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-155736
    MAPK-IN-2
    		Inhibitor 98.54%
    MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFRT790M IC50=69 nM and B-RAFV600E IC50=83 nM).
    MAPK-IN-2
  • HY-112460
    CDK2-IN-3
    		Inhibitor
    CDK2-IN-3 (compound 3) is a potent and selective CDK2 inhibitor with an IC50 of 60 nM.
    CDK2-IN-3
  • HY-16462
    CDK9-IN-2
    		Inhibitor 98.72%
    CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.
    CDK9-IN-2
  • HY-13461
    PHA-767491
    		Inhibitor 99.85%
    PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
    PHA-767491
  • HY-I0996
    1,1-Dimethylethyl 4-(4-amino-3-pyridinyl)-1-piperazinecarboxylate
    		99.92%
    1,1-Dimethylethyl 4-(4-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-(4-amino-3-pyridinyl)-1-piperazinecarboxylate
  • HY-162919
    YK-2168
    		Inhibitor 98.05%
    YK-2168 is a differentiated selective inhibitor of CDK9.
    YK-2168
  • HY-145072
    BSJ-01-175
    		Inhibitor 99.49%
    BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.
    BSJ-01-175
  • HY-111379
    EHT 5372
    		Inhibitor 98.12%
    EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively.
    EHT 5372
  • HY-114338A
    Dalpiciclib hydrochloride
    		Inhibitor 98.22%
    Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively. Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.
    Dalpiciclib hydrochloride
  • 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-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-W011428
    Olomoucine
    		Inhibitor 99.87%
    Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM). Olomoucine regulates cell cycle and shows anti-melanin tumor activity.
    Olomoucine
  • HY-163786
    PROTAC CDK4/6 degrader 1
    		Degrader 98.88%
    PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
    PROTAC CDK4/6 degrader 1
  • HY-149974
    CDK8-IN-13
    		Inhibitor 99.14%
    CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity.
    CDK8-IN-13
  • HY-15504A
    RGB-286638 free base
    		Inhibitor 98.87%
    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-100023
    LY3177833
    		Inhibitor 99.48%
    LY3177833 (Example 4) is an orally active CDC7 and pMCM2 inhibitor with IC50 values of 3.3 nM and 290 nM, respectively. LY3177833 is a senescence inducer.
    LY3177833
  • 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-50767R
    Palbociclib (Standard)
    		Inhibitor
    Palbociclib (Standard) is the analytical standard of Palbociclib. This product is intended for research and analytical applications. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
    Palbociclib (Standard)
  • HY-15777AS
    Ribociclib-d6 hydrochloride
    		Inhibitor 98.37%
    Ribociclib-d6 (LEE011-d6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib 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.
    Ribociclib-d<sub>6</sub> hydrochloride
  • HY-162037
    CDDD11-8
    		Inhibitor 99.62%
    CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation.
    CDDD11-8
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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