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-161168
    Cyclin K degrader 1
    Degrader 99.86%
    Cyclin K degrader 1 (compound 40) is an AT7519 (HY-50940) based Cyclin K degrader with DC50 of 21 nM. Cyclin K degrader 1 has an affinity for cyclin K that is ~500-fold higher than its affinity for CDK12.
    Cyclin K degrader 1
  • HY-139328
    CDK12-IN-5
    Inhibitor 99.01%
    CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1).
    CDK12-IN-5
  • HY-19988
    THZ1-R
    Inhibitor 98.06%
    THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.
    THZ1-R
  • HY-14620A
    Farnesene (mixture of isomers)
    98.01%
    Farnesene (mixture of isomers) is a farnesene with mixture of isomers. Farnesene is a herbivore-induced plant volatile (HIPV). Farnesene has an important effect on insect resistance in many plant species.
    Farnesene (mixture of isomers)
  • HY-103646
    CK7
    Inhibitor 99.72%
    CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.
    CK7
  • HY-N9561
    Vanicoside B
    Inhibitor 99.82%
    Vanicoside B is a phenylpropanoyl sucrose derivative, can be isolated from the herb Persicaria dissitiflora. Vanicoside B targets cyclin-dependent kinase 8 (CDK8) and exhibits anti-tumor activity. The potential mechanism is Vanicoside B blocks CDK8-mediated signaling pathways and decreases the expression of epithelial-mesenchymal transition proteins, so that it leads to cell cycle arrest and apoptosis.
    Vanicoside B
  • HY-N7045
    Isosilybin B
    Inhibitor 99.32%
    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
  • HY-163640
    CDK4 degrader 1
    Degrader 99.50%
    CDK4 degrader 1 (ML 1–71) is a molecular glue degrader that targets CDK4.
    CDK4 degrader 1
  • HY-101042
    AG-494
    Inhibitor 98.69%
    AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
    AG-494
  • HY-148365
    NecroIr1
    Inhibitor 98.02%
    NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK4 expression.
    NecroIr1
  • HY-128867
    bio-THZ1
    Inhibitor 98.06%
    bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM.
    bio-THZ1
  • HY-162565
    CDD-2807
    Inhibitor 99.52%
    CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC50 of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive.
    CDD-2807
  • HY-46568
    CDK7/12-IN-1
    Inhibitor 99.66%
    CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth.
    CDK7/12-IN-1
  • HY-P10440
    Cdk5i peptide
    Inhibitor 99.83%
    Cdk5i peptide is a CDK5 inhibitory peptide with high binding affinity for Cdk5/p25 (Kd of 0.17 μM), which can block the interaction between CDK5 and p25 and reduce the kinase activity of CDK5/p25. Cdk5i peptide can be used in the stud y of neurodegenerative diseases.
    Cdk5i peptide
  • HY-15777S1
    Ribociclib-d8
    99.23%
    Ribociclib-d8 is the deuterium labeled Ribociclib. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
    Ribociclib-d<sub>8</sub>
  • HY-159805
    CDK2-IN-31
    Inhibitor 98.22%
    CDK2-IN-31 (compound I-125A) is a CDK2 inhibitor. CDK2-IN-31 can be used in cancer research.
    CDK2-IN-31
  • HY-112822
    ON-013100
    Inhibitor 99.66%
    ON-013100, an antineoplastic agent, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
    ON-013100
  • HY-115714
    CDK9-IN-12
    Inhibitor 99.65%
    CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.
    CDK9-IN-12
  • HY-112272
    Lerociclib
    Inhibitor 98.35%
    Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
    Lerociclib
  • HY-168518
    PROTAC CDK9 degrader-9
    Degrader 99.25%
    PROTAC CDK9 degrader-9 (compound 29) is a highly selective and efficient CDK9 degrader based on PROTAC technology. PROTAC CDK9 degrader-9 can be used in anti-cancer research.
    PROTAC CDK9 degrader-9
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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