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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 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. -
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. -
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. -
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. -
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.

