Catalog No.
Product Name
Application
Product Information
Citations
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CDK7 Inhibitor
SZ-015268 is a potent CDK7 inhibitor, exhibiting an IC50 of 23.56 nM. This compound demonstrates significant anti-tumor activity, effectively inhibiting the proliferation of various cancer cell lines, including HCC70 (IC50 33 nM), OVCAR-3 (IC50 80.56 nM), HCT116 (IC50 12.53 nM), and HCC1806 (IC50 61.55 nM). SZ-015268 serves as a valuable tool in cancer research, particularly in studies focused on cell cycle regulation and therapeutic strategies targeting CDK7. -
CDK9 PROTAC
PROTAC CDK9 degrader-6 is a proteolysis-targeting chimera (PROTAC) designed to specifically target and degrade cyclin-dependent kinase 9 (CDK9) through the ubiquitin-proteasome system. This compound effectively induces the degradation of CDK9, exhibiting DC50 values of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively. It is useful in research applications investigating the modulation of transcriptional regulation and the therapeutic potential in cancers driven by aberrant CDK9 activity. -
CDK9 Inhibitor
PROTAC CDK9/CycT1 Degrader-2 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 45 nM. This compound promotes targeted protein degradation, thereby modulating transcriptional regulation and influencing cellular processes associated with gene expression. It is valuable for research applications focused on cancer biology and therapeutic development by addressing dysregulated CDK9 activity. -
CDK4/6 Inhibitor
CDK4/6-IN-22 is a potent dual inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). By inhibiting these kinases, CDK4/6-IN-22 effectively disrupts cell cycle progression, making it a valuable tool in cancer research. This compound is particularly relevant for studies exploring therapeutic strategies for tumors characterized by dysregulated CDK4/6 activity. -
CDK Inhibitor
Aloisine B is a potent cyclin-dependent kinase (CDK) inhibitor. It effectively inhibits cell proliferation by inducing cell cycle arrest in both the G1 and G2 phases through competition for the ATP-binding pocket. This compound serves as a valuable tool for research in cancer biology and cell cycle regulation. -
Cyclin A/B RxL Inhibitor
Cyclin A/B RxL-IN-1 is an inhibitor that targets the interaction between Cyclin A/B and the hydrophobic patch (HP). With an IC50 of 0.12 μM, it effectively inhibits Cyclin A, demonstrating notable antitumor activity in cell line-derived xenograft (CDX) models. This compound is valuable for research on E2F-driven cancers, including small-cell lung cancer (SCLC), providing insights into therapeutic strategies. -
CDK2 Inhibitor
CDK2-IN-29 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 96 nM. Additionally, it shows activity against CDK4 with an IC50 of 360 nM. This compound is instrumental in the study of cell cycle regulation and has potential applications in cancer research, where CDK inhibition plays a critical role in controlling cell proliferation. -
CDK7 Inhibitor
CDK7-IN-8 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating an IC50 of 54.29 nM. This compound effectively inhibits the proliferation of specific cancer cell lines and has shown promising activity in various in vivo tumor models. CDK7-IN-8 is utilized in research applications targeting cancer therapeutics and cell cycle regulation studies. -
CDK7 Inhibitor
CDK7-IN-15 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), a key regulator of transcription and cell cycle progression. This pyrimidinyl derivative exhibits potent inhibitory activity, making it a valuable tool for investigating transcriptional dysregulation in various cancer types. CDK7-IN-15 is particularly relevant for cancer research focused on therapeutic strategies targeting aberrant transcriptional control. -
CDK2 Inhibitor
RLY-2139 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2). By selectively targeting CDK2, it disrupts cell cycle progression, making it a valuable tool for studying cell division and proliferation. RLY-2139 has potential applications in cancer research, particularly in exploring therapeutic strategies for CDK2-related malignancies. -
CDK
rel-(2S,3R)-Voruciclib hydrochloride is the rel-(2S,3R)-enantiomer of Voruciclib, a potent inhibitor of cyclin-dependent kinases (CDKs). This compound exhibits significant biological activity in regulating cell cycle progression and has potential applications in cancer research, particularly in therapeutic strategies targeting CDK-mediated pathways. Its oral bioavailability makes it a valuable tool for in vivo studies of cell proliferation and tumor growth. -
Cyclin A/B Inhibitor
Cyclin A/B RxL-IN-2 is a macrocyclic peptide that acts as a selective inhibitor of Cyclin A and Cyclin B. It exhibits high potency with an IC50 of 0.05 μM for Cyclin A and less than 0.02 μM for Cyclin B, alongside Kd values of 2.7 nM and 1.0 nM, respectively. This compound competes for binding at the hydrophobic patch of Cyclin A/B, disrupting interactions with the substrate RxL motif, leading to replication stress and DNA damage in E2F-high cells, as well as inducing mitotic catastrophe and apoptosis. Cyclin A/B RxL-IN-2 demonstrates efficacy in inhibiting tumor growth in NCI-H69 and NCI-H446 small cell lung cancer xenograft models, making it a valuable tool for research in small-cell lung cancer. -
CDK4/6 Inhibitor
PRT3645 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). It demonstrates potent inhibition with IC50 values less than 20 nM, making it a valuable tool for studying cell cycle regulation and cancer biology. PRT3645 is primarily utilized in research applications targeting tumor cell proliferation and therapeutic strategies for cancers associated with dysregulated CDK4/6 activity. -
CDK12 Inhibitor
GW780056X is a selective inhibitor of Cyclin-Dependent Kinase 12 (CDK12). It is known to reduce nuclear foci count in DM1 cells, demonstrating its potential in therapeutic strategies for myotonic dystrophy type 1. This compound serves as a valuable tool for investigating the molecular mechanisms underlying this genetic disorder and evaluating potential treatment options. -
CDK8 Inhibitor
CDK8-IN-18 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8) with an IC50 of 43 μM. This compound is instrumental in studying the regulatory roles of CDK8 in transcription and its implications in oncogenesis. CDK8-IN-18 is widely used in cancer research to explore the therapeutic potential of targeting CDK8 in malignancies. -
CDK7/9 Inhibitor
CDK7/9-IN-1 is a potent inhibitor of cyclin-dependent kinases 7 and 9, demonstrating a selective inhibition profile that favors CDK7. This compound exhibits IC50 values of 0.0656 μM and 0.00574 μM for CDK7 without and with 3 hours of pre-incubation, respectively, while inhibiting CDK9 with an IC50 of 2.14 μM after pre-incubation. CDK7/9-IN-1 is valuable for research applications related to cancer, particularly in studies targeting the regulation of transcription and cell cycle progression mediated by these kinases. -
CDK Inhibitor
CDK12-IN-7 is a potent inhibitor of cyclin-dependent kinases CDK12 and CDK2, exhibiting IC50 values of 42 nM and 196 nM, respectively. This compound demonstrates significant anti-cell proliferation activity, making it valuable for cancer research applications. Its selective inhibition of CDK12 may provide insights into tumorigenesis and potential therapeutic strategies in oncology. -
PTEFb/CDK9 Inhibitor
BAY-958 is a potent inhibitor of PTEFb/CDK9, demonstrating high selectivity within the cyclin-dependent kinase family. This compound exhibits significant antiproliferative effects against various cancer cell lines, including HeLa and MOLM-13. Additionally, BAY-958 shows favorable metabolic stability and effectively reduces tumor growth in mouse xenograft models while maintaining a low toxicity profile, making it a valuable tool for cancer research. -
CDK7 Inhibitor
CDK7-IN-26 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 of 7.4 nM. This compound demonstrates significant efficacy in inhibiting the proliferation of triple-negative breast cancer (TNBC) cell line-derived xenograft tumors in vivo. In vitro studies show that CDK7-IN-26 effectively targets MDA-MB-453 cells, exhibiting an IC50 of 0.15 μM, making it a valuable tool for cancer research focusing on CDK7 inhibition. -
CDK12 Inhibitor
CDK12-IN-4 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a potent inhibitory effect with an IC50 of 0.641 μM at elevated ATP levels (2 mM). This compound demonstrates no significant activity against CDK2/Cyclin E or CDK9/Cyclin T1, with IC50 values exceeding 20 μM under the same conditions. CDK12-IN-4 is valuable for research into transcription regulation and therapeutic targeting in cancer biology, particularly in studies involving DNA damage and repair pathways. -
CDK Inhibitor
Ulecaciclib is an orally active inhibitor of cyclin-dependent kinases (CDKs), specifically targeting CDK2, CDK4, CDK6, and CDK7 with Ki values of 0.62 μM, 0.2 nM, 3 nM, and 0.63 μM, respectively. This compound exhibits excellent pharmacokinetic properties and is capable of crossing the blood-brain barrier. Ulecaciclib is valuable for research applications in cancer biology, particularly in the study of cell cycle regulation and CDK-related pathways in various malignancies. -
CDK12 Inhibitor
CDK12-IN-9 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12) with an IC50 of 2.2 nM. This compound effectively inhibits phosphorylated serine 2 (pSER2), a key downstream marker associated with CDK12/13 activity. CDK12-IN-9 is suitable for cancer research, offering potential insights into therapeutic strategies targeting transcriptional regulation and DNA repair mechanisms in malignant cells. -
CDK2 Inhibitor
CDK2-IN-28 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), designed to modulate cell cycle progression. This compound demonstrates significant anti-proliferative activity against MKN1 cells, with an EC50 of 0.31 μM. CDK2-IN-28 is valuable for research into mechanisms of cell cycle regulation and potential therapeutic applications in cancer. -
CDK2 Inhibitor
CDK2-IN-51 is a pyrazolopyridine derivative that selectively inhibits cyclin-dependent kinase 2 (CDK2) with an IC50 value of 23.47 nM. This compound demonstrates significant biological activity by downregulating the expression of critical DNA replication factors, including Polα, MCM7, ORC2, and ORC4, leading to pre-G1 cell cycle arrest. CDK2-IN-51 is primarily utilized in the research of colorectal cancer, providing valuable insights into cell cycle regulation and potential therapeutic strategies. -
CDK9 Degrader
PROTAC CDK9 degrader-8 is a potent degrader targeting CDK9, exhibiting an IC50 value of 0.01 μM. This compound effectively induces the degradation of CDK9, making it a valuable tool for investigating the role of CDK9 in cancer biology and therapeutic resistance. It is suitable for use in studies aimed at understanding the mechanisms of tumor progression and exploring potential treatment strategies. -
CDK12/CDK13 Inhibitor/CycK Molecular Glue Degrader
SR-5037 is an orally active inhibitor of CDK12 and CDK13, with an IC50 of 31 nM, and functions as a molecular glue degrader for CycK, demonstrating a DC50 of 30 nM and Dmax exceeding 98%. By inhibiting the enzymatic activity of the CDK12/CycK and CDK13/CycK complexes, SR-5037 facilitates the recruitment of DDB1, leading to proteasome-mediated degradation of CycK. This compound has shown efficacy in degrading active CycK in mouse models of triple-negative breast cancer and is a valuable tool for investigating treatment options in such malignancies. -
CDK7 Inhibitor
CDK7-IN-17 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), a key regulator of transcription and cell cycle progression. This pyrimidinyl derivative demonstrates potent inhibitory activity against CDK7, making it a valuable tool in cancer research, particularly in studies related to transcriptional dysregulation in various malignancies. Its application in elucidating CDK7's role in tumorigenesis may provide insights into novel therapeutic strategies for cancer treatment. -
CDK7 Inhibitor
CDK7-IN-31 is a highly potent and orally bioavailable inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating a Kd value of 0.18 nM. This compound exhibits significant anticancer activity, making it a valuable tool for cancer research and therapeutic development. Its selective inhibition of CDK7 facilitates investigations into the role of this kinase in cell cycle regulation and transcriptional control. -
CDK Inhibitor
CDK8-IN-14 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), displaying an IC50 value of 39.2 nM. This compound demonstrates significant anti-proliferative effects on acute myeloid leukemia (AML) cells, with reported GC50 values of 0.02 ± 0.01 μM for Molm-13 and 0.03 ± 0.01 μM for MV4-11. Its potency makes it a valuable tool for research into CDK8-mediated signaling pathways and potential therapeutic strategies in AML. -
CDK4/6 Inhibitor
CDK4/6-IN-8 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), displaying IC50 values of 5.01 nM and 3.97 nM for each target, respectively. This compound effectively modulates cell cycle progression, making it a valuable tool for studies related to cancer biology and therapies targeting cell proliferation. Its precise inhibition of CDK4 and CDK6 positions it for use in research on tumor cell growth and the mechanistic exploration of cell cycle dysregulation in various malignancies. -
CDK12 Inhibitor
CDK12-IN-8 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), which primarily targets the phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II. By disrupting CDK12-mediated transcription elongation and DNA damage repair mechanisms, CDK12-IN-8 has significant implications for cancer research, particularly in malignancies characterized by elevated CDK12 expression, such as small cell lung cancer and triple-negative breast cancer. It serves as a valuable tool for exploring the role of CDK12 in oncogenic processes. -
CDK Inhibitor
KM05382 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), disrupting its activity and consequently leading to reduced transcription of the GAPDH gene. This compound plays a crucial role in regulating transcriptional control and has potential applications in understanding cell cycle dynamics and cancer research. Its unique mechanism makes it valuable for studies aimed at evaluating CDK9's role in gene expression and related pathways. -
CDK Inhibitor
p27 is a cyclin-dependent kinase (CDK) inhibitor that functions as a substrate for the SCFSkp2/Cks1 complex. This protein plays a crucial role in cell cycle regulation by inhibiting CDK activity, thereby impacting cell proliferation. p27 is widely used in cancer research to investigate the mechanisms of tumorigenesis and to explore therapeutic strategies for targeting cell cycle dysregulation. -
CDK9 Inhibitor
CLZX-205 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 2.9 nM. This compound is significant in cancer research due to its ability to inhibit the phosphorylation of RNA polymerase II, thereby impacting transcriptional regulation in oncogenic pathways. CLZX-205 serves as a valuable tool for studying CDK9-related mechanisms and therapeutic strategies in cancer biology. -
CDK9 Inhibitor
CDK9-IN-23 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9) with an IC50 value of less than 20 nM. This compound demonstrates effective inhibition of transcriptional regulation and is crucial for studying cellular processes such as proliferation and survival. CDK9-IN-23 is primarily used in research applications focused on cancer biology and the modulation of gene expression pathways. -
CDK2/4/6 PROTAC Degrader
PROTAC CDK2/4/6 Degrader-1 is a potent orally bioavailable degrader targeting CDK2, CDK4, and CDK6 through the proteolysis-targeting chimera (PROTAC) mechanism. This compound functions by facilitating the ubiquitination and degradation of these cyclin-dependent kinases, thereby inhibiting their activity. Its applications extend to the study of malignant melanoma, providing valuable insights into tumor biology and potential therapeutic interventions. This degrader is synthesized as a prodrug from PROTAC CDK2/4/6 Degrader-2, enabling enhanced functionality in biological systems. -
CDK9 PROTAC
PROTAC CDK9 degrader-5 is a targeted PROTAC that specifically degrades CDK9 through the proteasomal pathway. It effectively induces degradation of CDK9 with DC50 values of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively. This reagent is a valuable tool for investigating the role of CDK9 in various biological processes and for potential therapeutic applications in cancer research. -
CDK4/6 Inhibitor
CDK4/6-IN-17 is a potent orally active inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), exhibiting an IC50 range of 10-100 nM in BE(2) cells. This compound effectively inhibits tumor growth in the COLO205 xenograft model, making it a valuable tool for cancer research focused on cell cycle regulation and therapeutic strategies targeting CDK4/6 pathways. Its application in preclinical studies provides insights into the mechanistic effects of CDK4/6 inhibition on tumor progression. -
CDK4/CDK6 Inhibitor
CDK4/6-IN-19 is a selective inhibitor of CDK4 and CDK6, demonstrating IC50 values of 0.2 nM and 5.0 nM, respectively. It effectively inhibits cellular proliferation, making it a valuable reagent for cancer research applications, particularly in studies focused on cell cycle regulation and tumor growth. Its potent activity positions CDK4/6-IN-19 as a critical tool in evaluating potential therapeutic interventions against CDK4/6-dependent malignancies. -
CDK2 Inhibitor
CDK2-IN-15 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 2.9 μM. This compound plays a significant role in cancer research by modulating cell cycle progression and apoptosis. CDK2-IN-15 is suitable for studies aimed at understanding CDK2's role in tumorigenesis and potential therapeutic strategies in oncology. -
CDK7 Inhibitor
CDK7-IN-7 is a potent and selective inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating an IC50 of less than 50 nM. This compound effectively interferes with CDK7 activity, leading to reductions in transcriptional regulation and cellular proliferation. CDK7-IN-7 is valuable for research applications focused on cancer biology, transcription regulation, and therapeutic strategies targeting cell cycle dysregulation. -
CDKs PROTAC Degrader
TMX-2138 is a potent CDKs PROTAC degrader that achieves IC50 values of 8.7 nM for CDK1/cyclinB, 10.9 nM for CDK2/cyclinA, 7.0 nM for CDK5/p25, and 25.7 nM for CDK9/cyclinT1. This compound facilitates the ubiquitination and subsequent degradation of cyclin-dependent kinases (CDKs), making it a valuable tool for investigating their roles in cellular processes. TMX-2138 is particularly relevant for research focused on ovarian cancer, enabling the study of CDK-targeted therapies and their potential therapeutic implications. -
CDK8 Inhibitor
CDK8-IN-15 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting a potent IC50 of 57 nM. This compound enhances the thermal stability of CDK8 while effectively inhibiting NF-κB signaling pathways. CDK8-IN-15 demonstrates promising biological activity in an in vitro psoriasis model induced by TNF-α, alleviating inflammation and promoting the expression of anti-inflammatory markers such as Foxp3 and IL-10. This makes it a valuable tool for research into psoriasis and related inflammatory disorders. -
CDK12/CDK13 Inhibitor
YJZ5118 is a selective inhibitor of cyclin-dependent kinases 12 and 13 (CDK12/CDK13), demonstrating IC50 values of 39.5 nM and 26.4 nM, respectively. This compound suppresses the transcription of DNA damage response genes, induces DNA damage in tumor cells, and effectively inhibits cellular proliferation while triggering apoptosis. YJZ5118 specifically impedes RNA polymerase II Ser2 phosphorylation and enhances Akt pathway activity, exhibiting synergistic effects when combined with Akt inhibitors. It is a valuable research tool for studying various cancers, including prostate cancer. -
CDK4 Inhibitor
CDK4-IN-4 is a selective inhibitor of Cyclin-dependent kinase 4 (CDK4), with an IC50 value of less than 10 nM. This compound plays a critical role in cancer research by selectively interfering with cell cycle regulation, thus inhibiting the proliferation of cancer cells. CDK4-IN-4 is suitable for studies focusing on cell cycle dynamics and the therapeutic potential of CDK4 inhibition in various cancer models. -
CDK7 Inhibitor
CDK7-IN-5 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 value of less than 100 nM. This compound exhibits significant anticancer activity, making it a valuable tool in cancer research. Its ability to modulate transcriptional regulation positions CDK7-IN-5 as a promising candidate for studies aimed at investigating novel therapeutic strategies for cancer treatment. -
CDK2 Inhibitor
Cdk2/Cyclin Inhibitory Peptide II is a specific inhibitor of cyclin-dependent kinase 2 (CDK2), primarily influencing cell cycle regulation. This peptide has demonstrated the ability to induce apoptosis in U2OS osteosarcoma cells in a dose-dependent manner. Its application in research includes investigations into cell cycle dynamics and therapeutic strategies for cancer treatment. -
CDK1 Inhibitor
CDK1-IN-7 is a potent inhibitor of Cyclin-dependent kinase 1 (CDK1). It effectively inhibits the proliferation and migration of colorectal cancer cell lines, including HCT116 and Lovo. This compound serves as a valuable tool for investigating the role of CDK1 in colorectal cancer research and therapeutic strategies. -
CDK2 Inhibitor
CDK2-IN-52 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an impressive DC50 value of 1-10 nM. This compound effectively induces cell cycle arrest and inhibits the proliferation of tumor cells, making it a valuable tool for studying CDK2-overexpressing malignancies such as breast and ovarian cancers. CDK2-IN-52 facilitates research into potential therapeutic strategies targeting CDK2 in cancer treatment. -
CDK2 Inhibitor
CDK2-IN-14 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), known for its potency in inhibiting cell cycle progression. This compound plays a significant role in cancer research, allowing for the exploration of CDK2's involvement in tumorigenesis and potential therapeutic interventions. CDK2-IN-14 is suitable for studies aimed at understanding the mechanisms of cell proliferation and offers potential insights into novel cancer treatment strategies.
