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-143430A
    (S)-LY3177833 hydrate
    		Inhibitor
    (S)-LY3177833 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. (S)-LY3177833 hydrate shows broad in vitro anticancer activity.
    (S)-LY3177833 hydrate
  • HY-13266
    BS-181
    		Inhibitor 98.10%
    BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy.
    BS-181
  • HY-145599
    Tanuxiciclib
    		Inhibitor 98.0%
    Tanuxiciclib is a cyclin dependent kinase (CDK) inhibitor.
    Tanuxiciclib
  • HY-45661
    Inixaciclib
    		Inhibitor 99.93%
    Inixaciclib is a potent CDK inhibitor, can be used to research anticancer.
    Inixaciclib
  • HY-139011
    IV-361
    		Inhibitor 99.60%
    IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1).
    IV-361
  • HY-100023A
    LY3177833 monhydrate
    		Inhibitor 99.76%
    LY3177833 (Example 4) monhydrate is an orally active CDC7 and pMCM2 inhibitor with IC50 values of 3.3 nM and 290 nM, respectively. LY3177833 monhydrate is a senescence inducer.
    LY3177833 monhydrate
  • HY-157516
    CDK2-IN-22
    		Inhibitor 98.64%
    CDK2-IN-22 (compound 7I) is a potent CDK2 inhibitor with an IC50 of 64.42 nM. CDK2-IN-22 presents a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC50 values of 0.83 μM, 2.12 μM, 3.12 μM, and 8.61 μM, respectively.
    CDK2-IN-22
  • HY-114177A
    (S)-Ebvaciclib
    		Control 98.18%
    (S)-PF-06873600 it the S enantiomer of PF-06873600. PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK).
    (S)-Ebvaciclib
  • HY-168683
    CDK8 ligand 1
    		Degrader
    CDK8 ligand 1 is the ligand of CDK8. CDK8 ligand 1 can be used to synthesize LL-K8-22 (HY-149209).
    CDK8 ligand 1
  • HY-176165
    CDK9/EZH2-IN-1
    		Inhibitor
    CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC50: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC50 values are 136.3, 171.3 and 315.7 nM, respectively).
    CDK9/EZH2-IN-1
  • HY-168556
    YJ9069
    		Degrader
    YJ9069 is a selective CDK12/CDK13 PROTAC degrader with an IC50 of 22.22 nM for in VCaP cells. CDK12/13 degradation rapidly triggers gene-length-dependent transcriptional elongation defects, leading to DNA damage and cell-cycle arrest. YJ9069 effectively inhibits proliferation in subsets of prostate cancer cells and significantly suppresses prostate tumor growth. (Pink: CDK12/CDK13 degradation agent (HY-168658); Black: Linker (HY-W015967); Blue: ligand for E3 ligase (HY-103596)).
    YJ9069
  • HY-100035
    PT-262
    		Inhibitor 99.21%
    PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity.
    PT-262
  • HY-148214
    CDK2/4/6-IN-2
    		Inhibitor 98.20%
    CDK2/4/6-IN-2 is a CKD2/4/6 inhibitor, with IC50 values less than 1 μM, 10 nM, 100 nM respectively.
    CDK2/4/6-IN-2
  • HY-12843
    Bohemine
    		Inhibitor 98.93%
    Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.
    Bohemine
  • HY-N11439
    Albanol B
    		Inhibitor 99.79%
    Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2.
    Albanol B
  • HY-112811
    PROTAC CDK9 degrader-2
    		Inhibitor
    PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC.
    PROTAC CDK9 degrader-2
  • HY-114903
    (E/Z)-BIO-acetoxime
    		Inhibitor
    (E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM).
    (E/Z)-BIO-acetoxime
  • HY-117608
    ML 315
    		Inhibitor
    ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research.
    ML 315
  • HY-149636
    Multi-target kinase inhibitor 2
    		Inhibitor 99.82%
    Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
    Multi-target kinase inhibitor 2
  • HY-147646
    CDK1/Cyc B-IN-1
    		Inhibitor 98.47%
    CDK1/Cyc B-IN-1 (Compound 5) is a selective CDK1/Cyc B complex inhibitor with an IC50 of 97 nM. CDK1/Cyc B-IN-1 triggers apoptosis and G2/M cell cycle arrest. CDK1/Cyc B-IN-1 shows broad-spectrum cytotoxic action against cancer cell lines.
    CDK1/Cyc B-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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