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-130709
    PROTAC CDK2/9 Degrader-1
    		Inhibitor 99.85%
    PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand.
    PROTAC CDK2/9 Degrader-1
  • HY-N0404
    Sinigrin
    		Inhibitor 99.97%
    Sinigrin (Allyl-glucosinolate) is an orally active glucosinolate found in cruciferous plants. Sinigrin possesses multiple activities such as anti-cancer, antibacterial, antifungal, anti-inflammatory, antioxidant, and inhibition of fat synthesis. Sinigrin can be used in the research of tumors, inflammatory, and metabolic diseases.
    Sinigrin
  • HY-127104
    FMF-04-159-2
    		Inhibitor 99.64%
    FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively.
    FMF-04-159-2
  • HY-15815
    Bromosporine
    		Modulator 99.89%
    Bromosporine, a chemical probe, is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-Fluorouracil (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS.
    Bromosporine
  • HY-80013A
    THZ1 Hydrochloride
    		Inhibitor 99.06%
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
    THZ1 Hydrochloride
  • HY-114338A
    Dalpiciclib hydrochloride
    		Inhibitor 99.41%
    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-N0819
    Raddeanin A
    		Inhibitor 98.55%
    Raddeanin A is an oleanane-type triterpenoid saponin with oral activity. Raddeanin A inhibits SRC, mTOR, JNK, VEGFR2, NLRP3 inflammasome, Wnt/β-catenin, Wee1, PI3K/AKT signaling pathway, MAPK/ERK signaling pathway, AR-FL, AR-Vs, and downregulates the expression of p-PI3K and p-AKT. Raddeanin A inhibits osteoclast formation, bone resorption, osteolysis, cancer cell invasion, migration, proliferation, angiogenesis and epithelial-mesenchymal transition, while induces apoptosis, cell cycle arrest, ROS production, immunogenic cell death and dendritic cell maturation. Raddeanin A improves blood-retinal barrier function, alleviates inflammation, regulates the tumor microenvironment, and enhances the activity of anti-PD-1 antibody. Raddeanin A is applicable to the research of breast cancer-associated osteolysis, human osteosarcoma, colorectal cancer, glioblastoma, Alzheimer's disease, cholangiocarcinoma, melanoma, non-small cell lung cancer, castration-resistant prostate cancer and multiple myeloma.
    Raddeanin A
  • HY-112296
    T025
    		Inhibitor 99.64%
    T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research.
    T025
  • HY-157334
    DEG-77
    		Activator 99.03%
    DEG-77 is a molecular glue targeting IKZF2 and CK1α, with DC50 values of 15.3 nM and 10 nM, respectively. DEG-77 exhibits significant anti-tumor activity, inducing increased transcriptional levels of the pro-apoptotic protein Bax and the cell cycle arrest protein p21. DEG-77 is applicable to the research of acute myeloid leukemia (AmL), diffuse large B-cell lymphoma and ovarian cancer.
    DEG-77
  • HY-163814
    CDK2 degrader 1
    		Degrader 99.74%
    CDK2 degrader 1 (Compound 3) is a selective CDK2 molecular glue degrader with a Dmax (CDK2) of > 80% and a Ki (CRBN) > 1 μM. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers.
    CDK2 degrader 1
  • HY-12871B
    Atuveciclib
    		Inhibitor 99.75%
    Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb/CDK9 inhibitor. Atuveciclib (BAY-1143572) inhibits CDK9/CycT1 with an IC50 of 13 nM.
    Atuveciclib
  • HY-111556
    BSJ-03-123
    		Inhibitor 99.19%
    BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader.
    BSJ-03-123
  • HY-19807
    Indirubin-3'-monoxime
    		Inhibitor 99.80%
    Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
    Indirubin-3'-monoxime
  • HY-144981
    HQ461
    		Inhibitor 98.10%
    HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death.
    HQ461
  • HY-11009
    CGP60474
    		Inhibitor 98.90%
    CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.
    CGP60474
  • HY-10014
    R547
    		Inhibitor 99.57%
    R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
    R547
  • HY-15878
    LDC000067
    		Inhibitor 99.00%
    LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.
    LDC000067
  • HY-136252
    BSJ-04-132
    		Inhibitor 99.07%
    BSJ-04-132 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity.
    BSJ-04-132
  • HY-10424
    Milciclib
    		Inhibitor 99.89%
    Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
    Milciclib
  • HY-108359
    Alsterpaullone
    		Inhibitor 99.85%
    Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.
    Alsterpaullone
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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