1. Cell Cycle/DNA Damage
  2. CDK

CDK

CDKs (Cyclin-dependent kinases) are a family of protein kinases first discovered for their role in regulating the cell cycle. Types: Cdk1, Cdk2, Cdk3, Cdk4, Cdk5, Cdk6, Cdk7, Cdk8, Cdk9, Cdk11. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. They are present in all knowneukaryotes, and their regulatory function in the cell cycle has been evolutionarily conserved. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. 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. CDKs phosphorylate their substrates on serines and threonines, so they are serine-threonine kinases. CDK levels remains 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. cerevisiae (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 Related Products (69):

Cat. No. Product Name Effect Purity
  • HY-16297
    LY2835219 Inhibitor
    LY2835219 a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
  • HY-80013
    THZ1 Inhibitor
    THZ1 is a selective and potent covalent CDK7 inhibitor with IC50 of 3.2 nM.
  • HY-80013A
    THZ1 Hydrochloride Inhibitor
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with IC50 of 3.2 nM.
  • HY-50767
    Palbociclib Inhibitor
    Palbociclib is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.
  • HY-10492
    Dinaciclib Inhibitor
    Dinaciclib is a potent and selective inhibitor of CDKs, with IC90s of of 1, 1, 3, and 4 nM for CDK2, CDK5, CDK1, and CDK9 activity, respectively.
  • HY-12871
    BAY-1143572 Inhibitor
    BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.
  • HY-100023
    LY3177833 Inhibitor
    LY3177833 is an CDC7 and pMCM2 inhibitor extracted from patent US 20140275131and patent WO 2014143601 A1 compound example 4; has IC50 values of 3.3 nM and 290 nM, respectively。
  • HY-100791
    NSC23005 sodium Inhibitor
    NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
  • HY-50767A
    Palbociclib hydrochloride Inhibitor
    Palbociclib hydrochloride is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.
  • HY-A0065
    Palbociclib isethionate Inhibitor
    Palbociclib (isethionate) is a highly selective inhibitor of CDK4/6 with IC50s of 11 nM/16 nM, and shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. 
  • HY-15777
    LEE011 Inhibitor
    LEE011 is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-30237
    Roscovitine Inhibitor
    Roscovitine is a potent and selective CDK inhibitor with IC50 of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
  • HY-12529
    Ro-3306 Inhibitor
    Ro-3306 is a potent and selective inhibitor of CDK1 with Ki value of 35 nM for CDK1/cyclin B1, 10-fold selectivity relative to CDK2/cyclin E and >50-fold relative to CDK4/cyclin D.
  • HY-10005
    Flavopiridol Inhibitor
    Flavopiridol is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of around 40 nM.
  • HY-13942
    1-NM-PP1 Inhibitor
    1-NM-PP1 inhibits Cdk7 recovered from the mutant, but not the wild-type cells with an IC50 of ~50 nM with either substrate.
  • HY-12280
    THZ2 Inhibitor
    THZ2 is a potent and selective CDK7 inhibitor with IC50 of 13.9 nM.
  • HY-12293
    LY2857785 Inhibitor
    LY2857785 is a type I reversible and competitive ATP kinase inhibitor against, b>CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
  • HY-13266
    BS-181 Inhibitor
    BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
  • HY-10012
    AZD-5438 Inhibitor
    AZD-5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It also inhibits GSK3β, but is less potent to CDK5/6.
  • HY-15878
    LDC000067 Inhibitor
    LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.