Catalog No.
Product Name
Application
Product Information
Citations
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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. -
CDK4/6 PROTAC Degrader
PROTAC CDK4/6 degrader 1 is a dual-targeted degrader designed to selectively degrade cyclin-dependent kinases CDK4 and CDK6. With DC50 values of 10.5 nM and 2.5 nM, this compound effectively inhibits cell proliferation in Jurkat cells, demonstrating an IC50 of 0.18 μM. The compound promotes G1 phase cell cycle arrest and triggers apoptosis, making it a valuable tool for studying cancer biology and potential therapeutic applications in CDK-related malignancies. -
CDK12/CCNK Molecular Glue
NCT02 is a molecular glue degrader that targets CDK12 through the E3 ubiquitin ligase DDB1, resulting in the ubiquitination and subsequent proteasomal degradation of its partner protein CCNK. This mechanism leads to the downregulation of CDK12, inhibiting its downstream signaling pathways. NCT02 exhibits significant biological activity by inducing apoptosis in tumor cells, arresting the cell cycle, and selectively inhibiting the proliferation of colorectal cancer cells with TP53 mutations or belonging to the CMS4 molecular subtype. Additionally, NCT02 demonstrates potential in suppressing tumor growth in both in vitro and in vivo models. -
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. -
CCND1/CDK4 PROTAC Degrader
CPD-10 is a targeted CCND1 and CDK4 PROTAC degrader that effectively promotes the degradation of these proteins. Exhibiting significant anti-proliferative activity, CPD-10 induces apoptosis in cancer cell lines. It decreases the expression levels of cyclin D1, cyclin D3, CDK4, and phosphorylated Rb at serines 5807 and 811 in a dose-dependent manner, making it a valuable tool for research in cancer biology and therapeutic applications targeting cell cycle regulation. -
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. -
PROTAC CDK4/6 degrader
HEMTAC CDK4/6 degrader 1 is a PROTAC designed to target CDK4 and CDK6 through a dual-ligand approach involving HSP90. This compound effectively induces the degradation of CDK4/6 in B16F10 melanoma cells, leading to cell cycle arrest at the G0/G1 phase and subsequent apoptosis. It serves as a vital tool for cancer research, particularly in elucidating mechanisms of CDK4/6 regulation and their role in tumor progression. Additionally, HEMTAC CDK4/6 degrader 1 features an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds for advanced applications in chemical biology. -
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. -
CDK Inhibitor
3-Methylthienyl-carbonyl-JNJ-7706621 is a selective cyclin-dependent kinase (CDK) inhibitor, demonstrating potent activity with IC50 values of 6.4 nM for CDK1/cyclin B and 2 nM for CDK2/cyclin A. Additionally, it exhibits strong inhibition of GSK-3 (IC50=0.041 μM) and moderate inhibition against CDK4, VEGF-R2, and FGF-R2 with IC50s of 0.11, 0.13, and 0.22 μM, respectively. This compound is primarily utilized in cancer research to explore CDK-related pathways and therapeutic strategies. -
CDK1/Cyc B Inhibitor
CDK1/Cyc B-IN-1 is a selective inhibitor of the CDK1/cyclin B complex, demonstrating an IC50 of 97 nM. This compound effectively induces apoptosis and facilitates G2/M phase cell cycle arrest, making it a valuable tool for studying cell proliferation. CDK1/Cyc B-IN-1 exhibits broad-spectrum cytotoxic activity against various cancer cell lines, supporting its potential in cancer research applications. -
CDK/CRK Inhibitor
RGB-286147 is a selective ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and CDK-related kinases (CRKs), exhibiting IC50 values between 9 to 839 nM. This compound demonstrates minimal activity against non-CDK/CRK kinases. RGB-286147 induces apoptosis in cancer cells and shows significant anti-tumor effects, making it a valuable tool for research in cancer biology and therapeutic development targeting CDK pathways. -
CDK4/6 Degrader
LA-CB1 is a CDK4/6 degrader that promotes the degradation of cyclin-dependent kinases 4 and 6 through the ubiquitin-proteasome pathway. This action disrupts the CDK4/6-Cyclin D1-Rb-E2F signaling axis, leading to G0/G1 cell cycle arrest and apoptosis. LA-CB1 demonstrates potent anti-proliferative effects against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In models of triple-negative breast cancer, LA-CB1 significantly inhibits tumor growth in a dose-dependent manner, making it a valuable compound for research in breast cancer therapeutics. -
CDK6/PIM1 Inhibitor
CDK6/PIM1-IN-1 is a potent dual inhibitor targeting CDK6 and PIM1, with IC50 values of 39 nM and 88 nM, respectively, and an additional inhibition of CDK4 at an IC50 of 3.6 nM. This reagent significantly inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 demonstrates strong anti-AML activity, making it a valuable tool for research in cancer biology and therapeutic development. -
CDK Inhibitor
1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC is a cyclin-dependent kinase (CDK) inhibitor that plays a crucial role in cancer research. This compound induces apoptosis and effectively inhibits the proliferation of a variety of cancer cell lines, making it a valuable tool for studying cancer biology and therapeutic responses. Its ability to impact CDK activity provides insights into cell cycle regulation and potential cancer treatment strategies. -
HDAC1/2 and CDK2 Inhibitor
HDAC1/2 and CDK2-IN-1 is a dual inhibitor targeting HDAC1, HDAC2, and CDK2, with IC50 values of 70.7 μM, 23.1 μM, and 0.80 μM, respectively. This compound effectively disrupts the cell cycle and promotes apoptosis in tumor cells, demonstrating significant in vivo antitumor activity. It is suitable for research applications focused on cancer biology and therapeutic interventions targeting histone deacetylases and cyclin-dependent kinases. -
CDK2/9 Inhibitor
ZLMT-12 is a potent CDK2/9 inhibitor, demonstrating IC50 values of 0.002 μM and 0.011 μM against CDK9 and CDK2, respectively. This compound is derived from tacrine and exhibits weak inhibition of acetylcholinesterase (IC50 = 19.023 μM) and butyrylcholinesterase (IC50 = 2.768 μM). ZLMT-12 is characterized by low toxicity and notable antiproliferative activity, effectively inducing apoptosis and facilitating cell cycle arrest in the S and G2/M phases. This compound serves as a valuable tool for research in cell cycle regulation and therapeutic development in cancer biology. -
CDK7 Inhibitor
CDK7-IN-30 is a potent CDK7 inhibitor with an IC50 value of 7.21 nM, targeting the phosphorylation of RNA Polymerase II and CDK2. This compound demonstrates significant pro-apoptotic effects and exhibits anti-cancer activity, making it a valuable tool for cancer research. Its mechanism of action offers insights into cell cycle regulation and transcriptomic processes, facilitating the exploration of therapeutic strategies in oncology. -
CDK9 Inhibitor
A-1592668 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), which plays a critical role in transcriptional regulation. This compound induces apoptosis in various cancer cell lines and demonstrates synergistic effects when combined with Venetoclax, effectively inhibiting the growth of Jeko-1 tumors. A-1592668 is a valuable tool for research in cancer biology and therapeutic development targeting CDK9 pathways. -
CDK6/BRD4 Inhibitor
BC13 is a selective inhibitor of CDK6 and BRD4, demonstrating IC50 values of 234 nM and 36 nM, respectively. This compound exhibits notable antiproliferative effects, facilitating cell apoptosis and inducing DNA damage in various cell lines. Additionally, BC13 has been shown to elevate reactive oxygen species (ROS) levels, making it a valuable tool for research in cancer biology and therapeutic development targeting cell cycle regulation. -
HDAC1/CDK7 Inhibitor
HDAC1/CDK7-IN-1 is a dual inhibitor targeting HDAC1 and CDK7, exhibiting IC50 values of 893 nM and 248 nM, respectively. This compound effectively inhibits the proliferation of cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis specifically in HCT-116 cells, while also disrupting their migratory capacity. These properties make it a valuable tool for cancer research, particularly in exploring therapeutic strategies that target epigenetic regulation and cell cycle dynamics. -
CDK Inhibitor
5,6-Dichlorobenzimidazole riboside (DRB) functions as a selective inhibitor of several carboxyl-terminal domain kinases, notably casein kinase II and cell cycle-dependent kinases (CDKs). This nucleoside analog exhibits antitumor activity and has been shown to induce apoptosis in targeted cancer cells. Its role in modulating kinase activity makes DRB valuable for research in cancer biology and cell cycle regulation. -
CDK9 Inhibitor
Enitociclib is a highly selective CDK9 inhibitor, with an IC50 value of 3 nM, that disrupts transcriptional elongation by inhibiting Ser2/Ser5 phosphorylation of RNA polymerase II. This compound specifically targets and depletes short-lived oncogenic proteins such as c-MYC and MCL-1, thereby inducing apoptosis in tumor cells. Enitociclib also impairs enhancer RNA production and enhancer-promoter interactions, leading to downregulation of oncogene expression at the epigenetic level. Its efficacy is demonstrated through synergistic interactions with agents like Bortezomib, Lenalidomide, Pomalidomide, Venetoclax, and Paclitaxel, providing a valuable research tool for studying malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma, and pancreatic ductal adenocarcinoma. -
CDK Inhibitor
Borrelidin is a CDK inhibitor that acts by targeting threonyl-tRNA synthetase, isolating from the bacterium Streptomyces rochei. This compound demonstrates potent angiogenesis inhibition with an IC50 of 0.8 nM and induces apoptosis in endothelial tube-forming cells. Additionally, Borrelidin possesses significant antimalarial activity, exhibiting IC50 values of 1.9 nM and 1.8 nM against the K1 and FCR3 strains of Plasmodium falciparum, respectively. These properties make Borrelidin a valuable tool for research in cancer and malaria biology. -
CDK9 Inhibitor
NSC 107512 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9). As a member of the sangivamycin-like molecule class, it demonstrates significant biological activity by inhibiting cellular growth and inducing apoptosis in multiple myeloma tumors. This compound is valuable for research applications focused on cancer biology and the exploration of therapeutic strategies targeting CDK9-mediated pathways. -
CDK9 Inhibitor
AZ5576 is a potent and highly selective inhibitor of cyclin-dependent kinase 9 (CDK9), with an IC50 value of less than 5 nM. This compound effectively inhibits the phosphorylation of RNA polymerase II at Ser2, leading to a reduction in transcriptional elongation. AZ5576 is applicable in the research of hematological malignancies, aiding in the understanding of transcription regulation in cancer biology. -
CDK inhibitor
(R)-CR8 is a second-generation analog of Roscovitine and a potent inhibitor of CDK1, CDK2, CDK5, CDK7, and CDK9. It inhibits CDK1/cyclin B (IC₅₀ = 0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM), and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis, exhibits neuroprotective effects, and functions as a molecular glue degrader that promotes the degradation of cyclin K. -
CDK12/CDK13 PROTAC degrader
YJ1206 is an orally active and selective PROTAC degrader targeting CDK12 and CDK13, with an IC50 of 12.55 nM in VCaP cells. It induces DNA damage, promotes apoptosis, and leads to tumor regression in orthotopic WA74 patient-derived xenograft (PDX) models of resistant prostate cancer. Additionally, YJ1206 enhances antitumor efficacy when used in combination with AKT pathway inhibitors, highlighting its potential for combination therapy in advanced prostate cancer. -
CDK4/6 inhibitor
Culmerciclib (TQB3616) is a potent cyclin-dependent kinase (CDK)4/6 inhibitor with strong antineoplastic activity. It demonstrates significant synergistic antitumor effects in estrogen receptor (ER)-positive/HER2-negative and HER2-positive breast cancer models when combined with endocrine therapy or HER2-targeted treatments, supporting its potential for combination cancer therapy. -
CDK7 Inhibitor
SY-5609 (CDK7-IN-3) is an orally active, highly selective, and noncovalent inhibitor of CDK7, with a Kd of 0.065 nM. It demonstrates minimal activity against CDK2 (Ki = 2600 nM), CDK9 (Ki = 960 nM), and CDK12 (Ki = 870 nM), confirming its selectivity. SY-5609 induces apoptosis in tumor cells and exhibits potent antitumor activity, making it a promising candidate for targeted cancer therapy. -
CDK5 inhibitor
CP681301 is a potent CDK5 inhibitor with demonstrated antiproliferative activity. It reduces the expression of key stemness and proliferation markers—including CD133, OLIG2, SOX2, KI67, and phosphorylated CDK5—in glioma stem cells (GSCs). CP681301 also impairs self-renewal capacity in mouse glioma xenograft models and exhibits anti-tumor activity in *Drosophila*, making it a promising compound for glioma and cancer stem cell research. -
CDK2 inhibitor
INX-315 is an orally active and selective CDK2 inhibitor that induces G1 phase cell cycle arrest by reducing phosphorylation of CDK2 substrates. It exhibits dose-dependent tumor growth inhibition in xenograft mouse models and holds promise as a therapeutic candidate for cancer research targeting CDK2-driven malignancies. -
CDK8/19 inhibitor
Senexin B (SNX2-1-165; BCD-115) is a potent, highly water-soluble, and orally bioavailable inhibitor of CDK8 and CDK19, with Kd values of 140 nM for CDK8 and 80 nM for CDK19. It is a valuable tool for studying transcriptional regulation and has potential applications in cancer and inflammatory disease research. -
CDK2 inhibitor
Cirtociclib (BLU-222) is an orally active and highly selective CDK2 inhibitor. It disrupts retinoblastoma (Rb) signaling, leading to G1 cell cycle arrest and apoptosis, particularly in CCNE1-amplified endometrial cancer cells. Cirtociclib is a promising candidate for targeted therapy in CDK2-driven malignancies. -
CDK Inhibitor
Inixaciclib is a potent cyclin-dependent kinase (CDK) inhibitor with potential applications in anticancer research. By targeting CDKs involved in cell cycle regulation, Inixaciclib can inhibit tumor cell proliferation and is being explored as a therapeutic candidate in cancer treatment. -
CDK2 inhibitor
AZD8421 is a selective CDK2 inhibitor with an IC50 of 9 nM and demonstrated selectivity over CDK1, CDK4, and CDK6. It inhibits cancer cell proliferation by blocking pRB phosphorylation, leading to cell cycle arrest and senescence. AZD8421 shows strong single-agent efficacy and synergistic effects when combined with CDK4/6 inhibitors such as Palbociclib in in vivo models of breast and ovarian cancer. Additionally, it exhibits potent activity against drug-resistant breast cancer cells, making it a promising candidate for overcoming resistance in cancer therapy. -
DK/PI3K/BRD4 Inhibitor
SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of <2.5 nM for CDK4, 3.3 nM for CDK6, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, and 33 nM and 89 nM for BRD4 BD1 and BD2, respectively. It exhibits broad cytotoxic activity against cancer cells while sparing normal epithelial cells, highlighting its potential as a targeted cancer therapeutic with reduced toxicity. -
two-site molecular glue
LL-K12-18 is a two-site molecular glue that enhances the protein-protein interaction between CDK12 and DDB1, stabilizing the complex and promoting cyclin K degradation with an EC50 of 0.37 nM. It exhibits potent transcriptional repression and anti-proliferative activity in tumor cells, making it a valuable tool for cancer research. -
Casein Kinase inhibitor
BTX-A51 (Casein Kinase Inhibitor A51) is a potent, orally bioavailable inhibitor of casein kinase 1α (CK1α). It effectively induces apoptosis in leukemia cells and demonstrates strong anti-leukemic activity in preclinical models, making it a promising therapeutic candidate for hematologic malignancies.
