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Catalog No.
Product Name
Application
Product Information
Citations
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CDK Inhibitor
Otviciclib is a potent cyclin-dependent kinase (CDK) inhibitor that demonstrates significant anti-proliferative effects against various solid tumor cell lines, including HCT116, NCIH82, and DU145. This compound effectively induces cell cycle arrest in the G2/M phase and triggers apoptosis, exhibiting a favorable toxicity profile towards normal cells. Otviciclib shows broad-spectrum anticancer activity, making it a valuable tool for research applications related to colon, pancreatic, and lung cancers. -
CDK9/HDAC Dual Inhibitor
CDK9/HDAC1/HDAC3-IN-1 is a dual inhibitor targeting CDK9 and HDACs. With IC50 values of 0.17 μM for CDK9, 1.73 μM for HDAC1, and 1.11 μM for HDAC3, this compound effectively disrupts the activity of these proteins. It induces cancer cell apoptosis and causes cell cycle arrest at the G2/M phase. Additionally, CDK9/HDAC1/HDAC3-IN-1 exhibits broad-spectrum anti-cancer effects, demonstrating efficacy against various malignancies, including breast, cervical, and liver cancers, as evidenced in murine TNBC MDA-MB-231 xenograft models. -
CDK2 Inhibitor
CDK2-IN-9 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.63 µM. This compound demonstrates significant antiproliferative activity, inducing apoptosis and causing cell cycle arrest at the S and G2/M phases. CDK2-IN-9 is suitable for research applications focused on melanoma and the exploration of CDK2's role in cell cycle regulation and cancer biology. -
CDKs Inhibitor
(Rac)-Roscovitine is a selective inhibitor of cyclin-dependent kinases (CDKs), functioning by competitively binding to their active sites in place of ATP. This mechanism effectively inhibits CDK phosphorylation activity, leading to apoptosis in cancer cells. As a valuable research tool, (Rac)-Roscovitine is applicable in studies of cancer and various conditions associated with CDK dysregulation, including neurodegenerative diseases, cardiac disorders, and chronic inflammation. -
HDAC/CDK Inhibitor
CDK/HDAC-IN-2 is a dual inhibitor of histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs), exhibiting IC50 values of 6.4 nM for HDAC1, 0.25 nM for HDAC2, 45 nM for HDAC3, and >1000 nM for HDAC6,8, as well as 8.63 nM for CDK1, 0.30 nM for CDK2, and >1000 nM for CDK4,6,7. This compound demonstrates significant antiproliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. CDK/HDAC-IN-2 is particularly valuable in cancer research due to its potent antitumor efficacy. -
CDK9 Inhibitor
CDK9-IN-18 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), effectively obstructing its phosphorylation activity. This compound demonstrates significant anticancer properties, promoting apoptosis in various cancer cell lines while exhibiting low cellular toxicity. Its mechanism of action makes CDK9-IN-18 a valuable tool for research into cancer therapeutics and the regulation of gene expression. -
CDK2/Topo I Inhibitor
ZLHQ-5f is a dual inhibitor of Cyclin-dependent kinase 2 (CDK2) and Topoisomerase I (Topo I), exhibiting an IC50 of 0.145 μM against CDK2/CycA2. This compound effectively induces S-phase cell cycle arrest and triggers apoptosis in HCT116 cancer cells. Its favorable safety profile supports its potential applications in cancer research and therapeutic development. -
CDK2/9 Inhibitor
CDK2/9-IN-1 is an orally active dual inhibitor targeting cyclin-dependent kinases CDK2 and CDK9, with IC50 values of 0.004 μM and 0.009 μM, respectively. This compound induces apoptosis through G2/M cell cycle arrest, demonstrating notable antitumor activity. CDK2/9-IN-1 is useful for research applications focused on cancer biology and the modulation of cell cycle regulation. -
CDK2 Inhibitor
CDK2-IN-55 is a selective CDK2 inhibitor with an IC50 value of 4.7 nM, also exhibiting significant inhibitory action on CDK1 (IC50 = 26.3 nM), alongside moderate inhibition of Aurora A (IC50 = 92.0 nM) and CDK9 (IC50 = 288 nM). Its weak inhibitory profile on CDK4, CDK6, DYRK1A, and GSK3β (IC50 > 1000 nM) highlights its specificity. CDK2-IN-55 demonstrates potent anti-proliferative effects against various cancer cell lines, effectively inducing cell cycle arrest and apoptosis, making it a valuable tool for research related to colorectal, lung, and cervical cancers. -
Cdk1 Inhibitor
BMI-1026 is a potent cyclin-dependent kinase 1 (Cdk1) inhibitor with an IC50 of 2.3 nM. This compound effectively induces apoptosis by interfering with cell cycle progression, specifically by causing a G2-M phase arrest. Its ability to modulate Cdk1 activity makes BMI-1026 valuable for research applications focused on cell division, cancer biology, and therapeutic strategies targeting cell cycle dysregulation. -
CDK1 Inhibitor
CDK1-IN-8 is a potent inhibitor of Cyclin-dependent kinase 1 (CDK1), primarily targeting the regulation of cell cycle progression. This compound effectively inhibits cell migration, induces apoptosis, and causes cell cycle arrest at the G2/M phase. Notably, CDK1-IN-8 leads to significant downregulation of CDK1 protein levels in HepG2 cells, making it a valuable tool for investigating mechanisms in hepatocellular carcinoma research. -
CDK7 Inhibitor
SY-5102 is a potent and selective inhibitor of cyclin-dependent kinase 7 (CDK7) with a Kd of 0.03 nM. This compound exhibits significant anti-proliferative activity in HCC70 cells, with an EC50 of 9 nM, and effectively modulates CDK7-mediated functions, including downregulation of CDK2 Thr160 and RNA polymerase II Ser5 phosphorylation. SY-5102 induces G2/M cell cycle arrest and decreases c-Myc oncogene expression, leading to enhanced apoptosis in cancer cells. It is particularly relevant for research focused on triple-negative breast cancer (TNBC). -
CDKs Inhibitor
ZLWT-37 is a potent, orally active inhibitor of cyclin-dependent kinases (CDKs), specifically exhibiting IC50 values of 0.002 μM against CDK9 and 0.054 μM against CDK2. This compound effectively induces apoptosis and arrests the cell cycle at the G2/M phase in HCT116 cells. ZLWT-37 is valuable for researching CDK-related pathways and investigating therapeutic strategies in cancer treatment. -
CDK4 Inhibitor
ZDLD13 is a selective inhibitor of Cyclin-Dependent Kinase 4 (CDK4) with an IC50 of 0.38 μM. This β-carboline compound demonstrates potent anti-cancer activity against HCT116 cells, effectively inhibiting colony formation, invasion, and migration, while also inducing apoptosis and G1 phase cell cycle arrest. Additionally, ZDLD13 significantly inhibits tumor growth in HCT116 tumor xenograft models, making it a valuable tool for cancer research. -
CDK1 Inhibitor
CGP-74514 hydrochloride is a highly selective inhibitor of cyclin-dependent kinase 1 (CDK1) with an IC50 of 25 nM. By inhibiting the CDK1/cyclin B complex, it effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in tumor cells. This compound shows potential for use in research related to bladder cancer and other malignancies driven by CDK1 deregulation. -
PDE2/CDK2 Inhibitor
Aristolochic acid D is a selective inhibitor of PDE2 with an IC50 of 4.673 μM and CDK2 with an IC50 of 25 μM, derived from Aristolochia indica L. This compound demonstrates significant anti-inflammatory properties while exhibiting a non-carcinogenic and non-nephrotoxic profile. Aristolochic acid D is valuable for research applications focused on inflammation and tumor-related diseases, offering insights into therapeutic strategies. -
SHP2/CDK4 Inhibitor
SHP2/CDK4-IN-1 is a potent dual inhibitor of SHP2 and CDK4, exhibiting IC50 values of 4.3 nM and 18.2 nM, respectively. This compound effectively induces G0/G1 phase cell cycle arrest, thereby inhibiting the proliferation of triple-negative breast cancer (TNBC) cell lines. In preclinical studies, SHP2/CDK4-IN-1 demonstrated significant antitumor efficacy in the EMT6 syngeneic mouse model, making it a valuable tool for research on TNBC. -
CDK1/CDK2 Inhibitor
K00546 is a highly selective inhibitor of cyclin-dependent kinases CDK1 and CDK2, exhibiting IC50 values of 0.6 nM and 0.5 nM, respectively, for CDK1/cyclin B and CDK2/cyclin A complexes. In addition, K00546 effectively inhibits CDC2-like kinases CLK1 and CLK3, with IC50 values of 8.9 nM and 29.2 nM, respectively. This compound is valuable for research focused on cell cycle regulation and the mechanistic study of kinase activity in cancer biology. -
CDK Inhibitor
GW297361 is an oxindole compound identified as a cyclin-dependent kinase (CDK) inhibitor with a selective action on Pho85 in cellular systems. It demonstrates significant inhibitory effects on yeast Cdk1 and Pho85, exhibiting IC50 values of 20 nM and 400 nM, respectively. This compound is valuable for research applications focused on cell cycle regulation and the study of kinase signaling pathways. -
CDK/DYRK Inhibitor
ML 315 hydrochloride is a selective dual inhibitor targeting cyclin-dependent kinases (CDKs) and dual-specificity tyrosine-regulated kinases (DYRKs), exhibiting IC50 values of 68 nM and 282 nM, respectively. This compound is utilized in research focused on cancer and neurological diseases, providing insights into cell cycle regulation and neurodegenerative pathways. ML 315's potent inhibitory action makes it a valuable tool for studying therapeutic strategies in these critical areas. -
CDK Inhibitor
(R)-(+)-O-Demethylbuchenavianine is a selective inhibitor of Cyclin-dependent kinases (CDKs), specifically targeting CDK1 and CDK5 with IC50 values of 1.1 and 0.95 μM, respectively. Additionally, it shows inhibitory activity against glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1), and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), though with IC50 values greater than 10 μM. This compound is important for research focused on cell cycle regulation, cancer therapeutics, and neurodegenerative diseases. -
CDK/DYRK Inhibitor
ML 315 is a selective dual inhibitor of cyclin-dependent kinases (CDK) and dual-specificity tyrosine phosphorylation-regulated kinase (DYRK), exhibiting IC50 values of 68 nM and 282 nM, respectively. It demonstrates significant biological activity in modulating cell cycle progression and neuronal signaling pathways. This compound has applications in cancer research and the study of neurological diseases, facilitating insights into therapeutic targets within these areas. -
CDK4/6/9-AURKA/B Inhibitor
LCI133 is a selective multikinase inhibitor targeting CDK4, CDK6, CDK9, and AURKA/B, exhibiting nanomolar potency (IC50 values of 4.7 nM, 10.2 nM, 4.1 nM, 2.8 nM, and 10.6 nM, respectively). It effectively induces S/G2 cell-cycle arrest and promotes significant apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. Additionally, LCI133 demonstrates notable antitumor efficacy in preclinical models, particularly in BE(2)-C neuroblastoma xenograft studies, making it a valuable tool for cancer research and therapeutic development. -
CDK inhibitor
SNS-032 (BMS-387032) is a highly selective and potent inhibitor of cyclin-dependent kinases (Cdks) 2, 7, and 9, with in vitro growth inhibitory effects and ability to induce apoptosis in malignant B cells. -
CDK inhibitor
Flavopiridol HCl is an inhibitor of cyclin-dependent kinases. The (-)-cis form induces apoptosis in particular tumor cells. -
CDK Inhibitor
PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity. -
CDK Inhibitor
(S)-CR8 is a selective inhibitor of cyclin-dependent kinases (CDKs), demonstrating potent inhibitory activity with IC50 values of 0.060 μM for CDK2/cyclin E, 0.080 μM for CDK2/cyclin A, 0.11 μM for CDK9/cyclin T, 0.12 μM for CDK5/p25, and 0.15 μM for CDK1/cyclin B. This compound effectively reduces the survival of SH-SY5Y cells, with an IC50 of 0.40 μM, making it a valuable tool for studying cell cycle regulation and potential therapeutic strategies in cancer research. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
CDK Inhibitor
NSC693868 is a selective inhibitor of cyclin-dependent kinases CDK1 and CDK5, demonstrating IC50 values of 600 nM and 400 nM, respectively. This compound also exhibits weaker inhibition of GSK3β with an IC50 of 1 µM and does not affect CDC25 activity. NSC693868 is employed in research to elucidate the functions of CDK1 and CDK5 within various cellular signaling pathways. -
GSK-3α/β Inhibitor
(E/Z)-BIO-acetoxime is a potent and selective inhibitor of GSK-3α/β, exhibiting an IC50 of 10 nM. This compound demonstrates exceptional selectivity with over 200-fold preference against CDK5/p25, CDK2/cyclin A, and CDK1/cyclin B, with IC50 values of 2.4, 4.3, and 63 μM, respectively. Its strong inhibitory activity makes it a valuable tool for research focused on signaling pathways involved in cell proliferation, differentiation, and apoptosis. -
CDK9 Inhibitor
Tambiciclib is a potent and selective CDK9 inhibitor with an IC50 of 1 nM, exhibiting over 200-fold selectivity against other cyclin-dependent kinases and significant selectivity over DYRK1A/B and a wide range of kinases. This compound has demonstrated effective in vitro and in vivo antileukemic activity in acute myeloid leukemia (AML) models by inhibiting RNA Polymerase II phosphorylation, leading to downregulation of MCL1 and MYC, and subsequent induction of apoptosis. Tambiciclib is suitable for research applications focused on AML and related oncological studies. -
Cyclin/CDK Inhibitor
VMY-1-103 is a selective inhibitor of the cyclin-dependent kinase (CDK) complex, effectively arresting the cell cycle at the G1 phase. It has been demonstrated to reduce mitochondrial membrane potential, induce p53 phosphorylation, and trigger PARP cleavage, ultimately activating caspase-3 and initiating apoptosis in LNCaP prostate cancer cells. This compound is valuable for research applications focused on cancer biology and the mechanisms of cell cycle regulation and apoptosis. -
KDM1/CDK1 Inhibitor
KDM1/CDK1-IN-1 is a potent inhibitor of both KDM1 and CDK1, exhibiting IC50 values of 0.096 μM and 0.078 μM, respectively. This compound effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in HOP-92 cancer cells. Additionally, KDM1/CDK1-IN-1 demonstrates significant cytotoxic effects against a range of cell lines, including CCRF-CEM, HOP-92, and Hep-G2, with IC50 values of 16.34 μM, 3.45 μM, and 7.79 μM, respectively. Its ability to target critical regulators of the cell cycle makes KDM1/CDK1-IN-1 valuable for cancer research applications. -
CDK1 Inhibitor
Avotaciclib is an orally active inhibitor of cyclin-dependent kinase 1 (CDK1). It effectively inhibits tumor cell proliferation and induces apoptosis, making it a valuable compound for cancer research. This reagent is particularly relevant in the study of cancers, including pancreatic and lung cancer, where CDK1 plays a critical role in cell cycle regulation and tumor growth. -
Cyclins/Cdk Inhibitor
Aminopurvalanol A is a selective inhibitor of Cyclins/Cdk complexes, primarily targeting the G2/M-phase transition. This compound effectively inhibits cancer cell differentiation and proliferation, making it a valuable tool for cancer research. Additionally, Aminopurvalanol A has been shown to disrupt sperm fertilizing ability by inhibiting capacitation-dependent actin polymerization, highlighting its potential in reproductive biology studies. -
CDK9 Inhibitor
(-)-Enitociclib is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), with demonstrated capacity to induce apoptosis in various cancer cell lines. By inhibiting CDK9, it effectively reduces phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase II, leading to downregulation of critical oncogenes such as MYC and MCL1. This compound exhibits significant anti-proliferative effects against MYC-positive lymphoma and multiple myeloma cells, and shows synergistic potential when combined with therapies such as Bortezomib and Lenalidomide, making it a valuable tool in hematological cancer research. -
CDK8 Inhibitor
CDK8-IN-13 is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting an IC50 value of 51.9 nM. This compound induces apoptosis and modulates the expression of phosphorylated STAT1 at serine 727 and STAT5 at serine 726. Due to its antitumor properties, CDK8-IN-13 is valuable for research applications focusing on cancer biology and therapeutic development targeting the CDK8 pathway. -
CDK7 Inhibitor
Samuraciclib is a selective, ATP-competitive inhibitor of CDK7, exhibiting an IC50 of 41 nM. This compound demonstrates significant selectivity over CDK1, CDK2, CDK5, and CDK9, with fold selectivities of 45, 15, 230, and 30, respectively. Samuraciclib effectively inhibits the proliferation of breast cancer cell lines, with GI50 values ranging from 0.2 to 0.3 μM, indicating its potential as an effective therapeutic agent in oncology research. -
CDK1 Inhibitor
Avotaciclib trihydrochloride is an orally active inhibitor of cyclin-dependent kinase 1 (CDK1). This compound has demonstrated the ability to inhibit tumor cell proliferation and induce apoptosis, making it a valuable tool for cancer research. Avotaciclib trihydrochloride is particularly relevant for studies focused on pancreatic and lung cancers. -
CDK4 Inhibitor
CDK4-IN-3 is a potent irreversible inhibitor of cyclin-dependent kinase 4 (CDK4), exhibiting an IC50 of 25 nM and demonstrating over 10-fold selectivity for CDK4 compared to CDK6. This compound effectively arrests the cell cycle in the G₁ phase, leading to the induction of apoptosis in tumor cells. CDK4-IN-3 is valuable for research applications focused on solid tumors, including breast and lung cancers. -
CDK1 Inhibitor
CGP-74514 is a potent and selective inhibitor of cyclin-dependent kinase 1 (CDK1), exhibiting an IC50 of 25 nM. By targeting the CDK1/cyclin B complex, CGP-74514 effectively halts the cell cycle at the G2/M phase and triggers apoptosis in tumor cells. This compound is particularly valuable for research focused on bladder cancer and related therapeutic applications. -
CDK Inhibitor
CDK9-IN-7 is a selective and potent inhibitor of cyclin-dependent kinase 9 (CDK9), demonstrating an IC50 of 11 nM. This compound selectively inhibits CDK9 over other cyclin-dependent kinases, such as CDK4 and CDK6, with IC50 values of 148 nM and 145 nM, respectively. CDK9-IN-7 exhibits significant antitumor activity, inducing apoptosis in non-small cell lung cancer (NSCLC) cells, arresting the cell cycle in the G2 phase, and reducing the stemness characteristics of NSCLC. It is a valuable tool for research into cancer biology and potential therapeutic applications. -
Pan-CDK Inhibitor
AG-012986 is a potent pan-CDK inhibitor targeting multiple cyclin-dependent kinases including CDK1, CDK2, CDK4, CDK5, CDK6, and CDK9. It demonstrates significant biological activity with Kis of 9.2 nM for CDK4/cyclin, 44 nM for CDK1/cyclin B, and 94 nM for CDK2/cyclin A, alongside IC50 values of 4 nM for CDK9/cyclin T and 22 nM for CDK5/p35. AG-012986 effectively inhibits cell proliferation in cancer cell lines, inducing cell cycle arrest and apoptosis, making it a valuable tool for cancer research and therapeutic development. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib hydrochloride is a potent inhibitor of CDK2, JAK2, and FLT3, exhibiting IC50 values of 13 nM, 73 nM, and 56 nM, respectively. This orally active compound demonstrates significant efficacy in inhibiting the proliferation of various cancer cell lines. It is a valuable tool for research into therapeutic strategies targeting cell cycle regulation and signal transduction pathways in cancer. -
CDK Inhibitor
RGB-286638 free base is a potent CDK inhibitor targeting cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5, with IC50 values of 1, 2, 3, 4, 5, and 5 nM, respectively. Additionally, it inhibits GSK-3β, TAK1, Jak2, and MEK1, exhibiting IC50 values of 3, 5, 50, and 54 nM. This compound is valuable for research in cell cycle regulation, cancer therapeutics, and signaling pathways involving kinase activity. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib citrate is a potent inhibitor targeting CDK2, JAK2, and FLT3 kinases. This compound demonstrates significant biological activity in disrupting cell cycle progression and signaling pathways associated with cell proliferation and survival. It is utilized in cancer research applications, particularly for studies involving hematological malignancies and solid tumors where these kinases are dysregulated. -
CDK2/JAK2/FLT3 Inhibitor
Zotiraciclib hydrochloride is a novel small molecule inhibitor targeting cyclin-dependent kinase 2 (CDK2), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase 3 (FLT3). This reagent demonstrates anti-tumor activity by downregulating the Myc oncogene through CDK9 inhibition, contributing to reduced tumor growth. Zotiraciclib hydrochloride is particularly relevant for research into cancers capable of crossing the blood-brain barrier, and elevated levels of the MCL-1 protein may indicate its potential as a prognostic marker and therapeutic target in cancer studies.
