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

CDK

Cyclin dependent kinase

CDK

Related Products

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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-156114
    EGFR/CDK2-IN-2
    		Inhibitor
    EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor of EGFR and CDK-2 with IC50s of 19.6 and 87.9 nM, respectively. EGFR/CDK2-IN-2 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-2 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 0.39 μM.
    EGFR/CDK2-IN-2
  • HY-156444
    HDAC1/CDK7-IN-1
    		Inhibitor
    HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells.
    HDAC1/CDK7-IN-1
  • HY-162007
    PYRA-2
    		Inhibitor
    PYRA-2 is a CDC7 kinase inhibitor with potential for cancer research.
    PYRA-2
  • HY-161776
    P-gp/CDK2-IN-1
    		Inhibitor
    P-gp/CDK2-IN-1 (Compound 4j) is an inhibitor for is inhibitor for P-glycoprotein (P-gp) and for cyclin-dependent kinase-2 (CDK2). P-gp/CDK2-IN-1 inhibits the proliferation of cancer cells SW-480 and MCF-7 wit IC50 of 38.6 μM and 26.6 μM. P-gp/CDK2-IN-1 exhibits antioxidant efficacy with EC50 of 580 μM in DPPH experiment.
    P-gp/CDK2-IN-1
  • HY-169412
    MAPK-IN-3
    		Inhibitor
    MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK.
    MAPK-IN-3
  • HY-E70689
    CDK7/CycH/MAT1 Recombinant Human Active Protein Kinase
    CDK7/CycH/MAT1 Recombinant Human Active Protein Kinase acts as a cyclin-dependent kinase activating kinase. CDK7 exists in several forms including a core tri-partite CDK7/CycH/MAT1 complex known as CAK (cyclin-dependent kinase activating kinase), as a component in the general transcription factor TFIIH and as a component of larger complexes containing pol II and other transcription factors.
    CDK7/CycH/MAT1 Recombinant Human Active Protein Kinase
  • HY-130133
    DHW-221
    		Inhibitor
    DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research[1][2][3].
    DHW-221
  • HY-143257
    CDK4/6-IN-7
    		Inhibitor
    CDK4/6-IN-7 is a potent, selective and orally active CDK4/6 inhibitor, with IC50s of 1.58 and 4.09 nM, respectively. CDK4/6-IN-7 can be used for the research of breast cancer.
    CDK4/6-IN-7
  • HY-149407
    Multi-kinase-IN-4
    		Inhibitor
    Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
    Multi-kinase-IN-4
  • HY-172194
    JNJ-3738
    		Inhibitor
    JNJ-3738 (Compound 148) is the inhibitor for CDK7 with a Ki of 21.75 nM. JNJ-3738 inhibits the proliferation of CDK7 WT expressing A549 with pIC50 of 7.37.
    JNJ-3738
  • HY-E70667
    CDK18/CycY Recombinant Human Active Protein Kinase
    CDK18 is a neuronal kinase that phosphorylates TAU protein when overexpressed in human brain. CDK18 shares a conserved PCTAIRE amino acid sequence in the helical α-C region of the kinase N-lobe. CDK18/CycY Recombinant Human Active Protein Kinase is an ortholog of CDK18.
    CDK18/CycY Recombinant Human Active Protein Kinase
  • HY-E70655
    CDK1/CycE2 Recombinant Human Active Protein Kinase
    CDK1 is a cyclin-dependent kinase that functions as a serine/threonine protein kinase, and is a key player in cell cycle regulation. CDK1/CycE2 Recombinant Human Active Protein Kinase is an ortholog of CDK1.
    CDK1/CycE2 Recombinant Human Active Protein Kinase
  • HY-143429
    Cdc7-IN-15
    		Inhibitor
    Cdc7-IN-15 (Example 108) is a cdc7 kinase inhibitor. Cdc7-IN-15 can be used for cancer research.
    Cdc7-IN-15
  • HY-172234
    PF-06842874
    		Inhibitor
    PF-06842874 is a CDK4/Cyclin D1 and CDK6/Cyclin D3 inhibitor (Ki values are 62 and 130 nM, respectively). PF-06842874 can be used in the research of pulmonary arterial hypertension and cancer.
    PF-06842874
  • HY-123034
    CDKI-83
    		Inhibitor
    CDKI-83 is a potent CDK9 and CDK1 inhibitor with Ki values of 21 nM and 72 nM for CDK9/T1 and CDK1/B, respectively. CDKI-83 demonstrates effective anti-proliferative activity in human tumour cell lines with a GI50<1 μM. CDKI-83 effectively induces apoptosis in A2780 human ovarian cancer cells. CDKI-83 reduces phosphorylation at Ser-2 of RNA polymerase II (RNAPII) by inhibiting cellular CDK9 activity, and down-regulates Mcl-1 and Bcl-2. CDKI-83 has the potential for anti-cancer research.
    CDKI-83
  • HY-112363
    Aloisine A
    		Inhibitor
    Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.
    Aloisine A
  • HY-170425
    CDK7-IN-32
    		Inhibitor
    CDK7-IN-32 (compound10) is a CDK7 inhibitor.
    CDK7-IN-32
  • 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-156083
    CDK9-IN-28
    		Inhibitor
    PROTAC CDK9/CycT1 Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1 Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1 Degrader-1 shows strong anti-proliferative activity in solid tumors.
    CDK9-IN-28
  • HY-149261
    H1k
    		Inhibitor
    H1k, a Eudistomin Y derivative, is a lysosome-targeted antiproliferation agent. H1k increases the autophagy signal and downregulate the expression of cyclin-dependent kinase (CDK1) and cyclin B1. H1k can be used in research of cancer.
    H1k
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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