CDK

CDK inhibitors block cyclin-dependent kinases (CDKs), the serine/threonine kinases that drive the cell cycle. Each CDK becomes active only when bound to a cyclin partner, and successive cyclin-CDK complexes order DNA replication and mitosis. CDK4 and CDK6 pair with D-type cyclins to control progression through G1, while CDK1 governs entry into mitosis. Palbociclib and abemaciclib are selective CDK4/6 inhibitors used to study G1 arrest and retinoblastoma protein phosphorylation. Dinaciclib and seliciclib act on several family members, including CDK2, CDK5 and CDK9, which also links them to transcription research. Ro 3306 inhibits CDK1 and is used to hold cells reversibly at the G2/M boundary for synchronization experiments.

Items 551-575 of 614

  • Cdc7-IN-21
    Cat. No.
    A54419

    Cdc7-IN-21

    Cdc7-IN-21 is a highly potent and selective inhibitor of Cdc7 with an IC50 of 0.07 nM. This compound is primarily utilized in cancer research, facilitating investigations into cell cycle regulation and potential therapeutic strategies targeting Cdc7-dependent pathways. Its specificity makes it a valuable tool for elucidating the role of Cdc7 in tumorigenesis and exploring new avenues for cancer treatment.

    1 mg
    $280.00
    5 mg
    $680.00
    All 7 sizes
  • Ulecaciclib
    Cat. No.
    A54420

    Ulecaciclib

    Ulecaciclib is an orally active inhibitor of cyclin-dependent kinases (CDKs), specifically targeting CDK2, CDK4, CDK6, and CDK7 with Ki values of 0.62 μM, 0.2 nM, 3 nM, and 0.63 μM, respectively. This compound exhibits excellent pharmacokinetic properties and is capable of crossing the blood-brain barrier. Ulecaciclib is valuable for research applications in cancer biology, particularly in the study of cell cycle regulation and CDK-related pathways in various malignancies.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • CDK12-IN-9
    Cat. No.
    A54421

    CDK12-IN-9

    CDK12-IN-9 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12) with an IC50 of 2.2 nM. This compound effectively inhibits phosphorylated serine 2 (pSER2), a key downstream marker associated with CDK12/13 activity. CDK12-IN-9 is suitable for cancer research, offering potential insights into therapeutic strategies targeting transcriptional regulation and DNA repair mechanisms in malignant cells.

    Out of stock

    All 3 sizes
  • CDK2-IN-28
    Cat. No.
    A54422

    CDK2-IN-28

    CDK2-IN-28 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), designed to modulate cell cycle progression. This compound demonstrates significant anti-proliferative activity against MKN1 cells, with an EC50 of 0.31 μM. CDK2-IN-28 is valuable for research into mechanisms of cell cycle regulation and potential therapeutic applications in cancer.

    Out of stock

    All 3 sizes
  • CDK2-IN-51
    Cat. No.
    A54423

    CDK2-IN-51

    CDK2-IN-51 is a pyrazolopyridine derivative that selectively inhibits cyclin-dependent kinase 2 (CDK2) with an IC50 value of 23.47 nM. This compound demonstrates significant biological activity by downregulating the expression of critical DNA replication factors, including Polα, MCM7, ORC2, and ORC4, leading to pre-G1 cell cycle arrest. CDK2-IN-51 is primarily utilized in the research of colorectal cancer, providing valuable insights into cell cycle regulation and potential therapeutic strategies.

    Out of stock

    All 3 sizes
  • PROTAC CDK9 degrader-8
    Cat. No.
    A54425

    PROTAC CDK9 degrader-8

    PROTAC CDK9 degrader-8 is a potent degrader targeting CDK9, exhibiting an IC50 value of 0.01 μM. This compound effectively induces the degradation of CDK9, making it a valuable tool for investigating the role of CDK9 in cancer biology and therapeutic resistance. It is suitable for use in studies aimed at understanding the mechanisms of tumor progression and exploring potential treatment strategies.

    Out of stock

    All 3 sizes
  • SR-5037
    Cat. No.
    A54426

    SR-5037

    SR-5037 is an orally active inhibitor of CDK12 and CDK13, with an IC50 of 31 nM, and functions as a molecular glue degrader for CycK, demonstrating a DC50 of 30 nM and Dmax exceeding 98%. By inhibiting the enzymatic activity of the CDK12/CycK and CDK13/CycK complexes, SR-5037 facilitates the recruitment of DDB1, leading to proteasome-mediated degradation of CycK. This compound has shown efficacy in degrading active CycK in mouse models of triple-negative breast cancer and is a valuable tool for investigating treatment options in such malignancies.

    5 mg
    $440.00
    10 mg
    $720.00
    All 4 sizes
  • CDK7-IN-17
    Cat. No.
    A54427

    CDK7-IN-17

    CDK7-IN-17 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), a key regulator of transcription and cell cycle progression. This pyrimidinyl derivative demonstrates potent inhibitory activity against CDK7, making it a valuable tool in cancer research, particularly in studies related to transcriptional dysregulation in various malignancies. Its application in elucidating CDK7's role in tumorigenesis may provide insights into novel therapeutic strategies for cancer treatment.

    1 mg
    $235.00
    5 mg
    $590.00
    All 5 sizes
  • CDK7-IN-31
    Cat. No.
    A54429

    CDK7-IN-31

    CDK7-IN-31 is a highly potent and orally bioavailable inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating a Kd value of 0.18 nM. This compound exhibits significant anticancer activity, making it a valuable tool for cancer research and therapeutic development. Its selective inhibition of CDK7 facilitates investigations into the role of this kinase in cell cycle regulation and transcriptional control.

    Out of stock

    All 3 sizes
  • CDK8-IN-14
    Cat. No.
    A54430

    CDK8-IN-14

    CDK8-IN-14 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), displaying an IC50 value of 39.2 nM. This compound demonstrates significant anti-proliferative effects on acute myeloid leukemia (AML) cells, with reported GC50 values of 0.02 ± 0.01 μM for Molm-13 and 0.03 ± 0.01 μM for MV4-11. Its potency makes it a valuable tool for research into CDK8-mediated signaling pathways and potential therapeutic strategies in AML.

    Out of stock

    All 3 sizes
  • CDK4/6-IN-8
    Cat. No.
    A54432

    CDK4/6-IN-8

    CDK4/6-IN-8 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), displaying IC50 values of 5.01 nM and 3.97 nM for each target, respectively. This compound effectively modulates cell cycle progression, making it a valuable tool for studies related to cancer biology and therapies targeting cell proliferation. Its precise inhibition of CDK4 and CDK6 positions it for use in research on tumor cell growth and the mechanistic exploration of cell cycle dysregulation in various malignancies.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • CDK12-IN-8
    Cat. No.
    A54433

    CDK12-IN-8

    CDK12-IN-8 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), which primarily targets the phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II. By disrupting CDK12-mediated transcription elongation and DNA damage repair mechanisms, CDK12-IN-8 has significant implications for cancer research, particularly in malignancies characterized by elevated CDK12 expression, such as small cell lung cancer and triple-negative breast cancer. It serves as a valuable tool for exploring the role of CDK12 in oncogenic processes.

    5 mg
    $675.00
    10 mg
    $1,040.00
    All 5 sizes
  • KM05382
    Cat. No.
    A54434

    KM05382

    KM05382 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), disrupting its activity and consequently leading to reduced transcription of the GAPDH gene. This compound plays a crucial role in regulating transcriptional control and has potential applications in understanding cell cycle dynamics and cancer research. Its unique mechanism makes it valuable for studies aimed at evaluating CDK9's role in gene expression and related pathways.

    25 mg
    $1,780.00
    50 mg
    $2,280.00
    All 3 sizes
  • p27
    Cat. No.
    A54436

    p27

    p27 is a cyclin-dependent kinase (CDK) inhibitor that functions as a substrate for the SCFSkp2/Cks1 complex. This protein plays a crucial role in cell cycle regulation by inhibiting CDK activity, thereby impacting cell proliferation. p27 is widely used in cancer research to investigate the mechanisms of tumorigenesis and to explore therapeutic strategies for targeting cell cycle dysregulation.

    Out of stock

    All 3 sizes
  • CLZX-205
    Cat. No.
    A54437

    CLZX-205

    CLZX-205 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 2.9 nM. This compound is significant in cancer research due to its ability to inhibit the phosphorylation of RNA polymerase II, thereby impacting transcriptional regulation in oncogenic pathways. CLZX-205 serves as a valuable tool for studying CDK9-related mechanisms and therapeutic strategies in cancer biology.

    Out of stock

    All 3 sizes
  • CDK9-IN-23
    Cat. No.
    A54438

    CDK9-IN-23

    CDK9-IN-23 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9) with an IC50 value of less than 20 nM. This compound demonstrates effective inhibition of transcriptional regulation and is crucial for studying cellular processes such as proliferation and survival. CDK9-IN-23 is primarily used in research applications focused on cancer biology and the modulation of gene expression pathways.

    Out of stock

    All 3 sizes
  • PROTAC CDK2/4/6 Degrader-1
    Cat. No.
    A54439

    PROTAC CDK2/4/6 Degrader-1

    PROTAC CDK2/4/6 Degrader-1 is a potent orally bioavailable degrader targeting CDK2, CDK4, and CDK6 through the proteolysis-targeting chimera (PROTAC) mechanism. This compound functions by facilitating the ubiquitination and degradation of these cyclin-dependent kinases, thereby inhibiting their activity. Its applications extend to the study of malignant melanoma, providing valuable insights into tumor biology and potential therapeutic interventions. This degrader is synthesized as a prodrug from PROTAC CDK2/4/6 Degrader-2, enabling enhanced functionality in biological systems.

    Out of stock

    All 3 sizes
  • PROTAC CDK9 degrader-5
    Cat. No.
    A54441

    PROTAC CDK9 degrader-5

    PROTAC CDK9 degrader-5 is a targeted PROTAC that specifically degrades CDK9 through the proteasomal pathway. It effectively induces degradation of CDK9 with DC50 values of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively. This reagent is a valuable tool for investigating the role of CDK9 in various biological processes and for potential therapeutic applications in cancer research.

    Out of stock

    All 3 sizes
  • CDK4/6-IN-17
    Cat. No.
    A54442

    CDK4/6-IN-17

    CDK4/6-IN-17 is a potent orally active inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), exhibiting an IC50 range of 10-100 nM in BE(2) cells. This compound effectively inhibits tumor growth in the COLO205 xenograft model, making it a valuable tool for cancer research focused on cell cycle regulation and therapeutic strategies targeting CDK4/6 pathways. Its application in preclinical studies provides insights into the mechanistic effects of CDK4/6 inhibition on tumor progression.

    Out of stock

    All 3 sizes
  • CDK4/6-IN-19
    Cat. No.
    A54443

    CDK4/6-IN-19

    CDK4/6-IN-19 is a selective inhibitor of CDK4 and CDK6, demonstrating IC50 values of 0.2 nM and 5.0 nM, respectively. It effectively inhibits cellular proliferation, making it a valuable reagent for cancer research applications, particularly in studies focused on cell cycle regulation and tumor growth. Its potent activity positions CDK4/6-IN-19 as a critical tool in evaluating potential therapeutic interventions against CDK4/6-dependent malignancies.

    25 mg
    $1,655.00
    50 mg
    $2,115.00
    All 3 sizes
  • CDK2-IN-15
    Cat. No.
    A54444

    CDK2-IN-15

    CDK2-IN-15 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 2.9 μM. This compound plays a significant role in cancer research by modulating cell cycle progression and apoptosis. CDK2-IN-15 is suitable for studies aimed at understanding CDK2's role in tumorigenesis and potential therapeutic strategies in oncology.

    1 mg
    $430.00
    5 mg
    $1,100.00
    All 2 sizes
  • CDK7-IN-7
    Cat. No.
    A54445

    CDK7-IN-7

    CDK7-IN-7 is a potent and selective inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating an IC50 of less than 50 nM. This compound effectively interferes with CDK7 activity, leading to reductions in transcriptional regulation and cellular proliferation. CDK7-IN-7 is valuable for research applications focused on cancer biology, transcription regulation, and therapeutic strategies targeting cell cycle dysregulation.

    5 mg
    $795.00
    All 1 sizes
  • TMX-2138
    Cat. No.
    A54446

    TMX-2138

    TMX-2138 is a potent CDKs PROTAC degrader that achieves IC50 values of 8.7 nM for CDK1/cyclinB, 10.9 nM for CDK2/cyclinA, 7.0 nM for CDK5/p25, and 25.7 nM for CDK9/cyclinT1. This compound facilitates the ubiquitination and subsequent degradation of cyclin-dependent kinases (CDKs), making it a valuable tool for investigating their roles in cellular processes. TMX-2138 is particularly relevant for research focused on ovarian cancer, enabling the study of CDK-targeted therapies and their potential therapeutic implications.

    Out of stock

    All 3 sizes
  • CDK8-IN-15
    Cat. No.
    A54447

    CDK8-IN-15

    CDK8-IN-15 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting a potent IC50 of 57 nM. This compound enhances the thermal stability of CDK8 while effectively inhibiting NF-κB signaling pathways. CDK8-IN-15 demonstrates promising biological activity in an in vitro psoriasis model induced by TNF-α, alleviating inflammation and promoting the expression of anti-inflammatory markers such as Foxp3 and IL-10. This makes it a valuable tool for research into psoriasis and related inflammatory disorders.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • YJZ5118
    Cat. No.
    A54448

    YJZ5118

    YJZ5118 is a selective inhibitor of cyclin-dependent kinases 12 and 13 (CDK12/CDK13), demonstrating IC50 values of 39.5 nM and 26.4 nM, respectively. This compound suppresses the transcription of DNA damage response genes, induces DNA damage in tumor cells, and effectively inhibits cellular proliferation while triggering apoptosis. YJZ5118 specifically impedes RNA polymerase II Ser2 phosphorylation and enhances Akt pathway activity, exhibiting synergistic effects when combined with Akt inhibitors. It is a valuable research tool for studying various cancers, including prostate cancer.

    Out of stock

    All 3 sizes

Items 551-575 of 614

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