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-148213
    CDK2/4/6-IN-1
    		Inhibitor
    CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research. CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CDK2/4/6-IN-1
  • HY-172224
    PARP1/CDK12-IN-1
    		Inhibitor
    PARP1/CDK12-IN-1 (107) is a dual inhibitor of CDK12 and PARP1, with IC50 values of 285 nM and 34 nM for CDK12 and PARP1, respectively.
    PARP1/CDK12-IN-1
  • HY-162270
    CDK2-IN-24
    		Inhibitor
    CDK2-IN-24 (compound 3f) is an inhibitor of cyclin-dependent kinase 2 with an elevated binding energy value .
    CDK2-IN-24
  • HY-P1906
    [pThr3]-CDK5 Substrate
    [pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM.
    [pThr3]-CDK5 Substrate
  • HY-153950
    CDK7-IN-22
    		Inhibitor
    CDK7-IN-22 (compound 101) is an CDK7 inhibitor with antitumor activity. CDK7-IN-22 shows selectivity on CDK7.
    CDK7-IN-22
  • HY-168209
    LBM22
    		Inhibitor
    LBM22 is a CDC2-like kinase 2 (CLK2) inhibitor with the IC50 of 3.9 nM. LBM22 has antiproliferative activity and inhibits serine/arginine-rich (SR) protein phosphorylation. LBM22 down-regulates the expression of Wnt-related proteins and anti-apoptotic proteins and can be used for study of non-small cell lung cancer.
    LBM22
  • HY-147598
    CDK7-IN-14
    		Inhibitor
    CDK7-IN-14 is a potent inhibitor of CDK7. CDK7-IN-14 is a pyrimidinyl derivative compound. CDK7-IN-14 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 3).
    CDK7-IN-14
  • HY-RS02358
    Cdk12 Rat Pre-designed siRNA Set A
    		Inhibitor

    Cdk12 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk12 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cdk12 Rat Pre-designed siRNA Set A
  • HY-161595
    CDK5-IN-4
    		Inhibitor
    CDK5-IN-4 (compound 4) is a potent multikinase type-II inhibitor targeting CDK5, with an IC50 of 9.8 μM. CDK5-IN-4 also inhibits GSK-3α, GSK-3β, CDK9, and CDK2, with IC50 values of 0.98, 4.00, 1.76, and 6.24 μM, respectively. CDK5-IN-4 can be used for glioblastoma research.
    CDK5-IN-4
  • HY-169557
    CDKI-IN-1
    		Inhibitor
    CDKI-IN-1 (Compound SNX12) is a cyclin-dependent kinase inhibitor (CDKI) inhibitor that can be used for research into degenerative diseases of the central nervous system.
    CDKI-IN-1
  • HY-167237
    Calactin
    		Inhibitor
    Calactin is a glycoside that can be isolated from Asclepias curassavica L.. Calactin activates caspase-3, caspase-8, caspase-9, and phosphorylates ERK. Calactin induces DNA damage, apoptosis, PARP cleavage, G2/M phase cell cycle arrest, shifts Bax/Bcl-2 expression, and shows anti-proliferation effects in leukemia cells. Calactin can be used for the research of leukemia.
    Calactin
  • HY-176451
    CDK9 degrader-1
    		Degrader
    CDK9 degrader-1 (Compound AZ-9) is a selective CDK9 degrader (DC50: 0.4073 µM). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuses with lysosomes to degrade CDK9 and its partner protein Cyclin T1 (DC50: 1.215 µM). CDK9 degrader-1 induces caspase 3-mediated apoptosis. CDK9 degrader-1 has antitumor activity in a mouse HCT116 xenograft model.
    CDK9 degrader-1
  • HY-112280A
    Crozbaciclib fumarate
    		Inhibitor 99.37%
    Crozbaciclib fumarate is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.
    Crozbaciclib fumarate
  • HY-177501
    Otviciclib
    		Inhibitor
    Otviciclib (Compound 86) is a CDK inhibitor. Otviciclib has potent anti-proliferative activity against solid tumor cells (such as HCT116, NCIH82 and DU145 cells) with no significant toxicity to normal cells, and effectively induces the G2/M phase cells arrest and apoptosis. Otviciclib has a broad-spectrum anticancer activity, such as colon, pancreatic and lung cancer.
    Otviciclib
  • HY-E70681
    CDK4/CycD1 Recombinant Human Active Protein Kinase
    CDK4 has a well-established role in cell-cycle controland CDK4-cyclin complexes are commonly deregulated in tumorigenesis. CDK4/CycD1 Recombinant Human Active Protein Kinase is an ortholog of CDK4.
    CDK4/CycD1 Recombinant Human Active Protein Kinase
  • HY-N0589S
    Dehydrodiisoeugenol-d4
    		Modulator
    Dehydrodiisoeugenol-d4 is the deuterium labeled Dehydrodiisoeugenol (HY-N0589). Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.
    Dehydrodiisoeugenol-d<sub>4</sub>
  • HY-129694
    Lenoremycin
    		Inhibitor
    Lenoremycin (Ro 21-6150) is a microbial metabolite. Lenoremycin decreases β-catenin and cyclin D1 proteins levels. Lenoremycin decreases cancer stem cells (CSCs) populations via inducing reactive oxygen species production.
    Lenoremycin
  • HY-155153
    CDK9-IN-24
    		Inhibitor
    CDK9-IN-24 (compound 21a) is a highly selective CDK9 inhibitor with significant inhibitory effect on tumor growth. CDK9-IN-24 effectively blocks cell proliferation and induces apoptosis by downregulating Mcl-1 and c-Myc, and can be used in acute myeloid leukemia research.
    CDK9-IN-24
  • HY-121081A
    BAY-1112054 hydrochloride
    		Inhibitor
    BAY-1112054 (BAY-958) hydrochloride is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-1112054 hydrochloride shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-1112054 hydrochloride exhibits good metabolic stability. BAY-1112054 hydrochloride effectively inhibits tumor growth in mouse xenograft models without significant toxicity.
    BAY-1112054 hydrochloride
  • HY-114178
    CDK8-IN-2
    		Inhibitor
    CDK8-IN-2 is an orally active CDK8 inhibitor of an IC50 values of 0.010 μM. CDK8-IN-2 shows a CDK19 IC50 value of 0.026 μM. CDK8-IN-2 inhibits phospho-STAT1, a pharmacodynamic biomarker of CDK8. CDK8-IN-2 inhibits WNT pathway activity. CDK8-IN-2 can be used for the research of colorectal carcinoma.
    CDK8-IN-2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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