2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. CDK

CDK

Cyclin dependent kinase

CDK

Related Products

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CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.

There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.

CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisia (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).

CDK Isoform Specific Products:

CDK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-181098
    FKA-9i
    		Inhibitor
    FKA-9i is an orally active anticancer agent. FKA-9i directly binds to and promotes the degradation of oncoproteins LRPPRC (kd: 7.387 μM), YBX1 (kd: 16.52 μM) and RPN1 (kd: 26.82 μM). FKA-9i inhibits the MAPK signaling pathway and mitochondrial oxidative phosphorylation. FKA-9i also induces cancer cell cycle arrest, apoptosis, mitochondrial dysfunction and ROS accumulation. FKA-9i can be used in the research of tumors such as gastric cancer.
    FKA-9i
  • HY-153443
    CDK4-IN-2
    		Inhibitor
    CDK4-IN-2 (A17) is a CDK4 inhibitor, with Ki and IC50 values of <10 nM. Used in cancer research.
    CDK4-IN-2
  • HY-173065
    CDK9-IN-36
    		Inhibitor
    CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model.
    CDK9-IN-36
  • HY-163721
    CDK7-IN-29
    		Inhibitor
    CDK7-IN-29 (compound 20) is an inhibitor of CDK7 with an IC50 value of 1.4 nM. CDK7-IN-29 has oral activity and good pharmacokinetic (PK) properties.
    CDK7-IN-29
  • HY-182044
    MRTX849-amide-C4-(o)-carborane
    		Inhibitor
    MRTX849-amide-C4-(o)-carborane is a KRASG12C inhibitor with mutation selectivity for cells expressing KRASG12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRASG12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRASG12C-positive cancers.
    MRTX849-amide-C4-(o)-carborane
  • HY-151255
    CDK8-IN-9
    		Inhibitor
    CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC50 value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies.
    CDK8-IN-9
  • HY-170942
    CDK9/PARP-IN-1
    		Inhibitor
    CDK9/PARP-IN-1 (compound 37) is a CDK9/PARP inhibitor. CDK9/PARP-IN-1 inhibits CDK9 and PARP1 with IC50s of 118 and 107 nM, respectively. CDK9/PARP-IN-1 exhibits broad-spectrum antiproliferative effects across multiple cancer cell lines.
    CDK9/PARP-IN-1
  • HY-182810
    CDK9 ligand 5
    		Ligand
    CDK9 ligand 5 (Compound 48) is a CDK9 ligand. CDK9 ligand 5 can be used as a ligand for target protein for PROTAC to develop and design degraders of PROTAC CDK9, such as PROTAC CDK9 degrader-9 (HY-168518). CDK9 ligand 5 can be used in cancer research.
    CDK9 ligand 5
  • HY-173310
    CDK2-IN-44
    		Inhibitor
    CDK2-IN-44 (Compound 46) is an inhibitor of cyclin-dependent kinase 2 (CDK2). CDK2-IN-44 can effectively inhibit the proliferation of cancer cells and exert its activity in inhibiting cancer cell growth by arresting the cell cycle, promoting Apoptosis, and inducing cellular senescence. CDK2-IN-44 holds promise for use in the research of ovarian cancer and breast cancer.
    CDK2-IN-44
  • HY-143380
    Cdc7-IN-9
    		Inhibitor
    Cdc7-IN-9 is a potent Cdc7 inhibitor and can be used for cancer research.
    Cdc7-IN-9
  • HY-182470
    AG-012986 dihydrochloride
    		Inhibitor
    AG-012986 (dihydrochloride) is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 (dihydrochloride) causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 (dihydrochloride) induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 (dihydrochloride) exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 (dihydrochloride) can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity.
    AG-012986 dihydrochloride
  • HY-161736
    ARN25499
    		Inhibitor
    ARN25499 (compound 15) is a CDC42 inhibitor. ARN25499 can be used in cancer-related research.
    ARN25499
  • HY-155038
    Antitumor agent-104
    		Inhibitor
    Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12.
    Antitumor agent-104
  • HY-149398
    PARP-1/2-IN-2
    		Inhibitor
    PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor.
    PARP-1/2-IN-2
  • HY-147797
    EGFR/HER2/CDK9-IN-2
    		Inhibitor
    EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity.
    EGFR/HER2/CDK9-IN-2
  • HY-RS02368
    Cdk16 Rat Pre-designed siRNA Set A
    		Inhibitor

    Cdk16 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk16 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cdk16 Rat Pre-designed siRNA Set A
  • HY-E70682
    CDK4/CycD2 Recombinant Human Active Protein Kinase
    CDK4 has a well-established role in cell-cycle controland CDK4-cyclin complexes are commonly deregulated in tumorigenesis. CDK4/CycD2 Recombinant Human Active Protein Kinase is an ortholog of CDK4.
    CDK4/CycD2 Recombinant Human Active Protein Kinase
  • HY-10793
    CDK2-IN-56
    		Inhibitor
    CDK2-IN-56 (compound 39) is a pyrazoloquinazoline-3-carboxamide and CDK2/CyA inhibitor. CDK2-IN-56 can be used for the research of cancer.
    CDK2-IN-56
  • HY-151580S
    CDK2-IN-14-d3
    		Inhibitor
    CDK2-IN-14-d3 is a potent and selective CDK2 inhibitor. CDK2-IN-14-d3 can be used in research of cancer.
    CDK2-IN-14-d<sub>3</sub>
  • HY-170979
    CDK9 ligand 3
    		Ligand
    CDK9 ligand 3 is the ligand for CDK9 and can be used for synthesis of PROTAC degrader PROTAC CDK9 degrader-11 (HY-170978).
    CDK9 ligand 3
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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