Catalog No.
Product Name
Application
Product Information
Citations
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Chk Inhibitor
XL-844 is an inhibitor of checkpoint kinases Chk1 and Chk2, leading to the induction of apoptosis in tumor cells by disrupting cell cycle arrest. Additionally, XL-844 demonstrates inhibitory effects on vascular endothelial growth factor receptors VEGFR1 and VEGFR3. This compound is primarily applied in anti-cancer research to explore its potential in enhancing therapeutic efficacy against various malignancies. -
Chk1 Inhibitor
CHK1-IN-8 is a selective Chk1 inhibitor with an IC50 value of less than 10 nM for human Chk1. This compound is valuable for investigating the role of Chk1 in cell cycle regulation and DNA damage response mechanisms in cancer research. Its potent inhibition of Chk1 makes it a useful tool for exploring therapeutic strategies in cancer treatment. -
Chk2 Inhibitor
PV1162 is a selective Chk2 inhibitor that functions by preventing ATP binding to Chk2, specifically targeting the gatekeeper-dependent hydrophobic pocket situated behind the ATP-binding site. With an IC50 of 0.29 nM, PV1162 effectively inhibits the phosphorylation activity of Chk2. This compound demonstrates significant potential for research applications in cancer therapy, particularly in the study of checkpoint regulation and tumor progression. -
Checkpoint Kinase (Chk) Inhibitor
CHK-IN-1 is a selective inhibitor of checkpoint kinases CHK1 and CHK2, which play crucial roles in the DNA damage response and cell cycle regulation. This compound exhibits anti-proliferative activity, making it a valuable tool for cancer research and therapeutic studies targeting tumor cell growth and survival. Its ability to regulate cellular checkpoint pathways provides a basis for exploring its efficacy in combination therapies and enhancing the understanding of cancer cell biology. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-3 is a selective dual inhibitor targeting bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). This compound effectively inhibits BRD4-BD1, PLK1, and BRDT-BD1, exhibiting IC50 values of 0.059 µM, 0.127 µM, and 0.245 µM, respectively. PLK1/BRD4-IN-3 can be employed in research applications focused on cancer biology, particularly in studies investigating cell proliferation and transcriptional regulation. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-2 is a dual inhibitor targeting both Polo-like kinase 1 (PLK1) and the bromodomain of BRD4, with an IC50 of 40 nM and 28 nM, respectively. This compound is valuable for research into cancer therapeutics and epigenetic regulation, demonstrating potential in studies focused on cell proliferation and transcriptional control. Its ability to simultaneously inhibit these key oncogenic pathways positions PLK1/BRD4-IN-2 as a crucial tool for advancing cancer research and drug discovery initiatives. -
CDK/GSK3β/JNK Inhibitor
Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation. -
RAS/RAS-RAF Inhibitor
RAS/RAS-RAF-IN-1 is a potent inhibitor targeting the RAS and RAS-RAF signaling pathways. With a dissociation constant (KD) in the range of 5.0 μM to 15 μM for cyclophilin A (CYPA), this compound demonstrates significant binding affinity. RAS/RAS-RAF-IN-1 exhibits notable antitumor activity, making it a valuable tool for cancer research and therapeutic development. -
Ras-Raf Inhibitor
Cyclorasin 9A5 is an 11-residue cyclic peptide that acts as an orthosteric inhibitor of the Ras-Raf protein interaction, exhibiting an IC50 of 120 nM. This compound is valuable for studying the Ras signaling pathway's involvement in various cancers and cellular processes. Its cell-permeable nature allows for effective in vitro and in vivo applications in cancer research and drug development targeting Ras-dependent pathways. -
pan-KRAS PROTAC Degrader
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment. -
KRAS-PDEδ Inhibitor
NHTD is a selective inhibitor of KRAS-PDEδ, targeting the prenyl-binding pocket of PDEδ and modulating the cellular localization of KRAS. This action effectively inhibits the proliferation of KRAS-mutant cancer cells and promotes apoptosis. NHTD is a valuable tool for investigations into KRAS-driven non-small cell lung cancer (NSCLC) and related oncology research. -
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. -
CDK2/GSK3β Inhibitor
Tagtociclib hydrate is a potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2) and glycogen synthase kinase 3 beta (GSK3β), displaying inhibition constants of 1.16 nM and 537.81 nM, respectively. This compound demonstrates significant anti-tumor activity, particularly in cancers characterized by cyclin E1 amplification. Tagtociclib hydrate serves as a valuable research tool for studying cell cycle regulation and therapeutic strategies targeting kinase pathways in cancer biology. -
PLK2 Inhibitor
8012-3246 is a selective inhibitor of Polo-like kinase 2 (PLK2) with an IC50 of 774.5 nM. This compound effectively suppresses the phosphorylation of GSK3β, demonstrating its potential role in cellular signaling modulation. Additionally, 8012-3246 exhibits significant anticancer activity, particularly against colorectal cancer, making it a valuable tool for cancer research applications focusing on PLK2-related pathways. -
Cyclin D1 Inhibitor
DIF-3 is a potent cyclin D1 inhibitor that promotes the degradation of cyclin D1 and c-Myc by activating GSK-3β. This compound suppresses Wnt/β-catenin signaling pathway-associated proteins, leading to the induction of reactive oxygen species (ROS) and autophagy. Additionally, DIF-3 has demonstrated the ability to inhibit the growth of Trypanosoma cruzi in HT1080 cells, showcasing its antitumor properties in both in vitro and in vivo settings. Its multifaceted mechanism positions DIF-3 as a valuable tool for cancer research and cellular biology studies. -
CDKL5/GSK3 Inhibitor
SGC-CDKL5/GSK3 is a selective inhibitor targeting CDKL5 and GSK3α/β. This compound demonstrates potent inhibition, with IC50 values of 4.6 nM for CDKL5, 24 nM for GSK3β, and 9.5 nM for GSK3α, as assessed by the NanoBRET assay. Its specificity and efficacy make it a valuable tool for investigating central nervous system diseases and related biological pathways. -
GSK3/CDK9 Inhibitor
ABC1183 is a selective dual inhibitor targeting GSK3 and CDK9, effectively inhibiting GSK3β, GSK3α, and CDK9/cyclin T1 with IC50 values of 657 nM, 327 nM, and 321 nM, respectively. This compound exhibits notable anti-inflammatory and anti-tumor activities, making it a valuable tool for cancer research and inflammation-related studies. Its ability to modulate critical signaling pathways positions ABC1183 as a promising candidate for further investigation in therapeutic applications. -
GSK-3/CDK5/CDK2 Inhibitor
GSK-3/CDK5/CDK2-IN-1 is a potent inhibitor targeting GSK-3, CDK5, and CDK2. This imidazole derivative has demonstrated effectiveness in modulating pathways relevant to tumorigenesis and neurodegenerative disorders. Its ability to inhibit these kinases makes it a valuable tool for investigating mechanisms underlying cancer proliferation and neurodegeneration. -
GSK-3/CDK2/CDK5 Inhibitor
GSK-3 Inhibitor 4 is a potent inhibitor of Glycogen Synthase Kinase 3 (GSK-3), Cyclin-Dependent Kinase 2 (CDK2), and Cyclin-Dependent Kinase 5 (CDK5), demonstrating IC50 values of 0.56 nM for GSK-3β, 0.45 nM for GSK-3α, 0.47 μM for CDK2, and 0.68 μM for CDK5. This compound effectively attenuates the phosphorylation of Tau protein, making it a valuable tool for investigating mechanisms underlying Alzheimer's disease. Its oral bioavailability and ability to penetrate the blood-brain barrier further enhance its utility in neuropharmacological research. -
CDK8 Inhibitor
CDK8-IN-12 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting a potent Ki value of 14 nM. This compound also demonstrates off-target activity against GSK-3α, GSK-3β, and PCK-θ with Ki values of 13 nM, 4 nM, and 109 nM, respectively. CDK8-IN-12 has been shown to exert significant anti-proliferative effects on MV4-11 cancer cells, making it a valuable tool for research in oncology and the exploration of CDK8-related pathways in cancer progression. -
CDK/GSK-3 Inhibitor
CDK5-IN-4 is a potent multikinase type-II inhibitor primarily targeting cyclin-dependent kinase 5 (CDK5), with an IC50 of 9.8 μM. Additionally, it exhibits inhibitory activity against GSK-3α and GSK-3β with IC50 values of 0.98 μM and 4.00 μM, as well as CDK9 and CDK2, with IC50 values of 1.76 μM and 6.24 μM, respectively. This compound is particularly relevant for research on glioblastoma and may aid in understanding its molecular mechanisms. -
CDK7 Inhibitor
CDK7-IN-20 is a highly potent and selective irreversible inhibitor of cyclin-dependent kinase 7 (CDK7), exhibiting an IC50 value of 4 nM. Demonstrating over 206-fold selectivity for CDK7 compared to CDK1, CDK2, CDK3, CDK5, CDK6, CDK9, and CDK12, CDK7-IN-20 is a valuable tool for studying the role of CDK7 in cellular processes. Its potential applications extend to researching autosomal dominant polycystic kidney disease (ADPKD) and other related pathologies. -
CDK/GSK3 Inhibitor
Aloisine RP106 is a potent inhibitor of cyclin-dependent kinases (CDKs) Cdk1/cyclin B and Cdk5/p25, as well as glycogen synthase kinase 3 (GSK3), with IC50 values of 0.70 µM, 1.5 µM, and 0.92 µM, respectively. This compound is valuable for research applications targeting cell cycle regulation and neurodegenerative diseases, where CDK and GSK3 activity contribute to pathological processes. Researchers can utilize Aloisine RP106 to investigate the role of these kinases in various biological contexts including cancer and neurobiology. -
GSK-3β/CDK-2/CDK-4 Inhibitor
UNC10112785 is a potent inhibitor of serine/threonine kinases, specifically targeting GSK-3β, CDK-2, and CDK-4 with IC50 values of 0.031 μM, 0.016 μM, and 1.99 μM, respectively. This compound exhibits significant biological activity that positions it as a valuable tool in the study of type 2 diabetes. Its ability to modulate key pathways involved in metabolic regulation makes it an essential reagent for researchers investigating therapeutic interventions in diabetic conditions. -
CDK4/6 Inhibitor
Palbociclib hydrochloride is a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6, with IC50 values of 11 nM and 16 nM, respectively. This compound demonstrates significant anti-proliferative activity, effectively inducing cell cycle arrest in malignant cells. Palbociclib hydrochloride is utilized in research focused on HR-positive and HER2-negative breast cancer as well as hepatocellular carcinoma, making it a valuable tool for understanding tumor biology and therapeutic responses. -
CDK7 Inhibitor
YKL-5-124 is a selective and irreversible inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound exhibits over 100-fold selectivity for CDK7 compared to CDK9 and CDK2 and has negligible activity against CDK12 and CDK13. YKL-5-124 effectively induces cell-cycle arrest, inhibits E2F-driven transcription, and has a limited impact on the phosphorylation status of RNA polymerase II, making it a valuable tool for research in cell cycle regulation and transcriptional control. -
CDK Inhibitor
Romaciclib monohydrochloride is a selective CDK inhibitor that targets CDK8 and CDK19. This compound exhibits potent inhibition of CDK8/CycC and CDK19/CycC kinase activities with IC50 values of 4.4 nM and 10.4 nM, respectively. Additionally, it weakly inhibits CDK9 with an IC50 of 1070 nM, while having no significant activity against other CDK isoforms. Romaciclib monohydrochloride is known to inhibit the phosphorylation of STAT1 at S727 and STAT5 at S726, demonstrating potential anti-tumor activity valuable for cancer research applications.
