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-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-100429
    CAN508
    		Inhibitor 99.71%
    CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
    CAN508
  • HY-150023
    BI-1622
    		Inhibitor 98.02%
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
    BI-1622
  • HY-157516
    CDK2-IN-22
    		Inhibitor 98.64%
    CDK2-IN-22 (compound 7I) is a potent CDK2 inhibitor with an IC50 of 64.42 nM. CDK2-IN-22 presents a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC50 values of 0.83 μM, 2.12 μM, 3.12 μM, and 8.61 μM, respectively.
    CDK2-IN-22
  • 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-145563
    Eciruciclib
    		Inhibitor 98.03%
    Eciruciclib is an antineoplastic and potent cyclin dependent kinase (CDK) inhibitor.
    Eciruciclib
  • HY-161828A
    (S)-JWZ-5-13
    		Degrader 99.62%
    (S)-JWZ-5-13 (compound 17-Neg), a PROTAC CDK7 degrader, is a negative control compound of JWZ-5-13 (HY-161828). (S)-JWZ-5-13 displays similar in vitro CDK7 inhibition (IC50 = 21.1 nM) to JWZ-5-13, but fails to induce CDK7 degradation in cells.
    (S)-JWZ-5-13
  • HY-45661
    Inixaciclib
    		Inhibitor 99.93%
    Inixaciclib (NUV-422) is a blood-brain barrier-penetrant inhibitor of CDK2, CDK4 and CDK6. Inixaciclib inhibits cancer cell growth. Inixaciclib induces anti-tumor activity in xenograft models of glioblastoma, CDK4/CDK6 inhibitor-resistant HR+ HER2- metastatic breast cancer, and anti-androgen-resistant prostate cancer. Inixaciclib can be used for the research of relapsed or metastatic castration-resistant prostate cancer.
    Inixaciclib
  • 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-112811
    PROTAC CDK9 degrader-2
    		Inhibitor 99.22%
    PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC.
    PROTAC CDK9 degrader-2
  • HY-128669S
    Abemaciclib metabolite M2-d6
    		Inhibitor 99.90%
    Abemaciclib metabolite M2-d6 is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity.
    Abemaciclib metabolite M2-d<sub>6</sub>
  • HY-103380
    NSC 625987
    		Inhibitor 98.01%
    NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2.
    NSC 625987
  • HY-139725
    CDK5-IN-1
    		Inhibitor 98.47%
    CDK5-IN-1 is a potent CDK5 inhibitor with an IC50 less than 10 nM. CDK5-IN-1 is greater than 100-fold more active against CDK5 than CDK2. CDK5-IN-1 is used for kidney diseases research.
    CDK5-IN-1
  • HY-155787
    SHR5428
    		Inhibitor 99.80%
    SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM).
    SHR5428
  • HY-130514
    SMAPP1
    		99.43%
    SMAPP1 is an activator of protein phosphatase-1 (PP1). SMAPP1 increases phosphorylation of CDK9’s Ser90 and Thr186 residues, but not Ser175. SMAPP1 induces HIV-1 replication, upregulates HIV-1 transcription that led to the reactivation of latent HIV-1 provirus.
    SMAPP1
  • HY-119715
    AG-012986
    		Inhibitor 99.78%
    AG-012986 is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity.
    AG-012986
  • HY-112463
    CDK1-IN-2
    		Inhibitor 98.89%
    CDK1-IN-2 is a CDK1 inhibitor (IC50: 5.8 μM).
    CDK1-IN-2
  • HY-131978
    DB18
    		Inhibitor 99.15%
    DB18 is a potent and selective inhibitor of CDC2-like kinases (CLKs), with IC50 values in the range of 10-30 nM for CLK1, CLK2 and CLK4. DB18 has anti-tumor activity.
    DB18
  • HY-169947
    DDO-6079
    		Inhibitor 98.92%
    DDO-6079 is a potent CDC37 inhibitor. DDO-6079 inhibits HSP90-CDC37 and CDC37-CDK4/6 chaperone complex by binding to an allosteric site on CDC37. DDO-6079 decreases the thermostability of CDK6.
    DDO-6079
  • HY-136726
    CGP-82996
    		Inhibitor 98.12%
    GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer.
    CGP-82996
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CDK Isoform Comparison

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