Catalog No.
Product Name
Application
Product Information
Citations
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CDK2 Inhibitor
GW8510 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) that also targets ribonucleotide reductase M2 (RRM2). This compound demonstrates significant neuroprotective effects and possesses anticancer properties. It is utilized in scientific research to explore mechanisms of cell proliferation and apoptosis in various cancer models, making it a valuable tool for studying the role of CDK2 in cancer and neurodegenerative diseases. -
CDK2 Molecular Glue Degrader
CDK2 degrader 6 is a potent CDK2 molecular glue degrader that functions through binding to cereblon and CDK2, leading to the ubiquitination and proteasomal degradation of CDK2. With a DC50 of 46.5 nM, it effectively modulates the cell cycle and reduces proliferation in breast cancer cells. Additionally, CDK2 degrader 6 demonstrates in vivo antitumor activity in gastric cancer mouse models, making it a valuable tool for research into breast and gastric cancers. -
CDK Inhibitor
DS96432529 is a potent CDK8 inhibitor that exhibits bone anabolic properties. This compound selectively inhibits cyclin-dependent kinase 8, leading to enhanced bone formation and potential therapeutic applications in osteoporosis and other bone-related disorders. Its oral bioavailability makes it a valuable tool for in vivo studies focusing on bone metabolism and development. -
CDK2 Inhibitor
CDK2-IN-23 is a highly potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.29 nM. This compound demonstrates significant pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models, making it a valuable tool in cancer research. Its selectivity and potency provide a promising avenue for studying CDK2's role in tumorigenesis and evaluating therapeutic strategies in oncology. -
CDK9 Inhibitor
CDK9 inhibitor HH1 selectively targets cyclin-dependent kinase 9 (CDK9), a key regulator of transcriptional control. This compound effectively inhibits CDK9 activity, leading to decreased transcription of oncogenes associated with cancer progression. HH1 serves as a valuable reagent for investigating therapeutic strategies in cancer research and studying the role of CDK9 in gene expression regulation. -
CDK Inhibitor
JH-XVI-178 is a potent and selective inhibitor targeting cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 1 nM and 2 nM, respectively. This compound exhibits low clearance rates and moderate oral pharmacokinetic characteristics, making it suitable for in vivo studies. JH-XVI-178 is valuable for research in transcriptional regulation and cancer biology, particularly in contexts where CDK8 and CDK19 play critical roles in oncogenic signaling pathways. -
CDK12/13 Inhibitor
MFH290 is a selective covalent inhibitor of cyclin-dependent kinases 12 and 13 (CDK12/13). By forming a covalent bond with Cys-1039 of CDK12, MFH290 effectively inhibits the phosphorylation of serine-2 in the C-terminal domain of RNA polymerase II, thus modulating transcriptional regulation. This compound is primarily utilized in cancer research to explore therapeutic strategies targeting CDK12/13-related pathways. -
CDK7 Inhibitor
YKL-5-124 TFA is a selective and irreversible inhibitor of Cyclin-dependent kinase 7 (CDK7), with IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound demonstrates over 100-fold selectivity for CDK7 compared to CDK9 and CDK2, and it shows no activity against CDK12 and CDK13. YKL-5-124 TFA effectively induces cell-cycle arrest, inhibits E2F-driven gene expression, and has minimal impact on RNA polymerase II phosphorylation, making it a valuable tool for research in cancer biology and transcription regulation. -
CDK12/13 Covalent Inhibitor
BSJ-01-175 is a potent covalent inhibitor of CDK12 and CDK13, targeting cyclin-dependent kinases involved in cell cycle regulation. This compound exhibits strong selectivity and effectively inhibits RNA polymerase II phosphorylation, leading to the downregulation of CDK12-targeted genes in cancer cells. BSJ-01-175 is valuable for research in cancer biology and therapeutic development aimed at CDK-mediated signaling pathways. -
CDK Inhibitor
2,4,6-Trihydroxybenzoic acid is a specific inhibitor of cyclin-dependent kinases (CDKs). It exhibits significant anti-proliferative activity, making it a valuable tool for cancer research. This compound is utilized in studies aimed at elucidating the role of CDKs in cell cycle regulation and tumorigenesis. -
CDK2 Degrader
CDK2 Degrader 3 is a selective degrader of cyclin-dependent kinase 2 (CDK2) that promotes degradation of the target protein. This compound induces G1 cell cycle arrest specifically in CCNE1-amplified cancer cells, making it a valuable tool for studying cell cycle regulation. CDK2 Degrader 3 is particularly relevant for research applications related to breast cancer. -
CDK7 PROTAC Degrader
JWZ-5-13 is a potent CDK7 PROTAC degrader that selectively targets cyclin-dependent kinase 7 for ubiquitin-proteasome system-mediated degradation. It exhibits significant antiproliferative effects on various cancer cell lines, making it an essential tool for studying pathways involved in malignancies such as ovarian cancer, diffuse large B-cell lymphoma, acute T-lymphoblastic leukemia, and non-small cell lung cancer. This compound facilitates the exploration of targeted protein degradation in cancer biology, offering insights into therapeutic strategies. -
CDK2 Inhibitor
CDK2-IN-30 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 value of ≤20 nM. By modulating CDK2 activity, this compound plays a critical role in regulating cell cycle progression. CDK2-IN-30 is utilized in cancer research to explore therapeutic strategies targeting cell cycle dysregulation, providing valuable insights into tumorigenesis and potential treatment pathways. -
Cdk5 Inhibitor
BML-259 is a potent inhibitor of cyclin-dependent kinase 5 (Cdk5), exhibiting IC50 values of 64 nM and 98 nM for Cdk5 and Cdk2, respectively. This compound is valuable in research focused on neurodegenerative diseases and neuronal signaling pathways since Cdk5 plays a critical role in neuronal development and function. Its selective inhibition can enhance understanding of Cdk5-related mechanisms and potential therapeutic applications. -
CDK12 Inhibitor
CDK12-IN-E9 is a potent and selective covalent inhibitor of cyclin-dependent kinase 12 (CDK12), with additional non-covalent inhibitory activity towards CDK9. This compound effectively engages its target while minimizing interaction with ABC transporter-mediated efflux mechanisms. Furthermore, CDK12-IN-E9 demonstrates a weak binding affinity to the CDK7/CyclinH complex, exhibiting an IC50 greater than 1 μM. It holds significant potential for research applications in studying transcriptional regulation and cancer biology. -
CDK11 Inhibitor
ZNL-05-044 is a potent inhibitor of cyclin-dependent kinase 11 (CDK11), demonstrating IC50 values of 0.23 μM for CDK11A and 0.27 μM for CDK11B, as assessed using the NanoBRET assay. This compound induces G2/M cell cycle arrest and disrupts RNA splicing mechanisms. ZNL-05-044 is valuable for research applications focusing on cell cycle regulation and the role of CDK11 in RNA processing. -
CDK8/19 Inhibitor
Senexin C is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8/19). It exhibits a favorable pharmacokinetic profile, promoting tumor-specific enrichment and eliciting tumor pharmacodynamic responses. Senexin C effectively inhibits the proliferation of MV4-11 leukemia cells, demonstrating good tolerability, making it a valuable tool for research into cancer therapeutics and cell cycle regulation. -
CDK Inhibitor
PKCζ-IN-1 is a selective inhibitor of Protein Kinase C zeta (PKCζ) and Cyclin-Dependent Kinase 2 (CDK2). It exhibits an IC50 value of 5.18 nM for PKCζ and 1.04 μM for CDK2, demonstrating a remarkable 200-fold selectivity. PKCζ-IN-1 effectively reduces CDK2 activity while simultaneously inhibiting PKCζ, making it a valuable tool for research in cellular signaling pathways and cancer biology. -
CDK Inhibitor
Olomoucine is a potent ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) including CDC2/cyclin B, Cdk2/cyclin A, and Cdk2/cyclin E, with IC50 values of 7 μM, as well as CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM). By targeting these kinases, Olomoucine effectively regulates cell cycle progression and exhibits antitumor activity against melanin-producing tumor cells. This compound is valuable for research into cell cycle regulation and cancer therapy. -
CDK2/CDK5 PROTAC Degrader
TMX-2172 is a selective bivalent PROTAC that targets CDK2 and CDK5, inducing their proteasomal degradation with IC50 values of 6.5 nM and 6.8 nM, respectively. This compound demonstrates notable selectivity for CDK2 and CDK5, while sparing other cyclin-dependent kinases such as CDK1, CDK4, CDK6, CDK7, and CDK9. TMX-2172 effectively inhibits the enzymatic activity of CDK2 and CDK5, leading to a reduction in ASCL1 protein levels, induction of cancer cell death, and antiproliferative effects. This reagent is applicable in research focused on ovarian cancer and small cell lung cancer. -
CDK12/7/9 Degrader
BSJ-5-63 is a potent PROTAC degrader targeting CDK12, CDK7, and CDK9. It effectively reduces protein expression levels of these kinases as well as RNAPII and Cyclin K, resulting in decreased mRNA expression of BRCA1 and BRCA2. This compound exhibits significant anticancer activity and is particularly relevant for research focused on prostate cancer. -
CDK2 Degrader
CDK2 Degrader 5 is a targeted degrader for cyclin-dependent kinase 2 (CDK2), achieving a maximum degradation (Dmax) of over 50% and up to 80% in the HiBiT Assay. This compound is integral for probing CDK2's role in cell cycle regulation and cancer biology, making it a valuable tool for researchers investigating therapeutic strategies in oncology. Its selective degradation mechanism allows for a deeper understanding of CDK2 functions in various cellular contexts. -
CDKs Inhibitor
(S)-Roscovitine is a selective inhibitor of cyclin-dependent kinases (CDKs), demonstrating the ability to cross the blood-brain barrier effectively. This compound exhibits neuroprotective properties, making it a valuable tool in the study of neurodegenerative conditions and stroke research. Its ability to modulate CDK activity is pivotal for investigating cell cycle regulation and potential therapeutic strategies in neurological disorders. -
CDK1 Inhibitor
CDK1-IN-1 is a potent inhibitor of cyclin-dependent kinase 1 (CDK1), exhibiting an IC50 value of 161.2 nM in complex with cyclin B. This compound demonstrates significant antiproliferative activity, selectively targeting cancer cells and inducing apoptosis through a p53-dependent mechanism via the intrinsic apoptotic pathway. CDK1-IN-1 is a promising candidate for targeted antitumor therapies in oncology research. -
CDK4/6 Inhibitor
CDK4/6-IN-15 is a selective inhibitor targeting cyclin-dependent kinases 4 and 6 (CDK4/6). This compound effectively suppresses the proliferation of cancer cells by inducing a G1 phase cell cycle arrest and inhibiting the phosphorylation of retinoblastoma protein (Rb) at serine 780. CDK4/6-IN-15 is valuable in research focused on cancer biology and therapeutic interventions that modulate cell cycle dynamics. -
CDK4/6 Inhibitor
Abemaciclib metabolite M18 is a potent inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), key regulators of the cell cycle. This compound exhibits significant antitumor activity and has been utilized in the formulation of PROTAC-based degraders targeting CDK4/6 alongside a CRBN ligand. Its application in cancer research highlights its potential for therapeutic development in various malignancies. -
CDK12/CDK13 PROTAC Degrader
ZLC491 is a PROTAC degrader that selectively targets CDK12 and CDK13, utilizing cereblon- and proteasome-dependent mechanisms for degradation. This compound effectively inhibits the transcription and expression of long genes, particularly those involved in DNA damage response pathways. ZLC491 demonstrates anti-proliferative effects in various triple-negative breast cancer cell lines, making it a valuable tool for research into targeted therapies for this aggressive cancer subtype. -
CDK9 Inhibitor
CDK9-IN-13 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 value of less than 3 nM. This compound effectively modulates transcriptional regulation by inhibiting CDK9's role in phosphorylating the RNA polymerase II elongation complex. Given its high potency, CDK9-IN-13 is a valuable tool for investigating the role of CDK9 in various cellular processes and its potential implications in cancer and other diseases. -
CDK9 Inhibitor
TP-1287 is a prodrug of Alvocidib and functions as an orally active inhibitor of cyclin-dependent kinase 9 (CDK9). By inhibiting CDK9, TP-1287 disrupts transcriptional regulation and induces apoptosis in cancer cells. This reagent is valuable for research on cancer therapeutics and exploring the role of CDK9 in various cellular processes. -
CDK2 Degrader
CDK2 Degrader 7 is an orally active compound that targets cyclin-dependent kinase 2 (CDK2) for selective degradation. It exhibits effective biological activity with DC50 values of 13 nM in MKN1 cells and 17 nM in TOV21G cells, leading to G1 phase arrest in MKN1 cells. Additionally, CDK2 Degrader 7 demonstrates efficacy in achieving tumor stasis in xenograft models of HCC1569 with CCNE1 amplification. This reagent is valuable for investigating the therapeutic potential in CCNE1-amplified cancers. -
CDK2/4/6 Inhibitor
CDK2/4/6-IN-2 is a selective inhibitor of cyclin-dependent kinases 2, 4, and 6, exhibiting IC50 values under 1 μM. This compound effectively inhibits cell proliferation and reduces the phosphorylation of the retinoblastoma protein at Ser807/811 in breast cancer cells. CDK2/4/6-IN-2 is suitable for research in cancer biology, particularly in studies focused on breast cancer. -
CDKs Inhibitor
TMX-3013 is a selective inhibitor of cyclin-dependent kinases (CDKs), effectively targeting CDK1, CDK2, CDK4, CDK5, and CDK6 with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. This reagent is valuable for research involving cell cycle regulation and cancer therapeutics. Additionally, TMX-3013 can be employed in the synthesis of PROTACs that utilize a polyethylene glycol (PEG) linker and Thalidomide as a cereblon (CRBN) recruiting moiety. -
CDK12 Inhibitor
CDK12-IN-6 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), demonstrating an IC50 of 1.19 μM at elevated ATP concentrations (2 mM). It exhibits strong specificity, showing no significant inhibition of CDK2/Cyclin E or CDK9/Cyclin T1 at concentrations exceeding 20 μM. This compound is valuable for research into transcription regulation and therapeutic strategies targeting CDK12-related pathways in cancer. -
pan-CDK Inhibitor
TMX-2039 is a potent pan-CDK inhibitor that targets multiple cyclin-dependent kinases, including cell cycle CDKs (CDK1, CDK2, CDK4, CDK5, and CDK6) as well as transcriptional CDKs (CDK7 and CDK9), exhibiting IC50 values of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5, and 25 nM, respectively. This compound is particularly notable for its utility in the development of PROTACs, facilitating targeted protein degradation and expanding therapeutic strategies in oncology and beyond. TMX-2039 is an essential tool for researchers investigating cell cycle regulation and transcriptional control pathways. -
CDK7 Inhibitor
CDK7-IN-4 is a potent inhibitor of Cyclin-dependent kinase 7 (CDK7), a crucial regulator of cell cycle progression and transcriptional control. This compound exhibits significant anticancer activity by selectively inhibiting the proliferation of various cancer cell lines, including those derived from colon, breast, lung, ovary, and stomach tumors, in a dose-dependent manner. CDK7-IN-4 serves as a valuable tool for research into cancer therapeutics and the underlying mechanisms of CDK7-related oncogenesis. -
PROTAC/CDK2 Degrader
CDK2 Degrader 2 is a potent PROTAC targeting cyclin-dependent kinase 2 (CDK2), facilitating its degradation in MKN1 cells with a DC50 value of less than 100 nM. This compound employs a novel design, integrating a ligand for the target protein along with a linker and a ligand for the E3 ligase cereblon (CRBN). CDK2 Degrader 2 is valuable for research applications focused on the regulation of cell cycle progression and the exploration of targeted protein degradation mechanisms. -
CDK2 Inhibitor
CDK2-IN-3 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting a potent inhibitory activity with an IC50 of 60 nM. This compound is essential for studying the role of CDK2 in cell cycle regulation and its implications in cancer biology. CDK2-IN-3 can be utilized in various research applications, including drug discovery and the investigation of cell proliferation and differentiation processes. -
CDK2 Degrader
CDK2 Degrader 4 is a selective degrader that targets cyclin-dependent kinase 2 (CDK2). This compound promotes the degradation of CDK2, thereby inhibiting its activity in cell cycle regulation. CDK2 Degrader 4 is significant for cancer research, providing insights into CDK2's role in tumor growth and proliferation. Its application can aid in the development of targeted therapies for CDK2-dependent malignancies. -
Cdk1/2 Inhibitor
Cdk1/2 Inhibitor III is a potent and selective inhibitor targeting cyclin-dependent kinases 1 and 2, with IC50 values of 0.6 nM and 0.5 nM, respectively. This compound demonstrates a high degree of selectivity, with IC50 values of 32 nM against VEGF-R2 and 140 nM against GSK-3β. In cellular assays, Cdk1/2 Inhibitor III effectively reduces proliferation, exhibiting IC50 values of 20 nM, 35 nM, and 92 nM in HCT-116, HeLa, and A375 cell lines, respectively. Its application is relevant for studies in cancer biology and cell cycle regulation. -
CDK Inhibitor
BS-194 is a selective and potent cyclin-dependent kinase (CDK) inhibitor, primarily targeting CDK2, CDK1, CDK5, CDK7, and CDK9 with IC50 values of 3, 30, 30, 250, and 90 nM, respectively. This compound effectively inhibits the proliferation of cancer cells, making it a valuable tool for cancer research. BS-194 is particularly relevant for studies focusing on breast and colon cancer, providing insights into cellular mechanisms and potential therapeutic strategies. -
CDK7/12 Inhibitor
CDK7/12-IN-1 is a selective inhibitor of cyclin-dependent kinases 7 and 12, exhibiting IC50 values of 3 nM and 277 nM, respectively. By inhibiting CDK7 and CDK12, this compound effectively disrupts key signaling pathways involved in tumor growth and proliferation. CDK7/12-IN-1 is a valuable tool for researchers investigating the role of these kinases in cancer biology and therapeutic development. -
Cdk5 Peptide Inhibior
Cdk5i peptide is an inhibitor targeting cyclin-dependent kinase 5 (CDK5), displaying a strong binding affinity for the CDK5/p25 complex with a dissociation constant (Kd) of 0.17 μM. This peptide effectively disrupts the interaction between CDK5 and p25, subsequently reducing the kinase activity of the CDK5/p25 complex. Cdk5i peptide is particularly relevant for research into neurodegenerative diseases, providing a valuable tool for elucidating the role of CDK5 in neuronal function and pathology. -
CDK Inhibitor
Zeltociclib is a potent cyclin-dependent kinase inhibitor that demonstrates significant antitumor activity. By selectively inhibiting CDK activity, it effectively disrupts cell cycle progression, making it a valuable candidate for cancer research. Zeltociclib is particularly relevant in studies examining therapeutic strategies against various malignancies. -
PROTAC CDK9 Degrader
PROTAC CDK9 degrader-9 is a selective and potent degrader designed to target cyclin-dependent kinase 9 (CDK9) via PROTAC technology. This compound facilitates the targeted degradation of CDK9, thereby modulating transcriptional regulation and influencing cell proliferation. It is particularly useful in anti-cancer research, where the inhibition of CDK9 can lead to suppression of oncogenic pathways. -
CDK7 Inhibitor
CDK7-IN-2 is a selective inhibitor of cyclin-dependent kinases 7 (CDK7), which plays a critical role in cell cycle regulation and transcriptional activation. By targeting CDK7, this compound disrupts the phosphorylation of the Rbpl subunit of RNA Polymerase II, thereby modulating gene expression. CDK7-IN-2 is valuable for research applications focused on cancer biology, particularly in studying aggressive and treatment-resistant tumor types. -
CDK Inhibitor
CDK9-IN-11 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), a critical regulator of transcription and cell cycle progression. This compound serves as a ligand for the PROTAC CDK9 Degrader-1, facilitating targeted degradation of CDK9. CDK9-IN-11 exhibits significant biological activity in cancer research, making it a valuable tool for studies focused on cell proliferation and transcriptional regulation. -
Cdk7 Inhibitor
YKL-1-116 is a selective and covalent inhibitor of cyclin-dependent kinase 7 (Cdk7), exhibiting enhanced potency compared to THZ1 against both Cdk7 wild type (Cdk7WT) and Cdk7 activated site mutant (Cdk7as). Importantly, YKL-1-116 does not inhibit Cdk9, Cdk12, or Cdk13, making it a valuable tool for studying Cdk7's role in transcriptional regulation and cellular processes. This compound can be utilized in research applications exploring the therapeutic potential of targeting Cdk7 in cancer and other diseases. -
CDK1 Inhibitor
CDK1-IN-2 is a selective inhibitor of cyclin-dependent kinase 1 (CDK1), exhibiting an IC50 value of 5.8 μM. This compound is primarily utilized in research focusing on cell cycle regulation and cancer therapeutics. By inhibiting CDK1 activity, CDK1-IN-2 serves as a valuable tool for studying the effects of cell proliferation and apoptosis in various cancer models. -
CCNE1:CDK2 Complex Inhibitor
CDK2-IN-31 is a potent inhibitor of the CCNE1:CDK2 complex, exhibiting an IC50 of 0.13 μM. It binds to a unique allosteric pocket at the interface of CCNE1 and CDK2, leading to significant structural changes in the CDK2 A-loop that disrupt its active conformation and hinder substrate binding. This compound effectively inhibits the phosphorylation of retinoblastoma protein 1 (RB1) in CCNE1-dependent ovarian cancer cells and disrupts the coenrichment of protein PRC1 with CCNE1-N112C:CDK2 complexes. CDK2-IN-31 is valuable for research investigating ovarian cancer mechanisms and potential therapeutic targets. -
CDK Inhibitor
CDK9-IN-12 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting optimal inhibitory activity with an IC50 value of 5.41 nM. Its ability to selectively target CDK9 makes it a valuable tool in research applications focused on transcriptional regulation and cancer therapy. This compound can aid in elucidating the role of CDK9 in various cellular processes and contribute to the development of novel therapeutic strategies.
