1. Vías de señalización
  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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-164664
    CDK2-IN-30
    Inhibitor 98.40%
    CDK2-IN-30 is a CDK2 inhibitor with an IC50 value ≤20 nM. CDK2-IN-30 modulates CDK2 activity to influence cell cycle regulation. CDK2-IN-30 can be used for the research of cancer.
    CDK2-IN-30
  • HY-16297AR
    Abemaciclib (Standard)
    Inhibitor
    Abemaciclib (Standard) is the analytical standard of Abemaciclib. This product is intended for research and analytical applications. Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    Abemaciclib (Standard)
  • HY-16366
    Briciclib
    Inhibitor 99.45%
    Briciclib (ON 014185) is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib can be used for the study of hematological system tumors and solid tumors.
    Briciclib
  • HY-149209
    LL-K8-22
    Degrader 99.06%
    LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research.
    LL-K8-22
  • HY-129180
    XY028-133
    Inhibitor 99.07%
    XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK.
    XY028-133
  • HY-137443
    Ipivivint
    Inhibitor 99.95%
    Ipivivint (Compound 38) is an orally active and potent CDC-like kinase (CLK) inhibitor with EC50 of 1 nM and 7 nM for CLK2 (human) and CLK3 (human), respectively. Ipivivint also inhibits the Wnt pathway (EC50=13 nM) and tyrosine phosphorylation-regulated kinase 1A (human) (EC50=5 nM).
    Ipivivint
  • HY-175842
    CDK2 degrader 7
    Degrader 99.51%
    CDK2 degrader 7 is an orally active CDK2 degrader, with DC50 values of 13 nM (MKN1cells) and 17 nM (TOV21G cells). CDK2 degrader 7 induces G1 phase arrest in MKN1 cells. CDK2 degrader 7 achieves tumor stasis in HCC1569 (CCNE1-amplified) xenograft models. CDK2 degrader 7 can be used for the study of CCNE1-amplified cancers.
    CDK2 degrader 7
  • HY-169245
    CDK-TCIP2
    Inhibitor 98.94%
    DK-TCIP2, linking inhibitor of CDK9 SNS-032 (HY-10008) with ligands of BCL6 BI-3812 (HY-111381), is a anticancer agent. DK-TCIP2 shows anticancer activity in vivo and in vitro and can be used for study of lymphoma cancer.
    CDK-TCIP2
  • HY-148065
    FMF-06-098-1
    Inhibitor 98.77%
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.
    FMF-06-098-1
  • HY-155723
    Leucettinib-92
    Inhibitor 98.54%
    Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3).
    Leucettinib-92
  • HY-153708
    SGC-CLK-1
    Inhibitor 99.12%
    SGC-CLK-1, a chemical probe, is a potent and selective inhibitor of Cdc2-like kinases CLK1, CLK2, and CLK4. SGC-CLK-1 can inhibit the growth of melanoma and glioblastoma cells.
    SGC-CLK-1
  • HY-156366
    SNX7886
    Degrader 99.71%
    SNX7886 is a CDK8/CDK19 PROTAC degrader. SNX7886 promotes the ubiquitination and degradation of CDK8 and CDK19. SNX7886 also promotes the degradation of CCNC. SNX7886 can be used in cancer research.
    SNX7886
  • HY-104013
    Aminopurvalanol A
    Inhibitor 98.98%
    Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization.
    Aminopurvalanol A
  • HY-111518
    JH-XI-10-02
    Inhibitor 99.73%
    JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.
    JH-XI-10-02
  • HY-103628
    PROTAC CDK9 Degrader-1
    Inhibitor 99.55%
    PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
    PROTAC CDK9 Degrader-1
  • HY-126675
    AS2863619 free base
    Inhibitor 99.87%
    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
    AS2863619 free base
  • HY-162919
    YK-2168
    Inhibitor 98.05%
    YK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. YK-2168 inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. YK-2168 induces apoptosis in tumor cells, suppresses expression of CDK9-regulated genes including MYC and Mcl1, and inhibits tumor growth in CDX mice models. YK-2168 can be used for the research of cancer, such as leukemia.
    YK-2168
  • HY-103712B
    Samuraciclib hydrochloride dihydrate
    Inhibitor 99.90%
    Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects.
    Samuraciclib hydrochloride dihydrate
  • HY-161724
    TFEB activator 2
    Modulator 98.84%
    TFEB activator 2 is an orally active compound that can cross the blood-brain barrier. TFEB activator 2 can bind to the dopamine transporter (DAT). TFEB activator 2 promotes TFEB nuclear translocation and lysosome biogenesis by targeting the DAT-CDK9-TFEB pathway. TFEB activator 2 has neuroprotective activity and can be used in the research of Alzheimer's disease and other diseases.
    TFEB activator 2
  • HY-164827
    CDK2 degrader 3
    Degrader 99.91%
    CDK2 degrader 3 is a selective CDK2 molecular glue-like degrader. CDK2 degrader 3 induces G1 cell cycle arrest in CCNE1-amplified cancer cells. CDK2 degrader 3 is applicable to breast cancer-related research.
    CDK2 degrader 3
Cat. No. Nombre del producto / Synonyms Species Source
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