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-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-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
    CDK7-IN-33
    		Inhibitor
    CDK7-IN-33 (Compound 148) is the inhibitor for CDK7 with a Ki of 21.75 nM. CDK7-IN-33 inhibits the proliferation of CDK7 WT expressing A549 with pIC50 of 7.37.
    CDK7-IN-33
  • 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-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
    CDC7 Human Pre-designed siRNA Set A
  • HY-170425
    CDK7-IN-32
    		Inhibitor
    CDK7-IN-32 (compound10) is a CDK7 inhibitor.
    CDK7-IN-32
  • 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
  • HY-170306
    LZ9
    		Inhibitor
    LZ9 is a ATP-competitive CDK1 and CDK2 inhibitor. LZ9 has the potential for the research of colorectal cancer (CRC).
    LZ9
  • 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-146335
    CLK1/4-IN-1
    		Inhibitor
    CLK1/4-IN-1 (compound 31) is a potent and selective Clk1 and Clk4 inhibitor with an IC50 value of 9.7 nM and 6.6 nM, respectively. CLK1/4-IN-1 has growth inhibitory activities against T24 cancer cells with GI50 of 1.1 μM. CLK1/4-IN-1 can be used for researching anticancer.
    CLK1/4-IN-1
  • HY-172970
    HQY1428
    		Inhibitor
    HQY1428 is an orally active CDK12 inhibitor. HQY1428 inhibits DNA replication, causes G2/M arrest in SKOV3 cells, induces DNA double-strand breaks and apoptosis. HQY1428 has anti-tumor activity in the SKOV3 xenograft mouse model. HQY1428 combined with the HER2 inhibitor Lapatinib (HY-50898) in the NCI-N87 xenograft mouse model produces a synergistic therapeutic effect.
    HQY1428
  • HY-149495
    CP-07
    		Degrader
    CP-07 is a potent and selective PROTACCDK9 degrader (DC50: 43 nM). CP-07 inhibits 22RV1 cell proliferation (IC50: 62 nM) and colony formation by down-regulating Mcl-1 and c-Myc. CP-07 inhibits 22RV1 xenograft tumor growth. CP-07 can be used for research of prostate cancer.
    CP-07
  • HY-172146
    CDK4/6-IN-24
    		Inhibitor
    CDK4/6-IN-24 (Compound A) is the inhibitor for CDK4/6. CDK4/6-IN-24 exhibits board-spectrum antitumor activity that inhibits multi cancer cells with IC50 of submicromolar levels.
    CDK4/6-IN-24
  • HY-162670
    Anticancer agent 238
    Anticancer agent 238 (compound 5) is an anticancer agent with a notably strong binding affinity towards the CDK-5 enzyme. Anticancer agent 238 shows a strong efficacy agains HCT116 and MCF7 cells, with IC50 values of 13.46 µM and 16.43 µM, respectively.
    Anticancer agent 238
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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