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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
CDK9 Inhibitor
KB-0742 dihydrochloride is a selective and orally bioactive inhibitor of CDK9, exhibiting an IC50 of 6 nM for the CDK9/cyclin T1 complex. This compound demonstrates over 50-fold selectivity for CDK9 compared to other CDK kinases, making it a valuable tool for precision research. KB-0742 dihydrochloride possesses strong anti-tumor activity, facilitating investigations into its efficacy in cancer biology and therapeutic applications. -
CDK4/6 Inhibitor
Dalpiciclib is a highly selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), demonstrating IC50 values of 12.4 nM and 9.9 nM, respectively. This orally active compound exhibits significant antitumor activity, particularly in breast cancer and esophageal squamous cell carcinoma. Dalpiciclib is utilized in research applications focused on tumor suppression and cell cycle regulation. -
WEE1 Inhibitor
Zedoresertib, a potent WEE1 inhibitor, exhibits an IC50 value of 0.8 nM and effectively inhibits phospho-CDC2. By abrogating the G2 checkpoint, Zedoresertib enhances the sensitivity of cancer cells to DNA-damaging agents, making it a valuable tool for anticancer research. This compound is essential for studies investigating cell cycle regulation and therapeutic strategies in oncology. -
CDK9 Inhibitor
KB-0742 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 6 nM for the CDK9/cyclin T1 complex. With over 50-fold selectivity against other CDK kinases, KB-0742 demonstrates significant anti-tumor activity. This compound is particularly valuable for research involving transcriptional regulation, cancer biology, and therapeutic strategies targeting CDK9-associated pathways. -
CDK4/6 Inhibitor
Dalpiciclib hydrochloride is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), with IC50 values of 12.4 nM and 9.9 nM, respectively. This compound exhibits significant antitumor activity, particularly in the context of breast cancer and esophageal squamous cell carcinoma. Dalpiciclib hydrochloride is valuable for research focused on cell cycle regulation and cancer therapeutics. -
PTEFb/CDK9 Inhibitor
Atuveciclib is a highly selective oral inhibitor of PTEFb/CDK9, demonstrating potent activity with an IC50 of 13 nM against the CDK9/CycT1 complex. This compound effectively disrupts transcriptional regulation, making it a valuable tool in cancer research and studies related to transcriptional control. Atuveciclib may be employed in investigations aimed at understanding the roles of CDK9 in various diseases, including cancer and other pathologies linked to aberrant transcriptional activity. -
CDK5 Inhibitor
GFB-12811 is a highly selective inhibitor of cyclin-dependent kinase 5 (CDK5) with an IC50 of 2.3 nM. Its potent action allows for effective modulation of CDK5 activity, making it a valuable tool for studying neurodegenerative diseases and related signaling pathways. This compound is suitable for research investigating the role of CDK5 in neuronal function and pathology. -
CDK4/6 Inhibitor
Abemaciclib metabolite M20 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). This compound exhibits potent anti-proliferative activity in various cancer cell lines, contributing to its potential use in cancer therapy. Research applications include studying cell cycle regulation and exploring therapeutic strategies for tumors driven by CDK4/6 activity. -
CDK2/5 Inhibitor
CDK5 inhibitor 20-223 is a potent inhibitor of cyclin-dependent kinases 2 and 5, exhibiting IC50 values of 6.0 nM and 8.8 nM, respectively. This compound demonstrates significant anti-colorectal cancer activity, making it a valuable tool for research in cancer biology and therapeutic development. Its selective inhibition of CDK2 and CDK5 provides insights into their roles in cell cycle regulation and oncogenesis. -
CDK4/6 Inhibitor
Abemaciclib metabolite M18 hydrochloride functions as a CDK4/6 inhibitor, exhibiting significant antitumor activity. This compound has been utilized in the design of PROTAC (Proteolysis Targeting Chimera) CDK4/6 degraders in conjunction with a CRBN ligand. Its role in targeted protein degradation research makes it a valuable tool for investigating cell cycle regulation and cancer therapeutics. -
CDK12 Inhibitor
CDK12-IN-2 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a nanomolar potency with an IC50 value of 52 nM. This compound also demonstrates inhibitory activity against CDK13, its closest homologue, but maintains strong selectivity for CDK12 over other kinases such as CDK2, CDK7, CDK8, and CDK9. CDK12-IN-2 effectively inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II, making it a valuable chemical probe for functional studies in cancer biology and transcription regulation. -
CDK5 Inhibitor
CDK5-IN-3 is a highly selective inhibitor of CDK5, demonstrating IC50 values of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. This compound is valuable for investigations into the role of CDK5 in cellular processes and is particularly relevant for research focused on autosomal dominant polycystic kidney disease (ADPKD). Its potency and specificity make CDK5-IN-3 an essential tool for elucidating the molecular mechanisms underlying CDK5-related pathologies. -
CDK2 Inhibitor
GW8510 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) that also targets ribonucleotide reductase M2 (RRM2). This compound demonstrates significant neuroprotective effects and possesses anticancer properties. It is utilized in scientific research to explore mechanisms of cell proliferation and apoptosis in various cancer models, making it a valuable tool for studying the role of CDK2 in cancer and neurodegenerative diseases. -
CDK Inhibitor
DS96432529 is a potent CDK8 inhibitor that exhibits bone anabolic properties. This compound selectively inhibits cyclin-dependent kinase 8, leading to enhanced bone formation and potential therapeutic applications in osteoporosis and other bone-related disorders. Its oral bioavailability makes it a valuable tool for in vivo studies focusing on bone metabolism and development. -
CDK2 Inhibitor
CDK2-IN-23 is a highly potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.29 nM. This compound demonstrates significant pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models, making it a valuable tool in cancer research. Its selectivity and potency provide a promising avenue for studying CDK2's role in tumorigenesis and evaluating therapeutic strategies in oncology. -
CDK9 Inhibitor
CDK9 inhibitor HH1 selectively targets cyclin-dependent kinase 9 (CDK9), a key regulator of transcriptional control. This compound effectively inhibits CDK9 activity, leading to decreased transcription of oncogenes associated with cancer progression. HH1 serves as a valuable reagent for investigating therapeutic strategies in cancer research and studying the role of CDK9 in gene expression regulation. -
CDK Inhibitor
JH-XVI-178 is a potent and selective inhibitor targeting cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 1 nM and 2 nM, respectively. This compound exhibits low clearance rates and moderate oral pharmacokinetic characteristics, making it suitable for in vivo studies. JH-XVI-178 is valuable for research in transcriptional regulation and cancer biology, particularly in contexts where CDK8 and CDK19 play critical roles in oncogenic signaling pathways.
