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

CDK

Cyclin dependent kinase

CDK

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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-183118
    CID-078
    		Inhibitor
    CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR+/HER2- breast cancer, RB1-altered solid tumors, and neuroblastoma.
    CID-078
  • HY-101257A
    CDK7-IN-1
    		Inhibitor 98.91%
    CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependent kinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215.
    CDK7-IN-1
  • HY-201330
    GDC-4198
    		Inhibitor
    GDC-4198 (RGT-419B) is an orally active CDK4/2 inhibitor with desired degrees of selectivity against kinases such as CDK6, CDK9 and GSK3β. GDC-4198 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. GDC-4198 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer.
    GDC-4198
  • HY-143430A
    (S)-LY3177833 hydrate
    		Inhibitor
    (S)-LY3177833 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. (S)-LY3177833 hydrate shows broad in vitro anticancer activity.
    (S)-LY3177833 hydrate
  • HY-139011
    IV-361
    		Inhibitor 99.60%
    IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1).
    IV-361
  • HY-100023A
    LY3177833 monhydrate
    		Inhibitor 99.76%
    LY3177833 (Example 4) monhydrate is an orally active CDC7 and pMCM2 inhibitor with IC50 values of 3.3 nM and 290 nM, respectively. LY3177833 monhydrate is a senescence inducer.
    LY3177833 monhydrate
  • HY-130517
    Cdc7-IN-5
    		Inhibitor
    Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
    Cdc7-IN-5
  • HY-112243A
    Cimpuciclib tosylate
    		Inhibitor 99.65%
    Cimpuciclib tosylate is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity.
    Cimpuciclib tosylate
  • HY-112418
    CDK4/6-IN-18
    		Inhibitor 98.9%
    CDK4/6-IN-18 (Example 2BrIC) is a selective CDK4/6 inhibitor. CDK4/6-IN-18 inhibits ionizing radiation (IR)-induced DNA damage in cells.
    CDK4/6-IN-18
  • HY-168620
    CDK6-IN-1
    		Inhibitor 98.77%
    CDK6-IN-1 (compound 4i) is a CDK6 inhibitor. CDK6-IN-1 inhibits cell growth and induces cell cycle arrest at G1-phase.
    CDK6-IN-1
  • HY-178227
    KY19334
    		Inhibitor
    KY19334 is a CXXC5-DVL inhibitor. KY19334 can activate the Wnt/β-catenin pathway by inhibiting CXXC5-Dvl interaction. KY19334 can inhibit cancer cells proliferation, migration, invasion and transformation by inhibiting CDK1. KY19334 can accelerate wound healing and exert regenerative effects. KY19334 can be used for the researches of cancer, inflammation, metabolic and neurological disease, such as cutaneous squamous cell carcinoma and diabetes.
    KY19334
  • HY-147125
    DDO-6600
    		Inhibitor 99.2%
    DDO-6600 is a covalent Hsp90 inhibitor. DDO-6600 disrupts the interaction between Hsp90 and its co-chaperone protein Cdc37, thereby inducing the degradation of kinase client proteins (such as AKT, CDK4, c-Raf). DDO-6600 has inhibitory activity against various cancer cells. DDO-6600 inhibits the migration and invasion of HCT-116 cells, and induces cell cycle arrest and apoptosis. DDO-6600 significantly inhibits tumor growth in the HCT-116 xenograft tumor model. DDO-6600 can be used for research on colorectal cancer.
    DDO-6600
  • HY-100035
    PT-262
    		Inhibitor 99.21%
    PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity.
    PT-262
  • HY-RS02309
    CDC7 Human Pre-designed siRNA Set A
    		Inhibitor

    CDC7 Human Pre-designed siRNA Set A contains three designed siRNAs for CDC7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CDC7 Human Pre-designed siRNA Set A
  • HY-402805
    DYRK2-IN-2
    		Inhibitor
    DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2, with its IC50 value being 40.3 nM. The inhibitory activity of DYRK2-IN-2 on DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM), and CLKs (IC50 = 540-6496 NM) is relatively low. DYRK2-IN-2 inhibits the phosphorylation of Tau protein at Thr212 and shows moderate cytotoxicity in HT22 cells. DYRK2-IN-2 can be used in cancer research.
    DYRK2-IN-2
  • HY-176444B
    (S)-CDK2 degrader 6
    		Degrader 99.69%
    (S)-CDK2 degrader 6 (Compound 8) is the S-enantiomer of CDK2 degrader 6 (HY-176444). (S)-CDK2 degrader 6 is a selective CDK2 molecular glue degrader with a DC50 of 166.7 nM in 24 h. (S)-CDK2 degrader 6 can be used for breast cancer research.
    (S)-CDK2 degrader 6
  • HY-171787
    PPA-037
    		Inhibitor
    PPA-037 is an orally active, highly potent and selective inhibitor of cyclin-dependent kinase 12 (CDK12). PPA-037 induces the degradation of cyclin K (Cyclin K), enhancing antiproliferative effects on tumor cells. PPA-037 is promising for research of cancers.
    PPA-037
  • HY-P1109
    [Ala92]-p16 (84-103)
    		Inhibitor 98.16%
    [Ala92]-p16 (84-103) is a peptide derived from the p16CDKN2/INK4a (p16) tumor suppressor protein. [Ala92]-p16 (84-103) binds to both cdk4 and cdk6 and inhibits cdk4-cyclin D1 kinase activity in vitro (IC50: 1.5 μM). [Ala92]-p16 (84-103) blocks cell cycle progression through the G1 phase.
    [Ala92]-p16 (84-103)
  • HY-B0402S1
    Amantadine-d6
    		98.10%
    Amantadine-d6 is the deuterium labeled Amantadine. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
    Amantadine-d<sub>6</sub>
  • HY-RS02398
    CDK8 Human Pre-designed siRNA Set A
    		Inhibitor

    CDK8 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK8 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CDK8 Human Pre-designed siRNA Set A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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