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-114338A
    Dalpiciclib hydrochloride
    		Inhibitor 98.22%
    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-137432B
    Avotaciclib hydrochloride
    		Inhibitor 99.75%
    Avotaciclib (BEY1107) hydrochloride is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib hydrochloride can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib hydrochloride can be used in the research of cancer such as pancreatic cancer and lung cancer.
    Avotaciclib hydrochloride
  • 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-153894
    SRX3177
    		Inhibitor 99.59%
    SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells.
    SRX3177
  • HY-149262
    CLK1-IN-3
    		Inhibitor 98.03%
    CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research.
    CLK1-IN-3
  • HY-18285
    Longdaysin
    		Inhibitor 99.83%
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
    Longdaysin
  • HY-I0996
    1,1-Dimethylethyl 4-(4-amino-3-pyridinyl)-1-piperazinecarboxylate
    		99.92%
    1,1-Dimethylethyl 4-(4-amino-3-pyridinyl)-1-piperazinecarboxylate is the impurity of Palbociclib (HY-50767). Palbociclib is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively.
    1,1-Dimethylethyl 4-(4-amino-3-pyridinyl)-1-piperazinecarboxylate
  • HY-100888A
    (R)-Simurosertib
    		Control 99.58%
    (R)-Simurosertib ((R)-TAK-931) is the (R)-enantiomer of Simurosertib. Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM .
    (R)-Simurosertib
  • HY-126251
    CDK9-IN-7
    		Inhibitor 98.05%
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
    CDK9-IN-7
  • HY-153260
    TP-1287
    		Inhibitor
    TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor.
    TP-1287
  • HY-114339
    CDK4/6-IN-2
    		Inhibitor 99.82%
    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
  • HY-W077292
    2,4,6-Trihydroxybenzoic acid
    		Inhibitor 99.73%
    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
  • HY-144995
    BSJ-02-162
    		Inhibitor 98.07%
    CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader. CDK4/6-IN-11 consists of a thalidomide-based E3 ligase ligand (blue part) Thalidomide-NH-CH2-COOH (HY-131717), a target protein ligand (red part) Palbociclib (HY-50767), and a PROTAC linker (black part) Boc-NH-C4-Br (HY-W007803). E3 ligase ligand and linker can form Thalidomide-NH-amido-C4-Br (HY-170307).
    BSJ-02-162
  • HY-18944
    FIT-039
    		Inhibitor 99.56%
    FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
    FIT-039
  • HY-151463
    CDK8-IN-11
    		Inhibitor 98.20%
    CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer.
    CDK8-IN-11
  • 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-111237
    Butyrolactone I
    		Inhibitor 99.80%
    Butyrolactone I is an orally active and ATP-competitive inhibitor of CDK1. Butyrolactone I inhibits NF-κB, cdc2 kinase, Bax, ROS production, modulates the PERK/CHOP. Butyrolactone I mitigates heat-stress-induced Apoptosis. Butyrolactone I shows anti-inflammatory and intestinal protective activity. Butyrolactone I has antitumor effects against non-small cell lung, small cell lung, prostate cancer and leukemia. Butyrolactone I can be used in NASH research.
    Butyrolactone I
  • HY-13461
    PHA-767491
    		Inhibitor 99.85%
    PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
    PHA-767491
  • HY-12871
    Atuveciclib Racemate
    		Inhibitor 98.48%
    Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
    Atuveciclib Racemate
  • HY-128769
    M2N12
    		Inhibitor 98.19%
    M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09  μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research.
    M2N12
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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