CDK Inhibitor

CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with K_is of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively. (from patent WO2019207463A1 example A93).

CDK2-IN-55 (Compound 12c) is a CDK2 inhibitor with an IC₅₀ value of 4.7 nM. CDK2-IN-55 also has a strong inhibitory effect on CDK1 (IC₅₀ = 26.3 nM), moderate inhibitory effects on Aurora A (IC₅₀ = 92.0 nM) and CDK9 (IC₅₀ = 288 nM), and very weak inhibitory activities on CDK4, CDK6, DYRK1A, and GSK3β (IC₅₀ > 1000 nM). CDK2-IN-55 shows strong anti-proliferative activity against various cancer cell lines, inducing cell cycle arrest and apoptosis. CDK2-IN-55 can be used for research on colorectal cancer, lung cancer, and cervical cancer.

CDK4 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK8-IN-5 is a potent CDK8 inhibitor with an IC₅₀ of 72 nM. CDK8-IN-5 shows anti-inflammatory activities with 43% IL-10 enhancement rate. CDK8-IN-5 has the potential for the research of inflammatory bowel disease.

8‑Acetonyldihydronitidine is a naturally occurring benzophenanthridine alkaloid with antibacterial, antifungal, and anti-proliferative activities against colorectal cancer cells. 8‑Acetonyldihydronitidine inhibits Staphylococcus aureus and exerts a potent antifungal effect against Cladosporium cladosporioides. 8‑Acetonyldihydronitidine activates the p53 signaling pathway, upregulates the expression of target genes including p21, BAX, and FAS, downregulates cyclin A and cyclin B, and induces cell cycle arrest and apoptosis, thereby suppressing the proliferation of colorectal cancer cells. 8‑Acetonyldihydronitidine is used in research related to colorectal cancer, fungal infections, and bacterial infections.

Anticancer agent 30 (compound 6f-Z), a 3-arylidene-2-oxindole derivative, is a selective CDK2 inhibitor with potent anticancer activity.

BMI-1026 is a cyclin-dependent kinase 1 (Cdk1) inhibitor with IC₅₀ of 2.3 nM. BMI-1026 induces apoptosis by arresting the G2-M phase.

CDK-IN-14 (B34) is a CDK2 inhibitor (IC₅₀=0.097 μM) with anti-hepatocellular carcinoma activity. CDK-IN-14 blocks the cell cycle of HepG-2 cancer cells through a caspase-mediated mechanism and induces apoptosis.

PROTAC BET Degrader-15 is a BET PROTAC degrader with DC₅₀ values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer.

CDK4 Rat Pre-designed siRNA Set A contains three designed siRNAs for CDK4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cdc7-IN-18 (compound 1-2) is a potent CDC7 inhibitor with an IC₅₀ of 1.29 nM for Cdc7/DBF4 enzyme. Cdc7-IN-18 shows antiproliferative activities with IC₅₀ of 53.62 nM in COLO205 cells.

CDK8-IN-20 (Compound 67j) is a selective, potent and orally active type I CDK8 inhibitor with an IC₅₀ of 70.5 nM. CDK8-IN-20 shows IC₅₀ values of 147.8, 726.9 and 217.4 nM for homologous kinase CDK19, CDK7 and CDK9. CDK8-IN-20 can inhibit the Wnt/β-catenin pathway and downregulate the expression of β-catenin, Cyclin D1, and c-Myc. CDK8-IN-20 can induce ROS production and cause G2/M and S phase arrest. CDK8-IN-20can be used for the research of cancer, such as colon cancer.

AG-024104 is a CDK inhibitor with K_i values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development.

CDK2-IN-57 is a selective Cdk2/CycE inhibitor with an IC₅₀ of 2.8 nM. CDK2-IN-57 inhibits Cdk1/2 kinase activity, blocks cell cycle progression, induces G₀-phase cell cycle arrest, and prevents S-phase entry. CDK2-IN-57 can be used for the research of colon carcinoma.

FAK1/2 Ligand-1 is a FAK1/FAK2 ligand with K_D values of 2.9 μM and 2.5 μM for binding to FAK1 and FAK2, respectively. FAK1/2 Ligand-1 induces G2/M phase arrest, activates DNA damage-related signaling pathways, and reduces the phosphorylation level of CDK1. Antitumor agent-220 is applicable to the research of triple-negative breast cancer.

Cdk7 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk7 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cucurbitacin E (Standard) is the analytical standard of Cucurbitacin E. This product is intended for research and analytical applications. Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.

PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC₅₀ of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer.

Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner.

CAIX/CDK-2-IN-1 is a dual-acting inhibitor of carbonic anhydrase IX (CA IX) and cyclin-dependent kinase-2 (CDK-2) with IC₅₀ values of 0.29 μM and 0.32 μM. The zein nanoparticls of CAIX/CDK-2-IN-1 can induce cancer cells apoptosis. CAIX/CDK-2-IN-1 can be used for the research of cancer, such as lung cancer.