Catalog No.
Product Name
Application
Product Information
Citations
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CDK12/13 Inhibitor
CDK12/13-IN-1 is a selective inhibitor of cyclin-dependent kinases 12 and 13 (CDK12/13). This compound demonstrates significant antitumor activity by interfering with the phosphorylation of RNA polymerase II, thereby disrupting transcriptional regulation in cancer cells. CDK12/13-IN-1 is utilized in research focused on cancer biology, particularly in exploring therapeutic strategies for tumors exhibiting CDK12/13 dependency. -
CDK4/6 Inhibitor
Dalpiciclib isethionate is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). By inhibiting the kinase activity of these enzymes, Dalpiciclib effectively disrupts the progression of the cell cycle from the G1 phase to the S phase, which reduces abnormal cellular proliferation. This compound is primarily utilized in cancer research, particularly in the study of breast cancer, where CDK4/6 dysregulation plays a critical role in tumor growth. -
CDK Inhibitor
CDK-IN-10 is a potent cyclin-dependent kinase (CDK) inhibitor that selectively blocks CDK activity. This compound has demonstrated significant antitumor effects, making it an invaluable tool for cancer research. Researchers can utilize CDK-IN-10 to investigate CDK regulation in cell cycle progression and explore its potential in therapeutic applications against various cancers. -
CDK8 Inhibitor
CDK8-IN-10 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting an IC50 value of 8.25 nM. This compound is instrumental in the study of CDK8's role in cancer progression and may provide insights into therapeutic strategies targeting this kinase. Its potency and selectivity make it a valuable tool for cancer research applications. -
CDK Inhibitor
AG-12275 is a selective cyclin-dependent kinase (CDK) inhibitor that targets CDK2 and CDK5. It exhibits potent inhibition of cancer cell proliferation by disrupting the cell cycle progression. This compound is valuable for investigating the roles of CDKs in cancer biology and the development of novel therapeutic strategies targeting these pathways. -
CDK9 Inhibitor
CDK9-IN-46 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), which plays a crucial role in transcriptional regulation. This compound demonstrates significant biological activity in reducing the phosphorylation of RNA polymerase II, thereby inhibiting gene transcription associated with cancer cell proliferation. CDK9-IN-46 is utilized in cancer research to explore therapeutic strategies targeting CDK9-dependent pathways. -
CDK4/6 Inhibitor
CDK4/6-IN-16 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), exhibiting a potent activity with an IC50 of 0.013 μM for CDK4. This compound has significant implications for the study of CDK4-mediated pathologies, particularly in cancer research. Its targeted inhibition of CDK4/6 may aid in the exploration of cell cycle regulation and therapeutic strategies for cancer treatment. -
CDK4/6 Inhibitor
YY173 is a selective dual inhibitor of CDK4 and CDK6, demonstrating IC50 values of 7.7 nM and 88 nM, respectively. This compound effectively inhibits the proliferation of Jurkat cells with an IC50 of 1.46 μM. YY173 serves as a valuable tool for research in cancer biology and is suitable for the synthesis of PROTAC CDK4/6 degrader 1, facilitating studies on targeted protein degradation. -
CDK7 Inhibitor
CDK7-IN-12 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), which is integral to transcriptional regulation and cell cycle control. This compound demonstrates significant capacity to impede the proliferation of malignant tumors in both in vitro and in vivo studies. CDK7-IN-12 is suitable for research applications focused on cancer biology and therapeutic development. -
CDK2 Inhibitor
CDK2-IN-36 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), a crucial regulator of the cell cycle. This compound exhibits significant anticancer activity by disrupting CDK2-mediated phosphorylation events, thereby promoting apoptosis and inhibiting tumor cell proliferation. CDK2-IN-36 is valuable for research focused on cancer biology, cell cycle regulation, and the development of targeted cancer therapies. -
CDK12/13 Inhibitor
CDK12/13-IN-2 is a covalent inhibitor targeting cyclin-dependent kinases 12 and 13, with IC50 values of 15.5 nM and 12.2 nM for CDK12 and CDK13, respectively. This compound effectively inhibits the proliferation of breast cancer cells and is particularly relevant for research into triple-negative breast cancer. Its selective action provides a valuable tool for studying the effects of CDK12/13 inhibition in cancer biology. -
CDK2 Inhibitor
CDK2-IN-46 is a highly selective cyclin-dependent kinase 2 (CDK2) inhibitor with an IC50 value of 0.3 nM. It demonstrates a significant selectivity of over 200-fold compared to other kinases, including CDK1, CDK4, CDK6, CDK7, and CDK9. This compound is valuable for studying cell cycle regulation and has shown improved pharmacokinetic profiles in both rat and cynomolgus monkey models, making it suitable for preclinical research in cancer biology and therapeutic development. -
CDK2/E Inhibitor
CDK2-IN-18 is a potent inhibitor of cyclin-dependent kinases CDK2/E and CDK4/D1, exhibiting IC50 values of 8 nM and 46 nM, respectively. This compound effectively inhibits tumor cell proliferation, making it valuable for cancer research applications, particularly in studying cell cycle regulation and exploring therapeutic strategies targeting CDK pathways. -
Cyclin A Inhibitor
CDK-IN-15 is a potent inhibitor of Cyclin A, exhibiting an IC50 value of 0.14 μM. This compound is useful for studying cell cycle regulation and the inhibition of cyclin-dependent kinases in cancer research. Its biological activity makes it a valuable tool in investigating the role of Cyclin A in various cellular processes and the development of novel therapeutic strategies. -
CDK Inhibitor
Tacaciclib is a selective cyclin-dependent kinase (CDK) inhibitor that exerts antineoplastic effects by disrupting cell cycle progression. It primarily targets CDK2 and CDK9, leading to the inhibition of cancer cell proliferation. This compound is useful in cancer research for exploring therapeutic pathways and mechanisms of resistance in tumor models. -
CDK8 Inhibitor
CDK8-IN-7 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting a Kd of 3.5 nM. This compound demonstrates notable cytotoxicity across various cancer cell lines, including MOLM-13, OCI-AML3, MV4-11, NRK, and H9c2, with IC50 values ranging from 4.8 to 25 µM. CDK8-IN-7 is a valuable tool for investigating the role of CDK8 in acute myeloid leukemia (AML) and other related malignancies. -
CDK2/4 Inhibitor
CDK2/4-IN-2 is a potent dual inhibitor of cyclin-dependent kinases 2 and 4, exhibiting IC50 values below 100 nM. This compound is instrumental in cancer research, providing insights into cell cycle regulation and the therapeutic potential of targeting CDK pathways. Its efficacy in inhibiting CDK2 and CDK4 makes it a valuable reagent for investigating tumor cell proliferation and developing anti-cancer strategies. -
CDK Inhibitor
rel-(2S,3R)-Voruciclib is a selective cyclin-dependent kinase (CDK) inhibitor, specifically the (2S,3R)-enantiomer of Voruciclib. This compound exhibits potent inhibition of CDK activity, making it valuable for the study of cell cycle regulation and cancer therapeutics. Its oral bioavailability allows for convenient administration in research applications focused on tumor growth inhibition and cell proliferation modulation. -
CDK-7 Inhibitor
CDK7-IN-25 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 of less than 1 nM. This compound plays a critical role in regulating transcription and cell cycle progression, making it a valuable tool in cancer research. CDK7-IN-25 can be utilized to investigate the effects of CDK7 inhibition on tumor cell proliferation and survival, as well as to explore its potential therapeutic applications in oncology. -
CDK Inhibitor
CDK2-IN-7 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), providing valuable insights into cancer biology. With an IC50 of less than 50 nM, it effectively disrupts CDK2 activity, facilitating studies on cell cycle regulation and tumor progression. This compound is useful for researchers investigating CDK-targeted therapies and cell proliferation in various cancer models. -
CDK4/6 Inhibitor
CDK4/6-IN-21 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), exhibiting IC50 values of 3.88 nM and 3.31 nM for CDK4 and CDK6, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research, particularly in studies targeting cell cycle regulation and proliferation in various malignancies. Its potent inhibition of CDK4 and CDK6 positions it as a promising candidate for therapeutic development in oncology. -
CDK4/CDK6 Inhibitor
CDK4/6-IN-5 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6), exhibiting binding affinities (Kis) of 0.2 nM for the CDK4/Cyclin D1 complex and 4.4 nM for the CDK6/Cyclin D3 complex. This compound demonstrates significant biological activity in interrupting cell cycle progression, making it a valuable tool for cancer research, especially in studies focused on tumor proliferation and therapeutic resistance mechanisms. Its potency and selectivity make CDK4/6-IN-5 an important reagent for investigating the roles of CDK4 and CDK6 in various cancer types. -
CDK8 Inhibitor
CDK8-IN-5 is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) with an IC50 of 72 nM. This compound exhibits significant anti-inflammatory activity, evidenced by a 43% enhancement in IL-10 levels. CDK8-IN-5 is applicable in research focusing on inflammatory bowel disease and related inflammatory conditions. -
CDK2 Inhibitor
Anticancer agent 30, a 3-arylidene-2-oxindole derivative, functions primarily as a selective inhibitor of cyclin-dependent kinase 2 (CDK2). This compound exhibits potent anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to modulate CDK2 activity positions it as a promising candidate for investigations into cell cycle regulation and tumor progression. -
CDK Inhibitor
AG-024104 is a potent cyclin-dependent kinase (CDK) inhibitor, demonstrating Ki values of 2.3 nM for CDK1/cyclin B, 1.8 nM for CDK2/cyclin A, and 0.67 nM for CDK4/cyclin D. By effectively inhibiting the kinase activity of these CDKs, AG-024104 is valuable in studying cell cycle regulation and cancer pathways. This inhibitor is also utilized as a negative control in peripheral leukocyte toxicity studies during preclinical development. -
CDK2 Inhibitor
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG) is a specific inhibitor of cyclin-dependent kinase 2 (CDK2). It has demonstrated the ability to induce apoptosis in U2OS osteosarcoma cells in a dose-dependent manner, making it a valuable tool for studying CDK2-mediated cell cycle regulation. This peptide is suitable for research applications aimed at understanding the role of CDK2 in cancer biology and potential therapeutic interventions. -
CDK Inhibitor
CDK-IN-19 is a potent cyclin-dependent kinase (CDK) inhibitor that selectively targets CDK enzymes involved in cell cycle regulation. This compound demonstrates significant antiproliferative activity and is valuable for cancer research applications, particularly in studying CDK-mediated pathways and the effects of cell cycle disruption in oncogenesis. Its role as a CDK inhibitor makes it a crucial tool for investigating therapeutic strategies aimed at cancer treatment. -
CDK Inhibitor
SNX2-1-108 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8). This compound plays a pivotal role in modulating transcriptional regulation and is essential for various cellular processes. Its inhibition of CDK8 activity has significant implications in cancer research, particularly in studying the regulatory pathways of gene expression and potential therapeutic interventions in CDK8-dependent malignancies. -
CDK2 Inhibitor
EF-4-177 is an allosteric inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 87 nM. This compound effectively interferes with spermatogenesis, making it a valuable tool for studying male reproductive biology and the regulatory mechanisms of cell cycle progression. Its oral activity enhances its utility in pharmacological research and potential therapeutic applications. -
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. -
PKMYT1 Inhibitor
PKMYT1-IN-12 is a selective inhibitor of the serine/threonine kinase PKMYT1, demonstrating an IC₅₀ of 2.6 nM. This compound effectively inhibits the phosphorylation of CDK1, with an IC₅₀ of 44 nM, making it a valuable tool for studying cell cycle regulation. Additionally, PKMYT1-IN-12 serves as a target protein ligand for the synthesis of PROTAC D16-M1P2, facilitating advancements in targeted protein degradation research. -
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.
