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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
CDK1 Inhibitor
Albanol B is a selective inhibitor of Cyclin-dependent kinase 1 (CDK1), derived from arylbenzofuran. This compound demonstrates significant potential in cancer research by inhibiting cell proliferation and down-regulating CDK1 expression, leading to G2/M cell cycle arrest and apoptosis in cancer cells. Additionally, Albanol B exhibits anti-Alzheimer's activity, antibacterial properties, and antioxidant effects, while also inducing mitochondrial reactive oxygen species (ROS) production and enhancing phosphorylation levels of AKT and ERK1/2. -
HDACs/CDKs Dual Inhibitor
CDK/HDAC-IN-3 is a dual inhibitor targeting histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs). It exhibits potent and selective activity, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM against CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, respectively. This compound is particularly relevant for research in acute myeloid leukemia (AML), providing insights into therapeutic strategies for this disease. -
CDK6/PIM1 Inhibitor
CDK6/PIM1-IN-1 hydrochloride is a potent dual inhibitor targeting CDK6 and PIM1, exhibiting IC50 values of 39 nM and 88 nM, respectively, along with significant inhibition of CDK4 (IC50=3.6 nM). This compound effectively inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 hydrochloride is a valuable tool for research investigating the role of CDK6 and PIM1 in cancer biology, particularly in the context of AML. -
cyclin D1 Inhibitor
Dehydrozingerone is a cyclin D1 inhibitor derived from ginger, known for its ability to downregulate cyclin D1 expression and induce G1 phase cell cycle arrest. This compound effectively reduces the proliferative capacity of castration-resistant prostate cancer cells in vitro and inhibits subcutaneous tumor growth by targeting cell proliferation and angiogenesis. Additionally, dehydrozingerone demonstrates notable antibacterial and antifungal properties, making it suitable for research into castration-resistant prostate cancer, bacterial infections, and food spoilage due to fungal infections. -
cyclin D1/CDK4 Inhibitor
Arcyriaflavin A is an indolo[2,3-a]carbazole compound that primarily acts as a cyclin D1/CDK4 inhibitor. This compound, derived from the marine ascidian Eudistoma sp. and the slime mold Arcyria denudata, demonstrates significant biological activity in regulating the cell cycle. Arcyriaflavin A is particularly relevant for research applications focusing on colon and lung cancer, providing insights into tumor growth and potential therapeutic strategies. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-2 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 145.35 nM, 129.07 nM, and 117.13 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to concurrently inhibit these kinases positions it as a promising candidate for studies focused on targeted therapy and oncogenic signaling pathways. -
EGFR/HER2/CDK9/COX-2 Inhibitor
CDK9-IN-41 is a potent inhibitor of CDK9, EGFR, HER2, and COX-2, exhibiting IC50 values of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM respectively. This compound demonstrates significant antitumor activity across various cancer cell lines, including leukemia, colon, melanoma, ovarian, and breast cancer. It serves as a valuable tool for exploring the role of these kinases in cancer biology and therapeutic applications. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-3 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 191.08 nM, 132.65 nM, and 113.98 nM, respectively. This compound demonstrates significant antitumor activity, making it valuable for research in cancer therapies and signaling pathways involving these targets. Its inhibitory effects on cell proliferation in cancer models may aid in the understanding and development of targeted treatment strategies. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-1 is a highly active inhibitor of EGFR, HER2, and CDK9, displaying IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively. This compound demonstrates significant antitumor properties, making it a valuable tool for cancer research. Its ability to target multiple kinases involved in cell proliferation and survival pathways supports investigations into therapeutic strategies for various malignancies. -
EGFR/CDK-2 Inhibitor
EGFR/CDK2-IN-1 is an inhibitor targeting both the epidermal growth factor receptor (EGFR) and cyclin-dependent kinase 2 (CDK2). This compound exhibits significant cytotoxicity against breast cancer MCF7 cells and liver cancer HepG2 cells, making it a valuable tool in cancer research. Its dual inhibition profile allows for exploration of synergistic effects in therapeutic strategies targeting these critical pathways in cancer proliferation and survival. -
CDK9/PARP Inhibitor
CDK9/PARP-IN-1 is a potent inhibitor of CDK9 and PARP1, demonstrating IC50 values of 118 nM and 107 nM, respectively. This dual inhibition results in significant antiproliferative effects across various cancer cell lines, making it a valuable tool for cancer research. CDK9/PARP-IN-1 is particularly relevant for studies investigating the therapeutic potential of targeting these pathways in oncology. -
PARP1/CDK12 Inhibitor
Antitumor agent-104 is a potent inhibitor of PARP1 and CDK12, targeting critical pathways in DNA damage repair in tumors. By inhibiting PARP1 enzymatic activity, it effectively reduces PAR protein levels, thus impairing the cellular mechanisms that protect tumor cells. This compound serves as a valuable tool in cancer research, especially in studies focused on understanding tumor biology and exploring novel therapeutic strategies. -
CDK-1/PARP-1 Inhibitor
UNPD139734 is a potent inhibitor of Cyclin-Dependent Kinase 1 (CDK-1) and Poly (ADP-ribose) polymerase 1 (PARP-1), forming stable complexes with both target proteins. This compound serves as a valuable lead for the structural optimization of dual-target anticancer agents, particularly in the context of breast cancer research. Its dual inhibition mechanism offers a promising avenue for investigating novel therapeutic strategies in oncology. -
CDK Inhibitor
Ryuvidine is a selective inhibitor of cyclin-dependent kinases (CDKs), specifically targeting SET domain-containing protein 8 (SETD8) with an IC50 of 0.5 µM, thereby suppressing the monomethylation of histone H4 at lysine 20 (H4K20). Additionally, Ryuvidine inhibits CDK4 with an IC50 of 6.0 µM and KDM5A, leading to the blockade of DNA synthesis. Its biological activity includes anticancer effects against various tumor types, including breast cancer, and it also demonstrates potential therapeutic benefits in arthritis research. -
CDK9/EZH2 Dual-target Inhibitor
CDK9/EZH2-IN-1 is a dual-target inhibitor designed to inhibit both CDK9 and EZH2, exhibiting IC50 values of 83.9 nM and 108.6 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing DNA double-strand breaks (DSBs). It effectively inhibits the proliferation of various cancer cell lines, including MKN45, MDA-MB-453, and SW620, with IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM, respectively. CDK9/EZH2-IN-1 is suitable for research applications in understanding cancer cell biology and therapeutic development. -
CDK2/CDK5 Inhibitor
(S)-PHA533533 is an inhibitor of cyclin-dependent kinases CDK2 and CDK5, demonstrating blood-brain barrier permeability with IC50 values of 37 nM and 55 nM, respectively. This compound effectively restores UBE3A expression by downregulating UBE3A-ATS, thereby alleviating the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 is a valuable tool for research applications related to Angelman syndrome and offers insights into therapeutic strategies for this genetic disorder. -
CDK2 Inhibitor
CDK2-IN-12 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 11.6 μM. This compound also inhibits human carbonic anhydrase isoforms I, II, IX, and XII, with respective KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 demonstrates notable anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. -
CA/CDK2 Inhibitor
Carbonic anhydrase inhibitor 14 is a potent inhibitor of carbonic anhydrases (CAs), exhibiting Ki values of 1203 nM for hCA I, 99.7 nM for hCA II, 9.4 nM for hCA IX, and 27.7 nM for hCA XII. Additionally, it effectively inhibits cyclin-dependent kinase 2 (CDK2) with an IC50 of 20.3 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications targeting both CA and CDK2 pathways. -
CDK2 Inhibitor
CDK2-IN-11 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), demonstrating an IC50 of 6.4 μM. With inhibitory constant (KI) values of 23.4 nM, 56.3 nM, and 44.3 nM for human carbonic anhydrases II, IX, and XII, respectively, it exhibits significant enzyme inhibition. CDK2-IN-11 is primarily utilized in anticancer research, making it a valuable tool for studies targeting cell cycle regulation and tumor progression. -
CDK/GSK3β/JNK Inhibitor
Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation. -
CDK9 Inhibitor
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. -
CDK9 Inhibitor
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 Inhibitor
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.
