Catalog No.
Product Name
Application
Product Information
Citations
-
CDK4/CDK6 Inhibitor
CDK4/6-IN-10 is a potent and selective inhibitor of CDK4 and CDK6, exhibiting IC50 values of 22 nM and 10 nM, respectively. This compound demonstrates significant antitumor activity and is particularly relevant for research targeting multiple myeloma (MM). Its oral bioavailability combined with its selectivity makes CDK4/6-IN-10 a valuable tool for investigating the therapeutic potential in cancer biology. -
PARP1/2/CDK12 Inhibitor
PARP-1/2-IN-2 is a potent inhibitor of PARP1, PARP2, and CDK12, exhibiting IC50 values of 34 nM, 30 nM, and 285 nM, respectively. This compound disrupts DNA damage repair mechanisms, leading to induced cell cycle arrest and apoptosis. Notable for its efficacy in targeted therapy, PARP-1/2-IN-2 effectively inhibits the growth of triple-negative breast cancer (TNBC) cells and demonstrates significant antitumor activity in TNBC xenograft models. This makes it a valuable tool for research in cancer biology and therapeutic development. -
CDK1 Inhibitor
Avotaciclib sulfate is an orally bioavailable inhibitor of cyclin-dependent kinase 1 (CDK1). It effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. This compound is particularly useful for research applications focused on oncology, including the study of pancreatic and lung cancer. -
CDK12/CDK13 Inhibitor
ZSQ836 is an orally active dual covalent inhibitor of CDK12 and CDK13, demonstrating an EC50 value of 32 nM for CDK12 inhibition. This compound has been shown to induce apoptosis and exhibits significant anticancer efficacy in vivo. ZSQ836 is a valuable tool for investigating the mechanisms and treatment strategies associated with ovarian cancer. -
CDK Inhibitor
R547 mesylate is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It exhibits inhibitory constants of 2 nM for CDK1/cyclin B, 3 nM for CDK2/cyclin E, and 1 nM for CDK4/cyclin D1. Due to its oral bioavailability and high specificity, R547 mesylate is valuable for investigating cell cycle regulation and the role of CDKs in cancer research. -
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. -
PROTAC CDK9 Degrader
PROTAC CDK9 degrader-12 is a selective CDK9 degrader that utilizes the E3 ubiquitin ligase-mediated proteasomal pathway for the degradation of CDK9, exhibiting a DC50 of 23 nM. This compound effectively inhibits CDK9-mediated transcriptional elongation of HIV-1, subsequently reducing HIV-1 RNA synthesis. PROTAC CDK9 degrader-12 is designed for research applications focused on HIV-1 infection and the study of transcriptional regulation. -
CDK Degrader
TR-213 is a potent molecular glue degrader that specifically targets Cyclin K (CDK). At a concentration of 1 μM, TR-213 demonstrates a significant inhibition of CDK12 and Cyclin levels, leading to decreases of 91% and 56%, respectively. This compound effectively inhibits RNA polymerase II activity and modulates alternative polyadenylation (APA), making it a valuable tool for cancer research and investigations into CDK-related pathways. -
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. -
CDK6-degrading PROTAC
YX-2-107 is a CDK6-degrading PROTAC with an IC50 of 4.4 nM, designed for selective degradation of CDK6. This compound effectively inhibits retinoblastoma (RB) phosphorylation and reduces FOXM1 expression in vitro. YX-2-107 has potential applications in research related to Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), demonstrating its ability to attenuate disease progression in rat models. -
CDK2 Degrader
CPS2 is a highly potent and selective PROTAC that irreversibly degrades cyclin-dependent kinase 2 (CDK2) with an IC50 of 24 nM. This compound is valuable for exploring the role of CDK2 in cell cycle regulation and has applications in the study of acute myeloid leukemia. Its unique mechanism provides a powerful tool for researchers investigating targeted protein degradation in cancer therapies. -
PROTAC CDK6 Degrader
CP-10 is a PROTAC designed to selectively target and degrade cyclin-dependent kinase 6 (CDK6) through its binding to Cereblon. Demonstrating a DC50 of 2.1 nM, this compound effectively inhibits the proliferation of various hematopoietic cancer cell lines, including multiple myeloma, and is capable of degrading both mutated and overexpressed forms of CDK6. Its specific activity makes CP-10 a valuable tool for research into CDK6-related malignancies and potential therapeutic strategies. -
PROTAC Degrader
SNX7886 is a potent PROTAC degrader targeting CDK8 and CDK19. It effectively induces degradation of CDK8 and CDK19, achieving up to 90% and 80% degradation, respectively, in 293 cells. This compound is valuable for research applications in understanding the role of CDK8/19 in various biological processes and cancer pathways. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
PROTAC CDK4/6 Degrader
BSJ-02-162 is a potent PROTAC degrader targeting CDK4/6 through the utilization of a thalidomide-based E3 ligase ligand and a selective CDK4/6 inhibitor. This compound effectively recruits ubiquitin ligases to facilitate the targeted degradation of CDK4/6, thereby modulating cellular responses to cell cycle regulation. BSJ-02-162 is designed for research applications exploring cancer therapies and the mechanisms of protein homeostasis within tumor cells. -
CDK2 molecular glue Degrader
CDK2 degrader 1 is a selective molecular glue degrader targeting cyclin-dependent kinase 2 (CDK2). It effectively induces ubiquitination and proteasomal degradation of CDK2 by binding to cereblon, achieving a Dmax greater than 80% and a Ki greater than 1 μM. This compound is utilized in cancer research, providing insights into tumor biology and potential therapeutic strategies. -
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. -
CDK2/4/6 PROTAC Degrader
PROTAC CDK2/4/6 Degrader-2 is a targeted protein degradator specifically designed to degrade cyclin-dependent kinases CDK2, CDK4, and CDK6. This compound effectively inhibits cell proliferation and induces cell cycle arrest and apoptosis in malignant melanoma cells. Its application extends to cancer research, particularly in investigating the role of CDK2/4/6 in tumor biology. The compound can also be converted into its prodrug form, enabling versatile utilization in various assays related to cancer therapeutics.
