilitating studies on tumor suppression and therapeutic strategies. -
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. -
p53 Y22C Activator
p53 Activator 15 is a novel p53 Y220C activator that functions by enhancing the DNA binding affinity of the mutated p53 protein, with a SC50 value of 0.58 nM. This compound demonstrates significant antiproliferative effects on NUGC-3 gastric cancer cells and effectively inhibits tumor growth in NUGC-3 xenograft models in both mouse and rat systems. p53 Activator 15 serves as a valuable tool for investigating the role of p53 activation in gastric cancer research. -
MDM2 Inhibitor
Caylin-1 is a potent inhibitor of MDM2, functioning through direct binding to the protein to disrupt its interaction with p53. This compound is an analog of Nutlin-3 and exhibits additional binding affinity to Bcl-XL, making it a valuable tool in multi-target anticancer research. Caylin-1's unique properties facilitate investigations into oncogenic pathways and the therapeutic potential of cancer treatments targeting both MDM2 and Bcl-XL. -
DNAJA1-mutP53 R175H Inhibitor
GY1-22 is an inhibitor targeting the DNAJA1-mutP53 R175H interaction pocket. This compound exhibits significant biological activity in disrupting the function of mutant p53, an important factor in various cancer types. GY1-22 is suitable for cancer research applications, particularly in studies focused on p53 mutations and their implications in tumorigenesis. -
p53 CREB PPI
MS7972 is a small molecule that specifically disrupts the interaction between the human p53 tumor suppressor protein and the CREB binding protein. At a concentration of 50 μM, MS7972 effectively inhibits this protein-protein interaction, making it a valuable tool for investigating the regulatory mechanisms underlying cellular processes influenced by p53 and CREB. This compound is primarily used in studies focused on cancer biology and transcriptional regulation. -
MDM-2/p53
WK298 is a potent small molecule inhibitor targeting the MDM2/MDMX-p53 interaction. By preventing the binding of MDM2 and MDMX to p53, WK298 effectively activates the p53 signaling pathway, leading to significant anti-tumor activity. This compound is valuable for research applications focused on cancer biology and the therapeutic modulation of p53-mediated pathways. -
MDM2 Degrader
MD-265 is a potent MDM2 degrader utilizing the PROTAC (PROteolysis TArgeting Chimeras) technology. It effectively promotes the degradation of MDM2, resulting in the reactivation of the p53 tumor suppressor pathway in cancer cells with wild-type p53. Preclinical studies demonstrate that MD-265 induces complete tumor regression and enhances long-term survival in leukemia models, making it a valuable tool for cancer research and therapeutic development. -
MDM2/GSPT1 Degrader
WB156 is a dual degrader targeting MDM2 and GSPT1, facilitating their degradation through the recruitment of Cereblon (CRBN) to the ubiquitin-proteasome pathway. This compound effectively induces ubiquitination, leading to a reduction in MDM2 and GSPT1 levels, which is valuable for investigating the role of these proteins in cancer biology. WB156 holds potential for research applications in various cancer types, including leukemia. -
MDM-2/p53
NU-8165 is a potent inhibitor of the MDM2-p53 protein-protein interaction, exhibiting notable anti-tumor activity. Designed based on NMR titration insights to identify critical binding regions, NU-8165 effectively activates MDM2 and p21 transcription in cellular assays. This compound shows preferential effects in wild-type p53 cell lines, making it a valuable tool for studying p53 signaling and therapeutic applications in cancer research. -
MDM-2/p53 Inhibitor
AM-8553 is a potent MDM2/p53 inhibitor, exhibiting a binding affinity with a KD of 0.4 nM for MDM2. This compound demonstrates significant anti-tumor activity by disrupting the MDM2-p53 interaction, thereby stabilizing p53 and promoting its tumor suppressive functions. AM-8553 is applicable in cancer research, particularly in studies targeting the MDM2/p53 pathway for therapeutic interventions. -
MDM2 Inhibitor
TB114 is a selective inhibitor of the MDM2 protein, demonstrating a Ki value of 0.4 nM. By inhibiting MDM2, TB114 enhances the tumor-suppressive functions of p53, leading to increased apoptosis in cancer cells. This compound holds significant promise for research applications focused on cancer therapies that target the MDM2-p53 interaction. -
MDM2 Inhibitor
Siremadlin succinate is a potent MDM2 inhibitor that selectively targets the p53-binding pocket of MDM2, disrupting its ability to mediate the ubiquitination and degradation of the p53 tumor suppressor. By activating the p53 pathway, Siremadlin succinate promotes p53-dependent cell cycle arrest and apoptosis in p53 wild-type cells. This compound is valuable for research applications focused on cutaneous melanoma and other cancers with dysregulated p53 signaling. -
p53 Activator
p53 Activator 9 is a potent activator of the p53 tumor suppressor protein, exhibiting an EC50 of 1.699 μM. This compound is valuable for research applications aimed at understanding p53-mediated pathways in cancer biology, cell cycle regulation, and apoptosis. Its ability to enhance p53 activity makes it a useful tool for studying therapeutic strategies targeting the p53 pathway. -
p53 Modulator, Apoptosis Inducer
Safrole oxide is a p53 modulator that enhances the expression of the p53 tumor suppressor protein, facilitating cell cycle arrest and promoting apoptosis. This compound effectively induces apoptosis in lung cancer cells while avoiding necrotic cell death. Safrole oxide is valuable for research focused on lung cancer mechanisms and therapeutic strategies. -
S100A2-p53 Interaction Inhibitor
S100A2-p53-IN-1 is a specific inhibitor of the S100A2-p53 protein interaction. S100A2, a calcium-binding protein, plays a significant role in cell signaling and is upregulated in pancreatic cancer. This compound demonstrates potent inhibitory activity against the MiaPaCa-2 pancreatic cancer cell line, achieving a growth inhibition concentration (GI50) in the range of 1.2-3.4 μM. It serves as a valuable tool for investigating the S100A2-p53 pathway in cancer research. -
TP53-MDM2 Inhibitor
NVP-CFC218 is a selective inhibitor targeting the TP53-MDM2 interaction, effectively displacing the p53 peptide from HDM2 with an IC50 value of 1.6 nM. This compound is instrumental in assessing pharmacological sensitivity in various cell line models and is widely utilized in cancer research to study tumor suppressor pathways and MDM2-mediated p53 regulation. -
Mutant p53 Stabilizer
P53 mutant stabilizer-1 is a covalent stabilizer specifically designed to target and stabilize mutant forms of the p53 protein. By restoring the wild-type function of p53 mutants, it serves as a valuable tool in cancer research, particularly in studies focused on cancers associated with p53 mutations. This compound enhances the understanding of p53-related pathways and potential therapeutic strategies for p53-mutated tumors. -
Mutant p53 Modulator
Mutant p53 Modulator-2 (Compound 1988) selectively targets and restores the function of mutant p53 proteins, facilitating the reactivation of tumor suppressor activity. This compound has demonstrated significant biological activity in promoting cell cycle arrest and apoptosis in cancer cells harboring p53 mutations. It is valuable for research applications focused on cancer therapeutics and understanding the role of p53 in tumorigenesis. -
MDM2/p53 Inhibitor
Phage-derived 12/1 peptide is a potent inhibitor of the MDM2/p53 interaction, effectively disrupting the binding between MDM2 and p53, as well as MDMX and p53. This peptide demonstrates significant antitumor activity, exhibiting IC50 values of 0.15 μM for MDM2 and 1.25 μM for MDMX. It serves as a valuable tool for research investigating the modulation of p53 activity and the therapeutic potential in targeting MDM2/MDMX pathways in cancer. -
p53 Activator
p53 Activator 8 is a potent activator of the p53 tumor suppressor protein. It exhibits significant anti-proliferative activity, particularly against MCF7 breast cancer cell lines, with an IC50 value of 0.5 μM. This compound is valuable for research into cancer biology and therapeutic strategies that aim to restore p53 function in tumor cells. -
MDM2/MDMX-p53 Interaction Inhibitor
pDI is a synthetic peptide that functions as an inhibitor of the MDM2 and MDMX-p53 interactions, exhibiting half-maximal inhibitory concentrations (IC50) of 10 nM and 100 nM, respectively. This compound is essential for research focused on colorectal cancer, providing insights into tumor suppression mechanisms and the modulation of p53 activity. Its ability to disrupt these critical protein-protein interactions makes pDI a valuable tool in cancer therapeutic studies. -
p53 Inducer
PK7242 is a potent inducer of mutant p53 reactivation, specifically targeting the p53-Y220C variant in cancer cells. This compound promotes growth inhibition, triggers cell-cycle arrest, and initiates apoptosis in tumor cells harboring the Y220C mutation. PK7242 is a valuable tool for investigating therapeutic strategies aimed at targeting p53 deficiencies in cancer research. -
MDM2 Antagonist
MI-219 is an MDM2 antagonist with a Ki of 13.3 μM, specifically designed to disrupt the interaction between MDM2 and p53. This compound effectively inhibits the proliferation of FSCCL cells, demonstrated by an IC50 of 2.5 μM. MI-219 is suitable for research applications focused on cancer biology, particularly in studies exploring pathways related to tumor suppression and the p53 signaling axis. -
p53-MDM2 Inhibitor
p53-MDM2-IN-2 is an orally active inhibitor targeting the p53-MDM2 interaction, exhibiting a Ki value of 0.25 μM. This compound demonstrates antitumor activity through the inhibition of the NF-κB signaling pathway. It is valuable in research studies focusing on cancer therapy and elucidating the molecular mechanisms of tumor suppression. -
MDM2 Inhibitor
MI-1063 is a selective inhibitor of MDM2 that disrupts the MDM2-p53 interaction, thereby activating the tumor suppressor activity of p53. This compound effectively inhibits the proliferation of cancer cell lines RS4-11 and MV4-11, demonstrating IC50 values of 179 nM and 93 nM, respectively. Additionally, MI-1063 serves as a valuable target protein ligand in the synthesis of the PROTAC degrader MD-265, facilitating advancements in targeted protein degradation research. -
MDM2 Inhibitor
MDM2-IN-26 is an inhibitor targeting MDM2, a critical negative regulator of the tumor suppressor p53. By disrupting the MDM2-p53 interaction, this compound effectively activates p53's tumor suppressor functions, providing a promising approach for cancer research. MDM2-IN-26 can be utilized to study the modulation of p53 activity in various cancer models and therapeutic applications. -
MDM2 Antagonist
Nutlin 1 is a potent MDM2 antagonist that reactivates the p53 pathway, playing a critical role in cell cycle regulation and apoptosis. With an IC50 of 0.26 μM, it effectively disrupts the MDM2-p53 interaction, promoting p53-mediated transcriptional activity. This compound is widely used in cancer research to explore the therapeutic potential of p53 reactivation in tumor cells. -
p53-MDM2 Inhibitor
p53-MDM2-IN-3 is a potent p53-MDM2 inhibitor with a Ki value of 0.25 μM, demonstrating oral bioavailability. This compound exhibits significant antitumor activity through its inhibition of the NF-κB signaling pathway. It serves as a valuable tool for cancer research, particularly in studies focused on targeting the p53-MDM2 interaction and the subsequent effects on tumor proliferation and survival. -
p53 (Y220C) Activator
p53 Activator 11 is a potent activator of the p53 (Y220C) mutant, exhibiting an EC50 value of 0.478 µM. This compound plays a critical role in enhancing the activity of mutant p53, making it a valuable tool for cancer research. It may facilitate studies aimed at understanding p53-mediated signaling pathways and therapeutic strategies for p53-related malignancies. -
MDM2-p53 Inhibitor
MDM2-p53-IN-18 is a potent inhibitor of the MDM2-p53 protein-protein interaction. This compound effectively disrupts the binding of MDM2 to the tumor suppressor p53, leading to the stabilization and activation of p53. It demonstrates significant biological activity in promoting apoptosis and cell cycle arrest in cancer cells, making it valuable for research applications in oncology and drug discovery targeting p53-related pathways. -
MDM2-p53 Inhibitor
Nutlin-2 is a selective inhibitor of the interaction between MDM2 and p53, exhibiting an IC50 of 0.14 μM. By occupying the hydrophobic pocket of MDM2, Nutlin-2 effectively disrupts the protein-protein interaction crucial for the regulation of p53, allowing for the stabilization and activation of this tumor suppressor. This compound is primarily utilized in cancer research to study p53-mediated pathways and to explore therapeutic avenues in tumors with MDM2 overexpression. -
MDM2 Inhibitor
RO5353 is an orally active MDM2 inhibitor that effectively disrupts the p53-MDM2 interaction, with an IC50 of 7 nM for MDM2. It demonstrates potent inhibitory effects on the proliferation of wild-type p53 cancer cells, achieving an average IC50 of 7 nM. In vivo studies reveal that RO5353 possesses significant antitumor efficacy and favorable pharmacokinetic properties in murine models, making it a valuable tool for cancer research focused on p53 pathway modulation. -
MDM-2/p53 Inhibitor
MDM2-p53-IN-20 is a synthetic inhibitor targeting the MDM2-p53 protein interaction. This compound disrupts the binding of MDM2 to p53, promoting the stabilization and activation of p53, a critical tumor suppressor involved in cell cycle regulation and apoptosis. MDM2-p53-IN-20 is primarily utilized in cancer research to study p53 pathway activation and to explore therapeutic strategies for tumors exhibiting MDM2 overexpression. -
PKC/PKD Inhibitor
PKC/PKD-IN-1 is a potent dual inhibitor of protein kinase C and protein kinase D, exhibiting an IC50 of 0.6 nM against PKD1. This compound demonstrates the ability to mitigate cardiac hypertrophy induced by high-salt diets, making it a valuable tool for investigating mechanisms related to heart failure. Its specificity and efficacy position it as a significant reagent for researchers focused on cardiac disease and kinase signaling pathways. -
PKD Inhibitor
3-IN-PP1 is a selective inhibitor of protein kinase D (PKD), demonstrating potent inhibition across PKD isoforms PKD1, PKD2, and PKD3 with IC50 values of 108 nM, 94 nM, and 108 nM, respectively. This compound exhibits broad-spectrum anticancer activity, effectively inhibiting the proliferation of various tumor cell lines. 3-IN-PP1 serves as a valuable tool for cancer research, particularly in studying the role of PKD signaling pathways in tumor growth and development. -
PKD Inhibitor
Protein kinase D inhibitor 1 is a potent pan-PKD inhibitor that exhibits IC50 values between 17 to 35 nM. This compound selectively inhibits the phosphorylation of cortactin mediated by Protein kinase D, thereby influencing cellular processes related to cytoskeletal dynamics and signal transduction. It is valuable for research applications focused on studying PKD signaling pathways and their impact on various cellular functions. -
RIPK2/3 Inhibitor
RIPK2/3-IN-2 is a potent dual inhibitor of receptor-interacting protein kinases 2 and 3 (RIPK2 and RIPK3), exhibiting IC50 values of 12 nM and 18 nM, respectively. This compound effectively induces necroptosis, showcasing an EC50 value of 0.16 μM. RIPK2/3-IN-2 can be utilized in research exploring programmed cell death mechanisms and the role of necroptosis in various pathological conditions. -
PERK Activator
MK-28 is a potent and selective activator of the protein kinase PERK (PKR-like ER kinase). This compound demonstrates significant pharmacokinetic properties, with a notable ability to penetrate the blood-brain barrier in murine models. MK-28 is primarily used in research related to ER stress response and unfolded protein response pathways, providing valuable insights into cellular homeostasis and neurodegenerative diseases. -
PERK Inhibitor
PERK-IN-2 is a highly potent inhibitor of the PERK (PKR-like ER kinase) pathway, exhibiting an IC50 of 0.2 nM. This compound effectively modulates unfolded protein response (UPR) signaling, making it valuable for studies investigating the roles of PERK in cellular stress responses and related diseases. Applications include research on cancer biology, neurodegeneration, and metabolic disorders.
