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-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-12293
    LY2857785
    Inhibitor 99.21%
    LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
    LY2857785
  • HY-144976
    dCeMM3
    98.19%
    dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.
    dCeMM3
  • HY-162255
    CDK2-IN-23
    Inhibitor 99.29%
    CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC50 = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer.
    CDK2-IN-23
  • HY-12653
    LDC4297
    Inhibitor 99.74%
    LDC4297 is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 value of 0.02-1.21 μM. LDC4297 can be used for the research of infection.
    LDC4297
  • HY-136250A
    BSJ-03-204 triTFA
    Inhibitor 99.87%
    BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 triTFA is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and has anti-cancer activity.
    BSJ-03-204 triTFA
  • HY-124639
    CDK9 inhibitor HH1
    Inhibitor 99.69%
    CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor. CDK9 inhibitor HH1 inhibits the transcription of CDK. CDK9 inhibitor HH1 can be used in research of cancer.
    CDK9 inhibitor HH1
  • HY-151071
    TMX-3013
    Inhibitor 98.02%
    TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs).
    TMX-3013
  • HY-P2559
    CDK7/9 tide
    99.92%
    CDK7/9 tide is peptide substrate for CDK7 or CDK9.
    CDK7/9 tide
  • HY-120497
    PKCζ-IN-1
    Inhibitor 99.1%
    PKCζ-IN-1 is a compound that inhibits PKCζ and CDK2, showing an IC50 value of 5.18 nM for PKCζ and 1.04 μM for CDK2, with significant selectivity of 200-fold. PKCζ-IN-1 can reduce the activity of CDK2 while inhibiting PKCζ.
    PKCζ-IN-1
  • HY-50914
    AZD5597
    Inhibitor 98.09%
    AZD5597 is an inhibitor of CDK with IC50 values of both 2 nM for CDK1 and CDK2. AZD5597 can inhibit the proliferation of tumor cells and has anti-tumor activity.
    AZD5597
  • HY-153244
    MFH290
    Inhibitor 98.12%
    MFH290 is a potent and highly selective cyclin-dependent kinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II). MFH290 is used for cancer research.
    MFH290
  • HY-100624
    Ryuvidine
    Inhibitor 99.23%
    Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM. Ryuvidine also inhibits KDM5A and blocks DNA synthesis. Ryuvidine has anticancer activity against tumors such as breast cancer. Ryuvidine improves arthritis.
    Ryuvidine
  • HY-13231
    CDK9-IN-1
    Inhibitor 98.52%
    CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87.
    CDK9-IN-1
  • 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-155805
    SGC-CAF382-1
    Inhibitor 98.15%
    CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain.
    SGC-CAF382-1
  • HY-101257B
    YKL-5-124 TFA
    Inhibitor 99.74%
    YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
    YKL-5-124 TFA
  • HY-15889
    AMG 925
    Inhibitor 99.02%
    AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
    AMG 925
  • HY-151110A
    PROTAC CDK12/13 Degrader-1 TFA
    Degrader 99.12%
    PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research.
    PROTAC CDK12/13 Degrader-1 TFA
  • HY-153278
    Q901
    Inhibitor 98.38%
    Q901 (CDK7-IN-21) is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 can be used for the research of cancer, such as colon cancer and lung cancer.
    Q901
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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