Catalog No.
Product Name
Application
Product Information
Citations
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CDK9 Inhibitor
CDK9-IN-34 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9) with an IC50 value of 0.25 μM. It demonstrates significant cytotoxic effects on cancer cell lines HCT116, MCF7, and K652, with IC50 values of 1.43 μM, 3.01 μM, and 50.27 μM, respectively. Additionally, CDK9-IN-34 exhibits antiviral properties against coronavirus 229E, displaying an IC50 of 145.92 μM. This compound serves as a valuable tool for investigating the roles of CDK9 in cancer and viral pathogenesis. -
10-Methoxycamptothecin Prodrug
MG16 is a prodrug of 10-Methoxycamptothecin, primarily targeting CDK6 and ASK1. It effectively induces cell cycle arrest and apoptosis in cancer cells, demonstrating significant anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer. This compound is valuable for research applications focused on cancer therapeutics and the exploration of cell cycle regulation. -
c-Myc Inducer
DMBA (7,12-Dimethylbenz(a)anthracene) is a potent c-Myc inducer known for its role as a carcinogen due to its polycyclic aromatic hydrocarbon structure. This compound is widely utilized in experimental research to induce tumor formation in rodent models, enabling the study of cancer biology, tumorigenesis, and potential therapeutic interventions. Its application is critical in understanding the mechanisms of cancer development and the role of oncogenes. -
c-Myc Inhibitor
WBC100 is a selective c-Myc inhibitor that functions as a molecular glue degrader targeting the ubiquitin E3 ligase CHIP to promote degradation via the 26S proteasome pathway. This compound demonstrates potent activity in models of c-Myc overexpressing tumors, enabling researchers to study its effects on tumor growth and progression. WBC100 is a valuable tool for investigating the role of c-Myc in various cancer types and for exploring potential therapeutic strategies. -
CDK9 PROTAC Degrader
KI-CDK9d-32 is a selective and potent degrader designed to target CDK9 through a PROTAC mechanism (DC50: 0.89 nM). It facilitates the ubiquitination and subsequent degradation of CDK9, effectively inhibiting the MYC signaling pathway and disrupting nucleolar homeostasis. This compound demonstrates significant anticancer activity, particularly against acute lymphoblastic leukemia and pancreatic cancer, making it a valuable tool for research in cancer biology and therapeutic development. -
CDK9 Inhibitor
YK-2168 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 5.9 nM. By inhibiting the phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain, YK-2168 effectively induces apoptosis in tumor cells and suppresses the expression of CDK9-regulated genes, including MYC and Mcl1. This reagent is valuable for research applications in cancer biology, particularly in the study of leukemia and tumor growth inhibition in CDX mouse models. -
c-MYC Inhibitor
MY05 is a selective inhibitor of the c-MYC protein, effectively disrupting the MYC-MAX interaction. This compound engages intracellular c-MYC, modulating its thermal stability and leading to a reduction in c-MYC transcriptional targets. MY05 demonstrates significant anticancer activity, particularly in triple-negative breast cancer (TNBC), making it a valuable tool for research in cancer biology and therapeutics. -
c-Myc Inhibitor
c-Myc inhibitor 6 is a selective c-Myc inhibitor that effectively reduces cancer cell viability while promoting the degradation of the c-Myc protein. This compound is invaluable for research into c-Myc dysregulation, which is implicated in various pathologies, including cancer, cardiovascular diseases, and viral infections. Its ability to target c-Myc positions it as a potential therapeutic agent in studies aimed at understanding and treating these conditions. -
c-Myc Inhibitor
c-Myc ligand 1 is a potent c-Myc inhibitor that functions as a target protein ligand for PROTAC (Proteolysis Targeting Chimera) technology. This compound is essential for the synthesis of the PROTAC c-Myc inhibitor 7, facilitating studies in cellular regulation and tumorigenesis. It serves as a critical tool in research focused on targeting and degrading oncogenic proteins associated with various cancers. -
c-MYC IRES inhibitor
IRES-C11 is an inhibitor of the c-MYC internal ribosome entry site (IRES) that specifically disrupts the interaction between the c-MYC IRES and its essential trans-acting factor, heterogeneous nuclear ribonucleoprotein A1. This selective inhibition allows for targeted modulation of c-MYC translation without affecting other IRES-mediated translations, such as those involving BAG-1, XIAP, and p53. IRES-C11 is a valuable tool for research investigating the regulatory mechanisms of c-MYC translation and its implications in cancer biology. -
c-Myc Inhibitor
10074-A4 is a potent inhibitor of the c-Myc oncogenic transcription factor. It binds to the c-Myc peptide at various sites along its sequence, interfering with its function and modulating gene expression. This compound exhibits significant anticancer activity, making it a valuable tool for research into c-Myc-related pathways and cancer therapeutics. -
c-Myc Inhibitor
Lusianthridin is a c-Myc inhibitor derived from Dendrobium venustum. This compound has demonstrated significant anti-migratory effects by enhancing c-Myc degradation, primarily through the inhibition of the Src-STAT3 signaling pathway. Lusianthridin is valuable for research applications focused on cancer biology and the regulation of gene expression associated with cell migration and proliferation. -
c-Myc Inhibitor
m-Se3 is a potent and selective inhibitor of the c-Myc transcription factor. By disrupting c-Myc activity, m-Se3 effectively inhibits tumor growth and demonstrates significant anti-cancer activity across various cancer models. This compound is useful for research related to cancer biology and therapeutic strategies targeting c-Myc-driven malignancies. -
c-Myc Inhibitor
APTO-253 hydrochloride is a small molecule c-Myc inhibitor that stabilizes G-quadruplex DNA, leading to cell cycle arrest and apoptosis in acute myeloid leukemia cells. This compound exerts its anticancer effects through the induction of the tumor suppressor Kruppel-like factor 4 (KLF4). Additionally, APTO-253 hydrochloride has demonstrated antiarthritic activity, contributing to its potential application in various cancer and inflammatory disease research studies. -
c-Myc Inhibitor
c-Myc inhibitor 14 (Compound 13A) is a selective inhibitor of the c-Myc protein, demonstrating an IC50 value of less than 100 nM in HL60 cell lines. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to target c-Myc positions it as a promising candidate for studies focused on tumorigenesis and therapeutic interventions in c-Myc-driven malignancies. -
c-Myc Inhibitor
c-Myc inhibitor 10 is a selective inhibitor targeting the c-Myc protein. This compound demonstrates enhanced cellular potency, attributed to improved permeability achieved through the methylation of the morpholine nitrogen. It is useful for research applications investigating the role of c-Myc in oncogenesis and related signaling pathways. -
CDK9 Inhibitor
KI-ARv-03 is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC₅₀ of 0.15 μM in the presence of 45 μM ATP, with over 130-fold selectivity for CDK9 relative to other CDKs. This compound effectively reduces androgen receptor (AR)-driven transcription and cellular proliferation in prostate cancer models. KI-ARv-03 is applicable in the study of various malignancies, including leukemia, pancreatic cancer, alveolar rhabdomyosarcoma, and castration-resistant prostate cancer. Additionally, it serves as a ligand for PROTAC synthesis, specifically for generating PROTAC KI-CDK9d-32. -
c-Myc Inhibitor
c-Myc inhibitor 8 is a potent inhibitor of the c-Myc transcription factor, a key regulator of cell proliferation and growth in various cancers. This compound effectively reduces cell viability in a range of cancer cell lines and shows significant inhibition of human prostate and lung cancer growth in mouse models. c-Myc inhibitor 8 is suitable for applications in cancer research, particularly in studies exploring therapeutic strategies targeting c-Myc-driven tumors. -
c-Myc Inhibitor
c-Myc inhibitor 12 is a selective inhibitor targeting the transcription factor c-Myc, exhibiting a pEC50 of 6.4. This compound demonstrates significant anti-cancer activity by disrupting c-Myc-mediated transcriptional regulation. It serves as a valuable research tool for investigating the role of c-Myc in cellular proliferation and tumorigenesis, enabling studies on potential therapeutic strategies in oncology. -
c-Myc Inhibitor
c-Myc inhibitor 9 is a selective inhibitor of c-Myc, exhibiting an logEC50 of ≥6. This compound has demonstrated the ability to inhibit tumor growth in nude mouse models, making it a valuable tool in cancer research. c-Myc inhibitor 9 provides researchers with a means to explore the role of c-Myc in tumor proliferation and therapeutic strategies targeting this oncogenic transcription factor. -
c-Myc Inhibitor
c-Myc inhibitor 4 is a potent inhibitor targeting the c-Myc oncogene. This compound effectively reduces c-Myc levels, making it a valuable tool in cancer research, particularly for studies focused on tumors driven by c-Myc overexpression. Its oral bioavailability facilitates in vivo research, allowing for the exploration of therapeutic implications in various malignancies. -
c-MYC Inhibitor
NUCC-0201642 is a selective c-MYC inhibitor, demonstrating an IC50 value greater than 40 μM. This compound is utilized in cancer research to explore the role of c-MYC in tumorigenesis and to investigate potential therapeutic strategies targeting c-MYC-driven malignancies. Its application may aid in the development of novel treatments for cancers characterized by elevated c-MYC expression. -
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. -
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. -
Nur77 Binder
4-PQBH is a potent binder of Nur77, exhibiting a dissociation constant (KD) of 1.17 μM. This compound significantly induces caspase-independent cytoplasmic vacuolization and paraptosis through the mediation of endoplasmic reticulum (ER) stress and autophagy pathways. 4-PQBH serves as a valuable tool for cancer research, particularly in the study of cell death mechanisms and neurodegenerative disorders. -
CDK7 Inhibitor
LDC4297 hydrochloride is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), exhibiting an IC50 of 0.13 nM. This compound effectively inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM and demonstrates broad antiviral activity against multiple families of viruses, including Herpesviridae, Adenoviridae, Poxviridae, Retroviridae, and Orthomyxoviridae, with EC50 values ranging from 0.02 to 1.21 μM. LDC4297 hydrochloride is valuable for research into viral infections and the underlying mechanisms of CDK7 in cellular pathways. -
CDK9 Inhibitor
CDK9-IN-30 is a selective inhibitor of Cyclin-dependent kinase 9 (CDK9), primarily targeting its role in transcription regulation. This compound exhibits potent antiviral activity by disrupting HIV-1 replication, making it a valuable tool for studying HIV-1 pathogenesis and exploring therapeutic strategies. Its inhibition of CDK9 can also provide insights into broader cellular processes related to transcriptional regulation and oncogenesis. -
KRAS Inhibitor
KRAS-IN-56 is a selective KRAS inhibitor that targets the interaction between GTP-bound KRAS and SOS1, demonstrating an EC50 of 33 μM. This compound effectively reduces phosphorylated ERK (p-ERK) levels, making it a valuable tool for studying MAPK signaling pathways. KRAS-IN-56 is particularly relevant for research applications involving lung cancer and other KRAS-driven malignancies. -
PLK2 Inhibitor
Y207–5465 is a potent and highly selective inhibitor of Polo-like kinase 2 (PLK2), exhibiting an IC50 value of 584.3 nM. This compound demonstrates limited anti-cancer activity in human colorectal cancer cell lines HT-29 and HCT-116. It is suitable for use in cancer research, providing insights into the role of PLK2 in tumorigenesis and therapeutic resistance. -
PLK4 Inhibitor
Ocifisertib fumarate is a potent and selective inhibitor of Polo-like kinase 4 (PLK4), exhibiting a Ki value of 0.26 nM and an IC50 of 2.8 nM. This compound demonstrates significant biological activity in the modulation of cell cycle progression and centrosome duplication. Ocifisertib fumarate is primarily utilized in research focused on cancer biology, particularly in studies assessing the role of PLK4 in tumorigenesis and potential therapeutic interventions targeting this kinase. -
PLK1 Inhibitor
Plogosertib is a selective and potent ATP-competitive inhibitor of the polo-like kinase 1 (PLK1) with an IC50 of 3 nM. This compound exhibits significant anti-proliferative activity, making it a valuable agent in cancer research. Plogosertib is applicable in studies involving various malignancies, including esophageal, gastric, leukemia, non-small cell lung cancer, ovarian, and squamous cell cancers. -
PLK4 Inhibitor
RP-1664 is a selective and orally active inhibitor of Polo-like kinase 4 (PLK4) with an IC50 of 3 nM. This compound exhibits remarkable selectivity toward PLK4 compared to related kinases such as AURKA, AURKB, and PLK1. RP-1664 disrupts centriole biogenesis in cancer cells, resulting in the accumulation of PLK4 and p21 proteins. Its anti-tumor activity has been demonstrated in models of breast cancer and neuroblastoma, particularly in TRIM37-high-expressing cellular contexts. -
PLK4 Inhibitor
PLK4-IN-4 is a potent inhibitor of polo-like kinase 4 (PLK4), demonstrating an IC50 value of 7.9 nM. This compound effectively disrupts PLK4 activity, a critical regulator of centriole duplication, making it a valuable tool for cancer research. PLK4-IN-4 is suitable for studies investigating the role of PLK4 in tumorigenesis and may aid in the development of targeted cancer therapies. -
PROTAC PLK4 Degrader
SP27 is a PROTAC that selectively degrades Polo-like kinase 4 (PLK4), exhibiting a DC50 of 19.5 nM. This compound is valuable for investigating the role of PLK4 in cellular processes and is particularly relevant in breast cancer research, enabling studies on potential therapeutic applications and mechanisms of action related to oncogenesis. -
PLK4 Inhibitor
PLK4-IN-1 is a selective inhibitor of PLK4, exhibiting an IC50 of less than or equal to 0.1 μM. This compound plays a critical role in cell cycle regulation through the inhibition of polo-like kinase 4 activity. Its application is significant in research focusing on cell proliferation, cancer therapeutics, and understanding mitotic processes. -
PLK1 Inhibitor
Cyclapolin 9 is a selective ATP-competitive inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 500 nM. This compound demonstrates potent inhibition specifically against PLK1, making it a valuable tool for studying cell cycle regulation and cancer biology. Its selectivity and efficacy support research applications focused on tumorigenesis and targeted cancer therapies. -
PLK1 Inhibitor
Dihydrobaicalein is a selective PLK1 inhibitor, exhibiting an IC50 of 6.3 μM. This compound also demonstrates inhibitory activity against VRK2 and PLK2, making it a valuable tool in cancer research. Derived from the natural source Scutellaria scandens, dihydrobaicalein is utilized in studies exploring cell cycle regulation and mitotic processes. Its ability to modulate specific kinases positions it as a significant candidate for further investigation in therapeutic applications. -
PLK1 Inhibitor
PLK1-IN-11 is a selective inhibitor of Polo-like kinase 1 (PLK1), exhibiting an IC50 of 1 μM. This compound demonstrates significant potential for modulating cell proliferation and mitotic progression. PLK1-IN-11 is suitable for investigation in various cancer models, including pancreatic, ovarian, breast, and non-small cell lung carcinoma, contributing to the understanding of cancer biology and the development of targeted therapies. -
Plk Inhibitor
BTO-1 is a selective inhibitor of Polo-like kinase (Plk), a key regulator of the cell cycle. This compound is designed to interfere with Plk activity, impacting downstream phosphorylation and dephosphorylation processes. BTO-1 is utilized in research focused on cell cycle regulation, cancer biology, and the development of novel therapeutic strategies targeting Plk pathways. -
PLK1 PROTAC Degrader
PROTAC PLK1 Degrader-3 is a PLK1-targeted PROTAC that facilitates the degradation of the Polo-like kinase 1 (PLK1) protein through the N-deglycosylation pathway, exhibiting a dissociation constant (Kd) of 2.2 μM. This compound is primarily utilized in research related to non-small cell lung cancer, enabling investigations into targeted protein degradation mechanisms. While the compound shows limited cell penetration, higher concentrations may be necessary to achieve effective degradation outcomes, making it suitable for various biological studies in oncological contexts. -
Polo-like Kinase (PLK) Inhibitor
DAP-81 is a potent inhibitor of Polo-like kinases (PLKs), a group of essential serine/threonine kinases involved in cell cycle regulation. This compound has been shown to dose-dependently increase the formation of monopolar spindles in treated cells, indicating its role in disrupting normal mitotic spindle assembly. High-resolution live-cell microscopy studies demonstrate that PLK activity is crucial for the integrity of bipolar mitotic spindles. By inhibiting PLK activity, DAP-81 destabilizes centromeric microtubules while enhancing the stability of other spindle microtubules, making it a valuable tool for researchers investigating cell division and potential anti-microtubule agents. -
Polo-like Kinase (PLK)
CAP-53194 is a selective inhibitor of Polo-like Kinase 1 (PLK1) with promising anticancer properties. It demonstrates significant selectivity, showing over 100-fold inhibition of PLK1 compared to PLK2-4 and other cell cycle-related kinases due to its ability to target unique features within the PLK1 binding site. CAP-53194 conforms to Lipinski's rule of five and meets various ADMET criteria, suggesting favorable pharmacokinetic characteristics. This compound represents a novel class of potential PLK1 inhibitors for further research and development in cancer therapeutics. -
PLK1/PRC1 Inhibitor
PLK1/PRC1-IN-1 is an inhibitor of the PLK1/PRC1 protein complex formation. This compound specifically targets the interaction between polo-like kinase 1 (PLK1) and protein-regulator of cytokinesis 1 (PRC1), disrupting their function. PLK1/PRC1-IN-1 is primarily utilized in research focused on non-small cell lung cancer (NSCLC) and provides insights into the mechanisms of cell division and tumor growth. -
PLK4 Inhibitor
CFI-400437 is an indolinone-derived, ATP-competitive inhibitor specifically targeting PLK4, exhibiting exceptional selectivity with an IC50 of 0.6 nM. This compound demonstrates potent inhibitory activity, making it a valuable tool for studying the role of PLK4 in cell cycle regulation and genomic stability. It is particularly useful in cancer research, where PLK4 dysregulation has been implicated in tumorigenesis. -
PLK4 Inhibitor
PLK4-IN-3 is a selective inhibitor targeting Polo-like kinase 4 (PLK4), exhibiting an IC50 value of 0.65 μM. This compound plays a critical role in disrupting cell division by modulating the function of PLK4, which is essential for cytokinesis and centriole biogenesis. PLK4-IN-3 is valuable in cancer research, particularly in studies investigating the proliferation and survival of cancer cells with dysregulated PLK4 activity. -
PLK1 Inhibitor
PLK1-IN-5 is a selective inhibitor of Polo-like Kinase 1 (PLK1), with an IC50 of less than 500 nM. This compound demonstrates significant anticancer activity, making it a valuable tool for researchers studying cancer biology and therapeutic interventions. Its ability to effectively inhibit PLK1 offers potential applications in the development of novel cancer treatments. -
PLK1 Inhibitor
PLK1-IN-4 is a highly selective and potent inhibitor of Polo-like kinase 1 (PLK1), exhibiting an IC50 of less than 0.508 nM. It demonstrates significant antiproliferative effects across a range of cancer cell lines and induces mitotic arrest at the G2/M checkpoint, thereby promoting apoptotic pathways in cancer cells. This compound is valuable for investigations into hepatocellular carcinoma and other malignancies where PLK1 plays a critical role in cell cycle regulation. -
PLK Inhibitor
PLK1-IN-2 is a potent inhibitor of the polo-like kinase 1 (PLK1), exhibiting an IC50 value of 0.384 μM. This compound disrupts PLK1 activity, which is crucial for regulating cell division and cancer cell proliferation. It is primarily utilized in cancer research to investigate the role of PLK1 in tumorigenesis and to assess its potential as a therapeutic target. -
PLK1 Ligand
POI ligand-4 is a selective ligand for Polo-like kinase 1 (PLK1), serving as a crucial building block in the development of PROTACs. This compound facilitates targeted degradation of PLK1, exemplified in the synthesis of PROTAC PLK1 Degrader-3. It is instrumental in advancing research on cancer therapies and PLK1-related pathways. -
PLK1 Inhibitor
PLK1-IN-10 is a potent inhibitor of the polo-like kinase 1 (PLK1) polo-box domain. This compound disrupts the interaction between PLK1 and the cell division regulator protein PRC1, leading to a reduction in the expression of the CDK1-Cyclin B1 complex. Additionally, PLK1-IN-10 interacts with glutathione (GSH), increasing cellular oxidative stress and promoting apoptosis. Its applications include cancer research and studies on cell cycle regulation.
