CDK Inhibitor

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.

CDK5 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC₅₀ of 0.21 μM. CDK2-IN-32 shows cytotoxicity against Vero cells with an IC₅₀ of 28.52 μM.

CDK1-IN-8 is a CDK1 inhibitor. CDK1-IN-8 inhibits cell migration, induces apoptosis, and arrests the cell cycle at the G2/M phase. CDK1-IN-8 leads to a significant downregulation of CDK1 protein levels in HepG2 cells. CDK1-IN-8 can be used for the study of hepatocellular carcinoma.

PIN1-IN-8 is a covalent inhibitor of Pin1, with IC₅₀ values of 4.19 μM and 1.54 μM against purified Pin1 and Pin1 enzymatic activity, respectively. PIN1-IN-7 exerts antiproliferative effects and induces apoptosis by downregulating c-Myc and Cyclin D1. PIN1-IN-7 can be used in the research of triple-negative breast cancer.

Cdc7-IN-12 (compound 1) is a potent CDC7 inhibitor with an IC₅₀ of <1 nM. Cdc7-IN-12 shows antiproliferative activities with IC₅₀ of 100-1000 nM in COLO205 cells. Cdc7-IN-12 has the potential for the research of cancer.

ODN BW001 sodium is an oligodeoxynucleotide (ODN). ODN BW001 sodium plays a regulatory role in the proliferation and activation of osteoblast.

CDK-IN-19 (Compound example 67.2) is a CDK inhibitor. CDK-IN-19 can be used for research of cancer.