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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. -
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. -
CDK4 Inhibitor
CDK4-IN-2 is a potent inhibitor of cyclin-dependent kinase 4 (CDK4) with a Ki and IC50 value of less than 10 nM. This compound effectively regulates cell cycle progression and is valuable in cancer research, particularly in studies focused on oncogenic signaling pathways and cell proliferation. It serves as a crucial tool for evaluating potential therapeutic strategies targeting CDK4 in various malignancies. -
CDK7 Inhibitor
CDK7-IN-29 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 value of 1.4 nM. This compound demonstrates oral bioavailability and favorable pharmacokinetic properties, making it suitable for in vivo studies. Its ability to inhibit CDK7 positions it as a valuable tool for investigating cellular processes related to transcription and cell cycle regulation, particularly in cancer research applications. -
CDK8 Inhibitor
CDK8-IN-9 is a potent type II cyclin-dependent kinase 8 (CDK8) inhibitor, exhibiting an IC50 value of 48.6 nM. This compound effectively inhibits tumor growth and serves as a valuable tool in colorectal cancer research. Its targeting of CDK8 makes it suitable for investigations into the molecular mechanisms underlying cancer progression and treatment responses. -
CDK2 Inhibitor
CDK2-IN-44 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2), a crucial regulator of the cell cycle. This compound effectively blocks the proliferation of cancer cells by inducing cell cycle arrest, promoting apoptosis, and triggering cellular senescence. CDK2-IN-44 is particularly relevant for research applications focused on ovarian and breast cancer, offering valuable insights into therapeutic strategies targeting CDK2 activity. -
CDK4/6 Inhibitor
CDK4/6-IN-13 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), pivotal regulators of the cell cycle. This compound demonstrates low nanomolar potency, exhibiting significant antiproliferative activity against various cancer cell lines. CDK4/6-IN-13 also offers favorable metabolic properties and pharmacokinetic profiles, making it a valuable tool for research in oncology and cell cycle regulation. -
CDK Inhibitor
Fovinaciclibum is a cyclin-dependent kinase (CDK) inhibitor that demonstrates significant antineoplastic activity. This compound is designed to selectively inhibit CDK enzymes, thereby disrupting cell cycle progression and promoting apoptosis in cancer cells. It is utilized in research focusing on tumor biology and therapeutic strategies for various malignancies. -
CDK1 Inhibitor
CDK1-IN-4 is a selective inhibitor of cyclin-dependent kinase 1 (CDK1), exhibiting IC50 values of 44.52 nM for CDK1, 624.93 nM for CDK2, and 135.22 nM for CDK5. This compound effectively disrupts the cell cycle, leading to inhibition of cancer cell proliferation. CDK1-IN-4 is suitable for research applications related to cancer biology and therapeutics targeting cell cycle regulation. -
CDK2 Inhibitor
CDK2-IN-27 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), demonstrating potent inhibition with IC50 values of less than 10 nM for the CDK2/cyclin E1 complex and 10-20 nM for the CDK2/cyclin B1 complex. This compound is crucial for studies focused on cell cycle regulation and cancer research, where CDK2 plays a significant role in cell proliferation. CDK2-IN-27 provides valuable insights into therapeutic strategies targeting CDK2 to halt tumor growth and enhance cancer treatment regimens. -
CDK inhibitor
(R)-DRF053 is a selective cyclin-dependent kinase (CDK) inhibitor that primarily targets Cdk5. This compound is known to enhance the formation of ductal precursor β cells, making it valuable for investigating pancreatic development and diabetes research. Additionally, (R)-DRF053 has been shown to inhibit Dil-ox-LDL uptake and reduce CD36 gene expression induced by advanced glycation end products (AGEs) in U937 cells, indicating its relevance in studies related to atherosclerosis and metabolic diseases. -
CDK Inhibitor
CCT68127 is a selective inhibitor of cyclin-dependent kinases (CDKs) that functions by disrupting cell cycle progression. This compound demonstrates significant anti-proliferative activity in various cancer cell lines, making it a valuable tool for cancer research. CCT68127 can be utilized to investigate CDK-related pathways and explore potential therapeutic strategies for malignancies. -
CDK Inhibitor
Olomoucine II is a potent inhibitor of cyclin-dependent kinases (CDKs), specifically exhibiting IC50 values of 0.06 µM for CDK9/cyclin T, 0.1 µM for CDK2/cyclin E, 0.45 µM for CDK7/cyclin H, 7.6 µM for CDK1/cyclin B, and 19.8 µM for CDK4/cyclin D1. This compound demonstrates significant antiproliferative activity, making it a valuable tool for studies investigating cell cycle regulation and cancer biology. Its selectivity and efficacy position Olomoucine II as an important reagent for research applications aimed at understanding CDK-related pathways. -
CDK Inhibitor
CDK1/2/4-IN-2 is a selective inhibitor of cyclin-dependent kinases 1, 2, and 4. This compound demonstrates significant anti-proliferative effects, making it a valuable tool for investigating cell cycle regulation and cancer biology. It is suitable for use in preclinical studies aimed at exploring therapeutic strategies for various malignancies. -
CDK2 Inhibitor
CDK2-IN-39 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), a crucial regulator of the cell cycle. This compound demonstrates significant activity in modulating CDK2-mediated phosphorylation, making it a valuable tool for studies on cell proliferation, cancer research, and cellular signaling pathways. CDK2-IN-39 can help elucidate the role of CDK2 in the progression of various cancers and may aid in the development of therapeutic strategies targeting cell cycle dysregulation. -
CDK2 Inhibitor
CDK2-IN-21 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2) with an IC50 of 0.24 µM. This compound demonstrates potent inhibitory activity, making it a valuable tool for cancer research. By targeting CDK2, CDK2-IN-21 can help elucidate the role of cell cycle regulation in tumorigenesis and facilitate the development of potential therapeutic strategies against cancer. -
CDK Inhibitor
ZK 304709 is a multi-target cyclin-dependent kinase (CDK) inhibitor that plays a critical role in cell cycle regulation. It effectively inhibits various CDKs, thereby preventing proliferation in cancer cells. This compound is valuable for studying mechanisms of cell cycle control and can aid in the development of novel therapeutic strategies against cancer. -
CDK9 Inhibitor
CDK9-IN-34 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9) with an IC50 value of 0.25 μM. It demonstrates significant cytotoxic effects on cancer cell lines HCT116, MCF7, and K652, with IC50 values of 1.43 μM, 3.01 μM, and 50.27 μM, respectively. Additionally, CDK9-IN-34 exhibits antiviral properties against coronavirus 229E, displaying an IC50 of 145.92 μM. This compound serves as a valuable tool for investigating the roles of CDK9 in cancer and viral pathogenesis. -
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. -
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. -
CDK7 Inhibitor
LDC4297 hydrochloride is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), exhibiting an IC50 of 0.13 nM. This compound effectively inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM and demonstrates broad antiviral activity against multiple families of viruses, including Herpesviridae, Adenoviridae, Poxviridae, Retroviridae, and Orthomyxoviridae, with EC50 values ranging from 0.02 to 1.21 μM. LDC4297 hydrochloride is valuable for research into viral infections and the underlying mechanisms of CDK7 in cellular pathways.

