CDK

Cat. No.

A25079

CAS No.

1209002-43-6

VMY-1-103

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.

Cat. No.

A25107

CAS No.

2541626-49-5

PROTAC CDK2/4/6 Degrader-2

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.

Cat. No.

A25347

CAS No.

2938990-92-0

KDM1/CDK1-IN-1

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.

Cat. No.

A25837

CAS No.

87084-99-9

Albanol B

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.

Cat. No.

A26449

CAS No.

2944087-54-9

CDK/HDAC-IN-3

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.

Cat. No.

A26763

CAS No.

265312-55-8

Ryuvidine

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.

Cat. No.

A26789

CAS No.

3081246-18-3

CDK9/EZH2-IN-1

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.

Cat. No.

A28429

CAS No.

1080-12-2

Dehydrozingerone

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.

Cat. No.

A28505

CAS No.

118458-54-1

Arcyriaflavin A

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.

Cat. No.

A28564

CAS No.

1180924-34-8

EGFR/HER2/CDK9-IN-2

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.

Cat. No.

A28713

CAS No.

1038061-96-9

CDK9-IN-41

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.

Cat. No.

A28716

CAS No.

422276-47-9

EGFR/HER2/CDK9-IN-3

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.

Cat. No.

A28719

CAS No.

879730-44-6

EGFR/HER2/CDK9-IN-1

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.

Cat. No.

A28754

CAS No.

2841405-96-5

EGFR/CDK2-IN-1

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.

Cat. No.

A28955

CAS No.

3032818-67-7

CDK9/PARP-IN-1

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.

Cat. No.

A28956

CAS No.

2245272-16-4

Antitumor agent-104

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.

Cat. No.

A28987

CAS No.

116764-24-0

UNPD139734

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.

Cat. No.

A30005

CAS No.

53-85-0

5,6-Dichlorobenzimidazole riboside

Synonyms: DRB

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.

Cat. No.

A30075

CAS No.

1610408-97-3

Enitociclib

Synonyms: (+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib

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.

Cat. No.

A30207

CAS No.

7184-60-3

Borrelidin

Synonyms: Treponemycin

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.

Cat. No.

A30230

CAS No.

22242-89-3

NSC 107512

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.

Cat. No.

A30247

CAS No.

2751721-40-9

AZ5576

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.

Cat. No.

A30318

CAS No.

1983983-41-0

Avotaciclib

Synonyms: BEY1107

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.

Cat. No.

A30420

CAS No.

220792-57-4

Aminopurvalanol A

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.

Cat. No.

A30427

CAS No.

1610408-96-2

(-)-Enitociclib ((R)-Enitociclib)

Synonyms: (R)-Enitociclib; (-)-BAY-1251152; (-)-VIP152

(-)-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.