1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. CDK

CDK

Cyclin dependent kinase

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).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-137449
    Rintodestrant
    Inhibitor 99.91%
    Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor.
    Rintodestrant
  • HY-137346
    DD-03-156
    99.90%
    DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17 (Blue: VHL ligand (HY-112078), Black: linker HY-124380 (HY-124380);Pink: BRAF inhibitor (HY-14660)).
    DD-03-156
  • HY-15166B
    (E/Z)-Zotiraciclib citrate
    Inhibitor 99.83%
    (E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor.
    (E/Z)-Zotiraciclib citrate
  • HY-W011109
    CKI-7
    Inhibitor 99.97%
    CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.
    CKI-7
  • HY-169910
    CDK2 degrader 4
    Inhibitor 99.71%
    CDK2 degrader 4 (compound 104) is a potent CDK2 degrader. CDK2 degrader 4 has the potential for the research of cancer.
    CDK2 degrader 4
  • HY-152263
    HEMTAC CDK4/6 degrader 1
    Inhibitor 98.18%
    HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HEMTAC CDK4/6 degrader 1
  • HY-161168
    Cyclin K degrader 1
    Degrader 99.86%
    Cyclin K degrader 1 (compound 40) is an AT7519 (HY-50940) based Cyclin K degrader with DC50 of 21 nM. Cyclin K degrader 1 has an affinity for cyclin K that is ~500-fold higher than its affinity for CDK12.
    Cyclin K degrader 1
  • HY-154851
    GSK-3 inhibitor 3
    Inhibitor 99.10%
    GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research.
    GSK-3 inhibitor 3
  • HY-B1165
    Cyproheptadine (hydrochloride sesquihydrate)
    99.74%
    Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
    Cyproheptadine (hydrochloride sesquihydrate)
  • HY-137342
    SB1-G-187
    Degrader 98.70%
    SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research. (Pink: multi-target kinase ligand (HY-125142); Blue: CRBN ligand (HY-A0003); Black: linker).
    SB1-G-187
  • HY-N9561
    Vanicoside B
    Inhibitor 99.82%
    Vanicoside B is a phenylpropanoyl sucrose derivative, can be isolated from the herb Persicaria dissitiflora. Vanicoside B targets cyclin-dependent kinase 8 (CDK8) and exhibits anti-tumor activity. The potential mechanism is Vanicoside B blocks CDK8-mediated signaling pathways and decreases the expression of epithelial-mesenchymal transition proteins, so that it leads to cell cycle arrest and apoptosis.
    Vanicoside B
  • HY-14372
    BS-194
    Inhibitor 99.13%
    BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer.
    BS-194
  • HY-111465
    CDK8-IN-4
    Inhibitor 99.39%
    CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC50 of 0.2 nM.
    CDK8-IN-4
  • HY-46568
    CDK7/12-IN-1
    Inhibitor 99.66%
    CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth.
    CDK7/12-IN-1
  • HY-P10440
    Cdk5i peptide
    Inhibitor 98.93%
    Cdk5i peptide is a CDK5 inhibitory peptide with high binding affinity for Cdk5/p25 (Kd of 0.17 μM), which can block the interaction between CDK5 and p25 and reduce the kinase activity of CDK5/p25. Cdk5i peptide can be used in the stud y of neurodegenerative diseases.
    Cdk5i peptide
  • HY-78428
    CDK-IN-6
    Inhibitor 99.43%
    CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities.
    CDK-IN-6
  • 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-15777S
    Ribociclib-d6
    99.9%
    Ribociclib-d6 (LEE011-d6) is a deuterium labeled Ribociclib (HY-15777). 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>
  • HY-102039
    CDK9-IN-8
    Inhibitor 99.16%
    CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC50 of 12 nM.
    CDK9-IN-8
  • HY-114339
    CDK4/6-IN-2
    Inhibitor 99.67%
    CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively.
    CDK4/6-IN-2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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