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-168664
    CPD-39
    Degrader 98.06%
    CPD-39 is a potent and orally active CCND1 and CDK4 heterobifunctional PROTAC degrader. CPD-39 shows anti-proliferation. (Pink: ligand for target protein (HY-50767); black: linker (HY-20240); Blue: E3 ligase ligand (HY-168667)).
    CPD-39
  • HY-P2559
    CDK7/9 tide
    99.92%
    CDK7/9 tide is peptide substrate for CDK7 or CDK9.
    CDK7/9 tide
  • HY-139875
    JH-XVI-178
    Inhibitor 98.87%
    JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC50 values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties.
    JH-XVI-178
  • HY-18313
    S6K1-IN-1
    Inhibitor 99.71%
    S6K1-IN-1 is a selective S6K1 inhibitor with an IC50 value of 52 nM. S6K1-IN-1 can be used in the research of obesity and insulin resistance-related diseases.
    S6K1-IN-1
  • HY-123600
    SRI-29329
    Inhibitor 99.14%
    SRI-29329 is a specific CLK inhibitor, with IC50 values of 78 nM, 16 nM and 86 nM for CLK1, CLK2 and CLK4, respectively.
    SRI-29329
  • HY-15504A
    RGB-286638 free base
    Inhibitor 98.07%
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
    RGB-286638 free base
  • HY-18285
    Longdaysin
    Inhibitor 99.83%
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
    Longdaysin
  • HY-N3389
    Licoisoflavone A
    Inhibitor 99.41%
    Licoisoflavone A is an orally active isoflavone. Licoisoflavone A inhibits proliferation, induces apoptosis, and causes G1/S phase arrest in colorectal cancer (CRC) cells. Licoisoflavone A inhibits the CDK2-Cyclin E1 axis. Licoisoflavone A inhibits lipid peroxidation with an IC50 of 7.2 μM. Licoisoflavone A shows a dose-dependent inhibition effect on SARS-CoV-2 infection. Licoisoflavone A exhibits significant anti-tumor efficacy in mice bearing CT26 cell subcutaneous xenografts. Licoisoflavone A can be used for the study of colorectal cancer and SARS-CoV-2 infection.
    Licoisoflavone A
  • HY-148063
    DB0614
    98.80%
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-I0998
    1,1-Dimethylethyl 4-(5-amino-3-pyridinyl)-1-piperazinecarboxylate
    1,1-Dimethylethyl 4-(5-amino-3-pyridinyl)-1-piperazinecarboxylate is the impurity of Palbociclib (HY-50767). Palbociclib is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively.
    1,1-Dimethylethyl 4-(5-amino-3-pyridinyl)-1-piperazinecarboxylate
  • HY-168555
    YJ1206
    Degrader
    YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker).
    YJ1206
  • HY-126675
    AS2863619 free base
    Inhibitor 99.87%
    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
    AS2863619 free base
  • HY-139254
    Indirubin-3′-oxime
    Inhibitor 99.10%
    Indirubin-3′-oxime (IDR3O), a synthetic derivative of indirubin, is a potent inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Indirubin-3′-oxime directly inhibits the activity of all three isoforms of JNK (JNK1, JNK2, and JNK3), with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM, respectively. Indirubin-3′-oxime can enhance height growth via activation of Wnt/β-catenin signaling in chondrocytes.
    Indirubin-3′-oxime
  • HY-144977
    dCeMM4
    Degrader 99.67%
    dCeMM4 (Compound 5) is a molecular glue degrader. dCeMM4 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.
    dCeMM4
  • HY-153894
    SRX3177
    Inhibitor 99.59%
    SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells.
    SRX3177
  • HY-149262
    CLK1-IN-3
    Inhibitor 98.54%
    CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research.
    CLK1-IN-3
  • HY-126251
    CDK9-IN-7
    Inhibitor 98.05%
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
    CDK9-IN-7
  • HY-112799
    DK419
    Inhibitor 99.86%
    DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.
    DK419
  • HY-137432B
    Avotaciclib hydrochloride
    Inhibitor 99.75%
    Avotaciclib (BEY1107) hydrochloride is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib hydrochloride can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib hydrochloride can be used in the research of cancer such as pancreatic cancer and lung cancer.
    Avotaciclib hydrochloride
  • HY-153260
    TP-1287
    Inhibitor
    TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor.
    TP-1287
Cat. No. Product Name / Synonyms Species Source
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