CDK

(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.

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.

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 Modulator 1 functions as a selective inhibitor of cyclin-dependent kinases (CDKs), influencing cell cycle progression. This compound has shown significant biological activity in blocking CDK activity, making it a valuable tool for research in cancer biology and cell proliferation studies. It is particularly useful in investigations related to cancer therapeutics and the regulation of cellular growth control pathways.

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-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-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.

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-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.

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.

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.

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.

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-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 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-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.

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-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.

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.

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.

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.

MG16 is a prodrug of 10-Methoxycamptothecin, primarily targeting CDK6 and ASK1. It effectively induces cell cycle arrest and apoptosis in cancer cells, demonstrating significant anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer. This compound is valuable for research applications focused on cancer therapeutics and the exploration of cell cycle regulation.

KI-CDK9d-32 is a selective and potent degrader designed to target CDK9 through a PROTAC mechanism (DC50: 0.89 nM). It facilitates the ubiquitination and subsequent degradation of CDK9, effectively inhibiting the MYC signaling pathway and disrupting nucleolar homeostasis. This compound demonstrates significant anticancer activity, particularly against acute lymphoblastic leukemia and pancreatic cancer, making it a valuable tool for research in cancer biology and therapeutic development.

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.

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.

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.

CDK9-IN-30 is a selective inhibitor of Cyclin-dependent kinase 9 (CDK9), primarily targeting its role in transcription regulation. This compound exhibits potent antiviral activity by disrupting HIV-1 replication, making it a valuable tool for studying HIV-1 pathogenesis and exploring therapeutic strategies. Its inhibition of CDK9 can also provide insights into broader cellular processes related to transcriptional regulation and oncogenesis.

PROTAC CDK9 degrader-4 is a potent CDK9 degradation agent that facilitates the targeted degradation of cyclin-dependent kinase 9. This compound effectively modulates transcriptional regulation by harnessing the power of PROTAC technology, leading to significant biological activity in various cellular contexts. It holds potential applications in cancer research and the study of transcriptional control mechanisms.

CDK7 ligand 2 is a selective inhibitor targeting CDK7, a crucial cyclin-dependent kinase involved in transcription regulation. This compound exhibits significant potential in drug discovery and development, particularly in the synthesis of PROTACs (Proteolysis Targeting Chimeras). Its application in research may facilitate novel therapeutic approaches for diseases associated with abnormal transcriptional control.

CDK9 ligand 4 functions as a potent ligand for cyclin-dependent kinase 9 (CDK9). This compound is instrumental in the design and development of PROTAC-based degraders, facilitating targeted degradation of CDK9 proteins, which plays a crucial role in transcriptional regulation and HIV-1 infection research. CDK9 ligand 4 contributes significantly to studies aimed at therapeutic strategies against viral infections and dysregulated transcriptional processes.

CDK4 Degrader 1 (ML 1–71) is a molecular glue degrader that specifically targets cyclin-dependent kinase 4 (CDK4). This compound promotes the selective degradation of CDK4, leading to reduced cell proliferation and induction of cell cycle arrest in various cancer models. It serves as a valuable tool for investigating CDK4's role in tumorigenesis and for the development of targeted therapies in cancer research.

HZ1 is a selective inhibitor of cyclin-dependent kinase-like 3 (CDKL3) that operates via targeted inhibition of this kinase. It demonstrates significant tumor-suppressive activity and has potential to circumvent resistance to CDK4/6 inhibitors. This compound is applicable in cancer research, particularly in studies focused on cell cycle regulation and therapeutic resistance mechanisms.

Ribociclib succinate is an orally active inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), functioning through ATP-competitive mechanisms. It demonstrates potent activity with IC50 values of 10 nM and 39 nM against CDK4 and CDK6, respectively, while exhibiting over 1,000-fold selectivity against the cyclin B/CDK1 complex. This selectivity makes it a valuable tool in cancer research, particularly in studies targeting cell cycle regulation and therapeutic strategies for hormone receptor-positive breast cancer.

Ribociclib succinate hydrate is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), functioning through competitive inhibition of ATP binding. With IC50 values of 10 nM and 39 nM against CDK4 and CDK6, respectively, it demonstrates significant selectivity over the cyclin B/CDK1 complex. This compound is utilized in cancer research, particularly in studies focusing on cell cycle regulation, tumor proliferation, and the therapeutic potential in various malignancies. Its ability to cross the blood-brain barrier allows for exploration in central nervous system-related cancers.

PROTAC CDK2-pRb degrader-1 is an orally active PROTAC that targets cyclin-dependent kinase 2 (CDK2) for degradation. This compound effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine 807/811 by promoting the ubiquitination and proteasomal degradation of CDK2. Demonstrating significant biological activity with EC50 values of 12 nM and 125 nM in human cells, PROTAC CDK2-pRb degrader-1 is particularly useful in research focused on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers, as it inhibits tumor growth and induces tumor stasis in xenograft models.