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-115924
    CDK1-IN-1
    		Inhibitor 99.33%
    CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent.
    CDK1-IN-1
  • HY-144995
    BSJ-02-162
    		Inhibitor 98.07%
    CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader.
    BSJ-02-162
  • 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-B0877
    Halcinonide
    		Activator 98.29%
    Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke.
    Halcinonide
  • HY-148523
    HQ005
    		Degrader 98.56%
    HQ005 is a potent CCNK degrader with an DC50 value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation.
    HQ005
  • HY-117025A
    Manzamine A hydrochloride
    		Inhibitor 99.66%
    Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1.
    Manzamine A hydrochloride
  • HY-155218
    TMX-2172
    		Degrader 99.38%
    TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC50 values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer.
    TMX-2172
  • HY-163640
    CDK4 degrader 1
    		Degrader 99.83%
    CDK4 degrader 1 (ML 1–71) is a molecular glue degrader that targets CDK4.
    CDK4 degrader 1
  • HY-169912
    CDK2 degrader 5
    		Degrader 99.17%
    CDK2 degrader 5 is a CRBN-binding CDK2 molecular glue degrader. CDK2 degrader 5 induces ubiquitination and subsequent proteasomal degradation of CDK2. CDK2 degrader 5 can be used for the research of cancer.
    CDK2 degrader 5
  • HY-N8146
    Bruceantinol
    		98.89%
    Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells.
    Bruceantinol
  • HY-168660
    CPD-10
    		Degrader 98.59%
    CPD-10 is a potent CCND1 and CDK4 PROTAC degrader. CPD-10 exhibits anti-proliferative effects on tumor cells and can also induce apoptosis. CPD-10 can be used for the study of breast cancer and lung cancer.
    CPD-10
  • HY-N3389
    Licoisoflavone A
    		Inhibitor 99.53%
    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-170442
    ECI830
    		Inhibitor 98.01%
    ECI830 (CDK2-IN-37) is an orally active, ATP-competitive and highly selective CDK2 inhibitor. ECI830 shows high selectivity over other CDK family members. ECI830 can be used for the study of HR+/HER2- breast cancer and CCNE1-amplified tumors (such as ovarian cancer and lung cancer).
    ECI830
  • 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-I0996
    1,1-Dimethylethyl 4-(4-amino-3-pyridinyl)-1-piperazinecarboxylate
    		99.69%
    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-15777R
    Ribociclib (Standard)
    		Inhibitor
    Ribociclib (Standard) is the analytical standard of Ribociclib. This product is intended for research and analytical applications. Ribociclib (LEE01) 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 (Standard)
  • HY-50767S
    Palbociclib-d8
    		Inhibitor 99.84%
    Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research.
    Palbociclib-d<sub>8</sub>
  • HY-145072
    BSJ-01-175
    		Inhibitor 99.88%
    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-139980
    CDK9-IN-13
    		Inhibitor 99.94%
    CDK9-IN-13 (compound 38) is potent and selective CDK9 inhibitor, with an IC50 of <3 nM. CDK9-IN-13 exhibits short half-lives in rodents.
    CDK9-IN-13
  • HY-12653A
    LDC4297 hydrochloride
    		Inhibitor 98.23%
    LDC4297 hydrochloride is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection.
    LDC4297 hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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