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-P2559
    CDK7/9 tide
    99.92%
    CDK7/9 tide is peptide substrate for CDK7 or CDK9.
    CDK7/9 tide
  • HY-129336
    Abemaciclib metabolite M20
    Inhibitor
    Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.
    Abemaciclib metabolite M20
  • HY-107407
    SB-218078
    Inhibitor 98.30%
    SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest.
    SB-218078
  • HY-104013
    Aminopurvalanol A
    Inhibitor 98.25%
    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-150082
    CP681301
    Inhibitor 99.18%
    CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila.
    CP681301
  • HY-N6954
    Garcinone C
    Inhibitor 99.66%
    Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active.
    Garcinone C
  • HY-100023
    LY3177833
    Inhibitor 99.48%
    LY3177833 (Example 4) is an orally active CDC7 and pMCM2 inhibitor with IC50 values of 3.3 nM and 290 nM, respectively. LY3177833 is a senescence inducer.
    LY3177833
  • HY-103712B
    Samuraciclib hydrochloride dihydrate
    Inhibitor 99.08%
    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-134911
    HS-243
    Inhibitor 99.95%
    HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity.
    HS-243
  • HY-12653
    LDC4297
    Inhibitor 98.25%
    LDC4297 is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 value of 0.02-1.21 μM. LDC4297 can be used for the research of infection.
    LDC4297
  • HY-15777AS
    Ribociclib-d6 hydrochloride
    Inhibitor 98.37%
    Ribociclib-d6 (hydrochloride) is a deuterium labeled Ribociclib. 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[1].
    Ribociclib-d<sub>6</sub> hydrochloride
  • HY-107419
    NU6140
    Inhibitor 99.07%
    NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs. NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively. Enhances the apoptotic effect, with anti-cancer activity.
    NU6140
  • HY-13033
    CDK-IN-2
    Inhibitor 98.97%
    CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.
    CDK-IN-2
  • HY-123600
    SRI-29329
    Inhibitor 99.73%
    SRI-29329 is a specific CLK inhibitor, with IC50 values of 78 nM, 16 nM and 86 nM for CLK1, CLK2 and CLK4, respectively.
    SRI-29329
  • HY-163814
    CDK2 degrader 1
    Inhibitor 99.74%
    CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. 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 (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker).
    CDK2 degrader 1
  • HY-112460
    CDK2-IN-3
    Inhibitor
    CDK2-IN-3 (compound 3) is a potent and selective CDK2 inhibitor with an IC50 of 60 nM.
    CDK2-IN-3
  • HY-145121
    DS96432529
    Inhibitor 99.93%
    DS96432529 is a potent and orally active bone anabolic agent through CDK8 inhibition.
    DS96432529
  • HY-145072
    BSJ-01-175
    Inhibitor 99.45%
    BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.
    BSJ-01-175
  • HY-137432
    Avotaciclib
    Inhibitor 99.72%
    Avotaciclib (BEY1107) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib can be used for the research of locally advanced or metastatic pancreatic cancer.
    Avotaciclib
  • HY-124639
    CDK9 inhibitor HH1
    Inhibitor 99.56%
    CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor. CDK9 inhibitor HH1 inhibits the transcription of CDK. CDK9 inhibitor HH1 can be used in research of cancer.
    CDK9 inhibitor HH1
Cat. No. Product Name / Synonyms Species Source
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