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-100429
    CAN508
    Inhibitor 99.59%
    CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
    CAN508
  • HY-45661
    Inixaciclib
    Inhibitor 99.93%
    Inixaciclib is a potent CDK inhibitor, can be used to research anticancer.
    Inixaciclib
  • HY-150023
    BI-1622
    Inhibitor 98.97%
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
    BI-1622
  • HY-12422A
    Voruciclib hydrochloride
    Inhibitor 99.23%
    Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
    Voruciclib hydrochloride
  • HY-50940A
    AT7519 TFA
    Inhibitor
    AT7519 (AT7519M) TFA as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
    AT7519 TFA
  • 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-168683
    CDK8 ligand 1
    Degrader 98.0%
    CDK8 ligand 1 is the ligand of CDK8. CDK8 ligand 1 can be used to synthesize LL-K8-22 (HY-149209).
    CDK8 ligand 1
  • HY-176165
    CDK9/EZH2-IN-1
    Inhibitor
    CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC50: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC50 values are 136.3, 171.3 and 315.7 nM, respectively).
    CDK9/EZH2-IN-1
  • HY-146213
    CDK4/6-IN-12
    Inhibitor 99.76%
    CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer.
    CDK4/6-IN-12
  • HY-168673
    CDK1-IN-6
    Inhibitor 99.96%
    CDK1-IN-6 (Ligand 3) is a potent CDK1 inhibitor. CDK1-IN-6 has the potential for the research of cancer.
    CDK1-IN-6
  • HY-156084
    LL-K9-3
    Degrader 99.2%
    LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs.
    LL-K9-3
  • HY-103381
    NSC693868
    Inhibitor 99.0%
    NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC50s of 600 nM and 400 nM, respectively. NSC693868 less potently inhibits GSK3β with an IC50 of 1 µM) and does not block CDC25 activity. NSC693868 is used to help define the roles of CDK1 and CDK5 in various signaling pathways.
    NSC693868
  • HY-103380
    NSC 625987
    Inhibitor 98.01%
    NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2.
    NSC 625987
  • HY-130514
    SMAPP1
    98.92%
    SMAPP1 is an activator of protein phosphatase-1 (PP1). SMAPP1 increases phosphorylation of CDK9’s Ser90 and Thr186 residues, but not Ser175. SMAPP1 induces HIV-1 replication, upregulates HIV-1 transcription that led to the reactivation of latent HIV-1 provirus.
    SMAPP1
  • HY-149964
    PROTAC CDK9 degrader-7
    Inhibitor 99.62%
    PROTAC CDK9 degrader-7 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-7 mediates CDK9 degradation via the proteasome.
    PROTAC CDK9 degrader-7
  • HY-116871
    YKL-1-116
    Inhibitor 98.67%
    YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7WT and Cdk7as, although Cdk7as is relatively resistant to this compound as well.
    YKL-1-116
  • HY-W478102
    CDK2-IN-13
    Inhibitor 98.20%
    CDK2-IN-13 (Compound 15) is a CDK2 inhibitor with an IC50 of 12 µM. CDK2-IN-13 can be used in research of cancer.
    CDK2-IN-13
  • HY-160501
    DS17
    Degrader 98.81%
    DS17 is a molecular glue that acts as a potent degrader of cyclin K, with an EC50 of 13 nM. DS17 plays an important role in cancer research.
    DS17
  • HY-113825
    CLK1/2-IN-1
    Inhibitor 99.87%
    CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 16 nM and 45 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities[1].
    CLK1/2-IN-1
  • HY-115992
    CDK4/6-IN-9
    Inhibitor 99.46%
    CDK4/6-IN-9 (compound 10) is a selective CDK4/6 inhibitor with an IC50 of 905 nM for CDK6/cyclin D1. CDK4/6-IN-9 has the potential for multiple myeloma (MM) research.
    CDK4/6-IN-9
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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