1. シグナル伝達
  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).

製品番号 製品名 製品効果 純度 構造式
  • HY-E70670
    CDK2/CycA2 Recombinant Human Active Protein Kinase
    CDK2 is a cyclin-dependent kinase involved in the control of the cell cycle. CDK2/CycA2 Recombinant Human Active Protein Kinase is an ortholog of CDK2.
    CDK2/CycA2 Recombinant Human Active Protein Kinase
  • HY-181036
    CDK12/13 ligand 3 Ligand
    CDK12/13 ligand 3 is a CDK12/13 PROTAC ligand. CDK12/13 ligand 3 can be conjugated with E3 ligase ligand (HY-W093272) and linker to synthesize CDK12/13 PROTAC degrader DN1679 (HY-181035). CDK12/13 ligand 3 can be used for cancer research.
    CDK12/13 ligand 3
  • HY-156116
    EGFR/CDK2-IN-4 Inhibitor
    EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC50s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 2.74 μM.
    EGFR/CDK2-IN-4
  • HY-175013
    CDK6/9-IN-2 Inhibitor
    CDK6/9-IN-2 is a highly active dual inhibitor of CDK6 (IC50 = 15 nM) and CDK9 (IC50 = 22 nM). CDK6/9-IN-2 is selective for CDK2, CDK8, and CDK11. CDK6/9-IN-2 inhibits the proliferation of HaCaT cells induced by IFN-γ/TNF-α and suppresses the STAT3 pathway and the expression of inflammatory factors. CDK6/9-IN-2 can alleviate psoriatic dermatitis and is useful in psoriasis research.
    CDK6/9-IN-2
  • HY-103248R
    Toyocamycin (Standard) Inhibitor
    DL-Aspartic acid (Standard) is the analytical standard of DL-Aspartic acid. This product is intended for research and analytical applications. DL-Aspartic acid (DL-Asp-OH) is a kind of biological materials or organic compounds that are widely used in life science research.
    Toyocamycin (Standard)
  • HY-151463A
    CDK8-IN-11 hydrochloride Inhibitor
    CDK8-IN-11 hydrochloride is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 hydrochloride inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 hydrochloride can be used in the research of colon cancer.
    CDK8-IN-11 hydrochloride
  • HY-130676
    CLK-IN-T3N
    CLK-IN-T3N, the negative control of CLK-IN-T3 (HY-115470), is a chemical probe for CDC-like kinase (CLK).
    CLK-IN-T3N
  • HY-182986
    LS-Q2 Inhibitor
    LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.
    LS-Q2
  • HY-179052
    Apoptosis inducer 50 Inhibitor
    Apoptosis inducer 50 (Compound 5e) is an apoptosis inducer as well as an autophagy inducer agent. Apoptosis inducer 50 exhibits potent and selective anti-cancer activity against triple-negative breast cancer cells and metastatic colon cancer cells. Apoptosis inducer 50 upregulates the expression of pro-apoptotic proteins (Bax, Bim, cleaved Caspase-9) and downregulates the expression of the anti-apoptotic protein (BCL-XL). Apoptosis inducer 50 upregulates key autophagy markers such as Beclin-1 and ATG5, and enhances the conversion of LC3-I to LC3-II., Apoptosis inducer 50 arrests cancer cells in the G1/S phase by upregulating the expression of p21 and p27 while downregulating Cyclin D1. Apoptosis inducer 50 increases the level of ROS.
    Apoptosis inducer 50
  • HY-175531
    EGFR-IN-169 Inhibitor
    EGFR-IN-169 is an epidermal growth factor (EGFR) (IC50 = 5.19 μM) inhibitor form panaxadiol. EGFR-IN-169 interferes with the migration and growth of colorectal cancer cells by inhibiting EGFR-mediated RalA/EMT pathway. EGFR-IN-169 shows an IC50 value of 4.46 μM and SI of 16.92 for HCT-116 cells. EGFR-IN-169 inhibits CDKs activity, induces G0/G1 cycle arrest and inhibits migration and invasion. EGFR-IN-169 reduces mitochondrial membrane potential and induces apoptosis and ROS production. EGFR-IN-169 can be used for the research of cancer, such as colorectal cancer.
    EGFR-IN-169
  • HY-P3731
    Cdk2/Cyclin Inhibitory Peptide II Inhibitor
    Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner.
    Cdk2/Cyclin Inhibitory Peptide II
  • HY-172872
    CDK2-IN-45 Inhibitor
    CDK2-IN-45 (Compound 8f) is a CDK2 inhibitor (IC50: 0.64 μM). CDK2-IN-45 inhibits the proliferation of DU-145 and PC-3 cell lines with IC50 of 2.20 μM and 4.17 μM, respectively. CDK2-IN-45 induces G0/G1 cell cycle arrest and apoptosis. CDK2-IN-45 can be used in prostate cancer research.
    CDK2-IN-45
  • HY-176189
    CDK1-IN-7 Inhibitor
    CDK1-IN-7 (compound M7) is a potent CDK1 inhibitor. CDK1-IN-7 inhibits the proliferation and migration of HCT116 and Lovo cells. CDK1-IN-7 can be used in the study of colorectal cancer.
    CDK1-IN-7
  • HY-146586
    Haspin-IN-1 Inhibitor
    Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC50 of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 221 nM and 916.3 nM, respectively.
    Haspin-IN-1
  • HY-177957
    CDK2-IN-52 Inhibitor
    CDK2-IN-52 (Compound Cpb No 39) is a selective cyclin-dependent kinase 2 (CDK2) inhibitor with a DC50 value of 1-10 nM. CDK2-IN-52 induces cell cycle arrest and suppresses tumor cell proliferation. CDK2-IN-52 is promising for research of CDK2-overexpressing malignancies such as breast and ovarian cancers.
    CDK2-IN-52
  • HY-151580
    CDK2-IN-14 Inhibitor
    CDK2-IN-14 (compound 4f) is a highly selective CDK2 inhibitor. CDK2-IN-14 can be used in research of cancer.
    CDK2-IN-14
  • HY-16366A
    Briciclib sodium Inhibitor
    Briciclib (ON 014185) sodium is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib sodium exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib sodium reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib sodium can be used for the study of hematological system tumors and solid tumors.
    Briciclib sodium
  • HY-162398
    LQ23 Inhibitor
    LQ23 is a selective inhibitor for CDC2-like kinase 2 (CLK2) with an IC50 of 1.4 nM. LQ23 exhibits anti-inflammatory activity.
    LQ23
  • HY-115993
    CDK4/6-IN-10 Inhibitor
    CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM).
    CDK4/6-IN-10
  • HY-P1933A
    [pSer2, pSer5, pSer7]-CTD TFA
    [pSer2, pSer5, pSer7]-CTD (TFA), a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNA polymerase II carboxy-terminal domain (CTD).
    [pSer2, pSer5, pSer7]-CTD TFA
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