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-18969
    LDC3140
    Inhibitor
    LDC3140 is a selective CDK7 inhibitor (IC50<5 nM). By inhibiting the activity of CDK7, LDC3140 affects the regulation of the cell cycle, leading to cell cycle arrest and thus inhibiting the proliferation of tumor cells. LDC3140 can be used in the research of cancer treatment.
    LDC3140
  • HY-112336
    Aloisine RP106
    Inhibitor
    Aloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC50s of 0.70µM, 1.5µM, 0.92 µM, respectively.
    Aloisine RP106
  • HY-N12218
    Roccellic acid
    Roccellic acid is a methanol extract of Roccella montagnei with cytotoxicity with an IC50 value of 71.26 μg/ml.
    Roccellic acid
  • HY-111932
    Indirubin-5-sulfonate
    Inhibitor
    Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.
    Indirubin-5-sulfonate
  • HY-149962
    PROTAC CDK9 degrader-5
    Inhibitor
    PROTAC CDK9 degrader-5 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-5 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-5 degrades CDK9 with DC50s of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively.
    PROTAC CDK9 degrader-5
  • HY-RS02366
    CDK16 Human Pre-designed siRNA Set A
    Inhibitor

    CDK16 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK16 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    CDK16 Human Pre-designed siRNA Set A
    CDK16 Human Pre-designed siRNA Set A
  • HY-RS02392
    CDK6 Human Pre-designed siRNA Set A
    Inhibitor

    CDK6 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    CDK6 Human Pre-designed siRNA Set A
    CDK6 Human Pre-designed siRNA Set A
  • HY-173147
    CDK2-IN-42
    Inhibitor
    CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 value of 10 nM. CDK2-IN-42 has anti-ESCC (Esophageal Squamous Cell Carcinoma) cell activity. It can block transcriptional elongation, downregulate the core genes in the G1 phase to induce cell cycle arrest, and alter the CDK12-ATM/ATR-CHEK1/CHEK2 signaling axis, resulting in DNA damage. CDK2-IN-42 can effectively inhibit tumor growth in a xenograft mouse model of human ESCC KYSE150. CDK2-IN-42 holds great promise for research in the field of cancer.
    CDK2-IN-42
  • HY-153704
    CDK4/6-IN-17
    Inhibitor
    CDK4/6-IN-17 (compound 12) is an orally active CDK4/6 inhibitor with IC50 ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model.
    CDK4/6-IN-17
  • HY-162529
    CDK4/6-IN-19
    Inhibitor
    CDK4/6-IN-19 (Compound II-7) is a CDK4/CDK6 inhibitor with IC50 values ​​of 0.2, 5.0 nM, respectively. CDK4/6-IN-19 also inhibits cell proliferation and can be used in cancer research.
    CDK4/6-IN-19
  • HY-19471
    (rac)-ZK-304709
    Inhibitor
    (rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET.
    (rac)-ZK-304709
  • HY-148651
    CDK2-IN-15
    Inhibitor
    CDK2-IN-15 (Compound 19) is an inhibitor of CDK2 with an IC50 of 2.9 μM. CDK2-IN-15 can be used for cancer research.
    CDK2-IN-15
  • HY-173523
    KI-CDK9d-32
    Degrader
    KI-CDK9d-32 is a CDK9 PROTAC degrader (DC50: 0.89 nM). KI-CDK9d-32 promotes the ubiquitination and degradation of CDK9. KI-CDK9d-32 inhibits the MYC pathway and disrupts nucleolar homeostasis. KI-CDK9d-32 has anticancer activity. (Pink: CDK9 ligand (HY-153718); Blue: E3 ligase CRBN ligand (HY-163233); Black: Linker (HY-W011657); E3 ligase CRBN ligand-linker conjugate (HY-173525)).
    KI-CDK9d-32
  • HY-RS02399
    Cdk8 Mouse Pre-designed siRNA Set A
    Inhibitor

    Cdk8 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk8 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Cdk8 Mouse Pre-designed siRNA Set A
    Cdk8 Mouse Pre-designed siRNA Set A
  • HY-103019E
    Enitociclib
    Inhibitor
    Enitociclib (BAY-1251152; VIP152) is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies.
    Enitociclib
  • HY-145402
    CDK7-IN-7
    Inhibitor
    CDK7-IN-7 is a potent and selective CDK7 kinase inhibitor with an IC50 of <50 nM (Patent CN112661745A, compound T-01).
    CDK7-IN-7
  • HY-149436
    CDK2/Bcl2-IN-1
    Inhibitor
    CDK2/Bcl2-IN-1 (compound 1), a saponin and a CDK-2 inhibitor (IC50=117.6 nM) with promising cytotoxicity against cancer cells. CDK2/Bcl2-IN-1 also inhibits Bcl-2, and induces apoptosis in A549 lung cancer cells.
    CDK2/Bcl2-IN-1
  • HY-164906
    TMX-2138
    Degrader
    TMX-2138 is a CDKs PROTAC degrader, with IC50s of 8.7 nM, 10.9 nM, 7.0 nM and 25.7 nM for CDK1/cyclinB, CDK2/cyclinA, CDK5/p25 and CDK9/cyclinT1, respectively. TMX-2138 promotes ubiquitination and degradation of CDKs. TMX-2138 can be used for the research of ovarian cancer (Pink: CDKs ligand (HY-151071); Blue: E3 ligase CRBN ligand (HY-14658); Black: linker (HY-W008352)).
    TMX-2138
  • HY-162600
    CDK8-IN-15
    Inhibitor
    CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases.
    CDK8-IN-15
  • HY-173273
    YJZ5118
    Inhibitor
    YJZ5118 is a CDK12/13 inhibitor with IC50 values of 39.5 nM and 26.4 nM against CDK12 and CDK13, respectively. By inducing DNA damage and Apoptosis, YJZ5118 effectively suppresses tumor cell proliferation and exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for research in the field of cancer.
    YJZ5118
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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