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

CDK

Cyclin dependent kinase

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).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-162416
    CDK7-IN-27
    Inhibitor
    CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependent kinase 7 (CDK7), with Ki of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase.
    CDK7-IN-27
  • HY-146214
    CDK4/6-IN-13
    As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.
    CDK4/6-IN-13
  • HY-128491
    UNC10112785
    Inhibitor
    UNC10112785 is a serine/threonine kinase inhibitor with a human GSK-3β IC50 of 0.031 μM, human CDK-2 IC50 of 0.016 μM, and human CDK-4 IC50 of 1.99 μM. UNC10112785 can be used for the research of type 2 diabetes.
    UNC10112785
  • HY-137432D
    Avotaciclib sulfate
    Inhibitor
    Avotaciclib (BEY1107) sulfate is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib sulfate can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib sulfate can be used in the research of cancer such as pancreatic cancer and lung cancer.
    Avotaciclib sulfate
  • HY-122888
    MPT0L145
    Inhibitor
    MPT0L145 is a PIK3C3/FGFR inhibitor, with a Kd value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC.
    MPT0L145
  • HY-RS02357
    Cdk12 Mouse Pre-designed siRNA Set A
    Inhibitor

    Cdk12 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk12 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Cdk12 Mouse Pre-designed siRNA Set A
  • HY-159535
    Fovinaciclibum
    Inhibitor
    Fovinaciclibum (Fovinaciclib) is a cyclin dependent kinase inhibitor, with antineoplastic effect.
    Fovinaciclibum
  • HY-163374
    Cdc7-IN-20
    Inhibitor
    Cdc7-IN-20 (EP-05) is an orally effective and selective Cdc7 inhibitor with IC50 and Ki values of 0.93 and 0.11 nM, respectively. Cdc7-IN-20 has antitumor activity.
    Cdc7-IN-20
  • HY-181116
    Anticancer agent 298
    Anticancer agent 298 is a bi-nuclear Cu(II)-hydrazone complexe. Anticancer agent 298 can bind to the CDK-2 active site (PDB ID: 3IG7) via hydrogen bonds with key amino acid residues. Anticancer agent 298 exerts cytotoxic effects against hepatocellular carcinoma cells, and has lower cytotoxicity against normal human embryonic kidney cells. Anticancer agent 298 can be used for the research of hepatocellular carcinoma.
    Anticancer agent 298
  • HY-168333
    5-HT6 inverse agonist 1
    Inhibitor
    5-HT6 inverse agonist 1 (Compound 33) is an antagonist for 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. 5-HT6 inverse agonist 1 inhibits the 5-HT6R mediated Cdk5 and mTOR signaling pathway. 5-HT6 inverse agonist 1 reduces tactile hypersensitivity in spinal nerve ligation (SNL)-induced rat model.
    5-HT6 inverse agonist 1
  • HY-182383
    VMY-1-101
    Inhibitor
    VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer.
    VMY-1-101
  • HY-115904
    FLT3/CDK4-IN-1
    Inhibitor
    FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo.
    FLT3/CDK4-IN-1
  • HY-182789
    VEGFR2-IN-86
    Inhibitor
    VEGFR2-IN-86 is a dual VEGFR2/CDK2 inhibitor, with an IC50 of 0.06 μM against VEGFR2 and an IC50 of 0.78 μM against CDK2. VEGFR2-IN-86 induces G-phase cell cycle arrest, reduces colony-forming ability and tumor cell migration capacity, and exerts antiproliferative activity in cancer cells. VEGFR2-IN-86 can be used for the research of breast cancer and prostate cancer.
    VEGFR2-IN-86
  • HY-183789
    CDK2-IN-59
    Inhibitor
    CDK2-IN-59 is a CDK2 inhibitor with a IC50 of 66.33 μM. CDK2-IN-59 stably interacts within the CDK2 active site and induces apoptosis in breast cancer cells. CDK2-IN-59 can be used for the research of breast cancer.
    CDK2-IN-59
  • HY-N7045R
    Isosilybin B (Standard)
    Inhibitor
    Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.
    Isosilybin B (Standard)
  • HY-E70665
    CDK17/CycY Recombinant Human Active Protein Kinase
    CDK17 is highly expressed in terminally differentiated neurons, particularly those found in hippocampal regions and olfactory bulbs. CDK17/CycY Recombinant Human Active Protein Kinase is an ortholog of CDK17.
    CDK17/CycY Recombinant Human Active Protein Kinase
  • HY-181131
    Anticancer agent 300
    Inhibitor
    Anticancer agent 300 (compound P14) is a CCND1, CDK4, CDK6, and CCNE1 modulator, with anti-proliferative, cell-cycle modulatory, senescence-inducing, and apoptosis-inducing activity. Anticancer agent 300 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma.
    Anticancer agent 300
  • HY-168163
    CDK12/13 ligand 1
    Degrader
    ALK-IN-29 (compound 4c) has a certain inhibitory effect on tyrosine protein kinases ALK, CDK2/CyclinE1 and FAK, among which the strongest inhibitory effect on ALK kinase is 40.63% at a concentration of 10 μM. ALK-IN-29 can be used for anti-cancer research.
    CDK12/13 ligand 1
  • HY-178119
    HER4/HER2-IN-1
    Inhibitor
    HER4/HER2-IN-1 (Compound 4b) is a HER4/HER2 inhibitor. HER4/HER2-IN-1 inhibits the proliferation of HER2-positive cells. HER4/HER2-IN-1 reduces the total expression level of HER2 in A431 cells, while the phosphorylated HER2 (p-HER2) does not decrease. HER4/HER2-IN-1 lowers the level of cell cycle protein D1 (cyclin D1) and stimulates the cleavage of PARP. HER4/HER2-IN-1 can be used for the study of cancer, such as breast cancer.
    HER4/HER2-IN-1
  • HY-151408
    CDK1-IN-4
    Inhibitor
    CDK1-IN-4 (10d) is a selective CDK1 inhibitor with IC50s of 44.52, 624.93 and 135.22 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN4 inhibits the growth of cancer cells by affecting cell cycle. CDK1-IN-4 can be used for the research of cancer.
    CDK1-IN-4
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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