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-176713
    KWZY-11
    Inhibitor
    KWZY-11 (Compound 11) is a potent PARP/CDK6 dual inhibitor with IC50 values of 156.8, 197.3, and 13.3 nM for PARP1, PARP2, and CDK6, respectively. KWZY-11 inhibits tumor cell proliferation by regulating the Wnt/β-catenin signaling pathway. KWZY-11 induces excessive DNA damage and apoptosis in MDA-MB-231 breast cancer cells.
    KWZY-11
  • HY-130850
    CDK9-IN-10
    Inhibitor 98.09%
    CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811).
    CDK9-IN-10
  • HY-164906
    TMX-2138
    Degrader
    TMX-2138 is a CDKs PROTAC degrader, with IC50s of 8.7 nM, 10.9 nM, 7.0 nM and 25.7 nM for CDK1/cyclinB, CDK2/cyclinA, CDK5/p25 and CDK9/cyclinT1, respectively. TMX-2138 promotes ubiquitination and degradation of CDKs. TMX-2138 can be used for the research of ovarian cancer (Pink: CDKs ligand (HY-151071); Blue: E3 ligase CRBN ligand (HY-14658); Black: linker (HY-W008352)).
    TMX-2138
  • HY-112371
    (S)-CR8
    Inhibitor 99.0%
    (S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM).
    (S)-CR8
  • HY-185121
    PROTAC CDK2/4/6 Degrader-2
    Degrader
    PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research.
    PROTAC CDK2/4/6 Degrader-2
  • HY-160213
    JA397
    Inhibitor
    JA397, a chemical probe, is a potent and selective inhibitor for the TAIRE family with cellular activity ranging from IC50 values of 21 nM to 307 nM.
    JA397
  • HY-180485
    PROTAC D16-M1P2
    PROTAC D16-M1P2 is an orally active PKMYT1 PROTAC degrader with a DC50 of 0.7 nM. PROTAC D16-M1P2 also inhibits the activity of PKMYT1 with an IC50 of 7.6 nM. PROTAC D16-M1P2 inhibits pCDK1 with an IC50 of 9 nM. PROTAC D16-M1P2 has demonstrated significant anti-tumor efficacy in mouse models and can be used for research on breast cancer.
    PROTAC D16-M1P2
  • HY-122665A
    HTH-01-091 TFA
    Inhibitor 99.48%
    HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research.
    HTH-01-091 TFA
  • HY-153556
    GW297361
    Inhibitor 98.13%
    GW297361 is an oxindole CDK inhibitor that elicits a Pho85-selective response in cells. GW297361 inhibits yeast Cdk1 and Pho85 with IC50s of 20 nM and 400 nM in vitro, respectively.
    GW297361
  • HY-111463
    CDK8-IN-3
    Inhibitor 98.17%
    CDK8-IN-3 is an inhibitor of CDK8 extracted from patent WO2016041618A1, compound example 1.7.
    CDK8-IN-3
  • HY-80013B
    (E/Z)-THZ1 dihydrochloride
    Inhibitor
    (E/Z)-THZ1 dihydrochloride is a selective inhibitor of CDK7 with an IC50 of 3.2 nM. (E/Z)-THZ1 dihydrochloride has antiproliferative effect.
    (E/Z)-THZ1 dihydrochloride
  • HY-RS02374
    CDK2 Human Pre-designed siRNA Set A
    Inhibitor

    CDK2 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    CDK2 Human Pre-designed siRNA Set A
  • HY-W077292R
    2,4,6-Trihydroxybenzoic acid (Standard)
    Inhibitor
    2,4,6-Trihydroxybenzoic acid, the flavonoid metabolite, is a CDK inhibitor. 2,4,6-Trihydroxybenzoic acid can be used for the research of cancer.
    2,4,6-Trihydroxybenzoic acid (Standard)
  • HY-50943R
    AT7519 Hydrochloride (Standard)
    Inhibitor
    AT7519 (Hydrochloride) (Standard) is the analytical standard of AT7519 (Hydrochloride). This product is intended for research and analytical applications. AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
    AT7519 Hydrochloride (Standard)
  • HY-112450
    Olomoucine II
    Inhibitor
    Olomoucine II is a potent CDK inhibitor with IC50 values of 0.06, 0.1, 0.45, 7.6, 19.8 µM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity.
    Olomoucine II
  • HY-N12625A
    (S)-(-)-O-Demethylbuchenavianine
    Inhibitor
    (S)-(-)-O-Demethylbuchenavianine (Compound (S)-(−)-1) is a flavonoidal alkaloids. (S)-(-)-O-Demethylbuchenavianine is a potent CDK inhibitor, with IC50 values of 0.03 and 0.05 μM for CDK1 and CDK5, respectively.
    (S)-(-)-O-Demethylbuchenavianine
  • HY-15612
    CDK4-IN-1
    CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.
    CDK4-IN-1
  • HY-N12625
    (R)-(+)-O-Demethylbuchenavianine
    Inhibitor 98.67%
    (R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC50s of 1.1, 0.95, >10, >10 and >10 μM, respectively.
    (R)-(+)-O-Demethylbuchenavianine
  • HY-157647
    1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC
    Inhibitor 99.9%
    1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) is an inhibitor of cyclin-dependent kinases (CDKs). 1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC induces apoptosis and inhibits the growth of various cancer cell lines.
    1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC
  • HY-111207
    CA224
    Inhibitor 99.94%
    CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity.
    CA224
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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