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 26-50 of 67

  • PROTAC CDK2/4/6 Degrader-2
    Cat. No.
    A25107

    PROTAC CDK2/4/6 Degrader-2

    PROTAC CDK2/4/6 Degrader-2 is a targeted protein degradator specifically designed to degrade cyclin-dependent kinases CDK2, CDK4, and CDK6. This compound effectively inhibits cell proliferation and induces cell cycle arrest and apoptosis in malignant melanoma cells. Its application extends to cancer research, particularly in investigating the role of CDK2/4/6 in tumor biology. The compound can also be converted into its prodrug form, enabling versatile utilization in various assays related to cancer therapeutics.

    Out of stock

    All 3 sizes
  • PROTAC CDK4/6 degrader 1
    Cat. No.
    A30477

    PROTAC CDK4/6 degrader 1

    PROTAC CDK4/6 degrader 1 is a dual-targeted degrader designed to selectively degrade cyclin-dependent kinases CDK4 and CDK6. With DC50 values of 10.5 nM and 2.5 nM, this compound effectively inhibits cell proliferation in Jurkat cells, demonstrating an IC50 of 0.18 μM. The compound promotes G1 phase cell cycle arrest and triggers apoptosis, making it a valuable tool for studying cancer biology and potential therapeutic applications in CDK-related malignancies.

    1 mg
    $870.00
    5 mg
    $1,790.00
    All 3 sizes
  • NCT02
    Cat. No.
    A30493

    NCT02

    NCT02 is a molecular glue degrader that targets CDK12 through the E3 ubiquitin ligase DDB1, resulting in the ubiquitination and subsequent proteasomal degradation of its partner protein CCNK. This mechanism leads to the downregulation of CDK12, inhibiting its downstream signaling pathways. NCT02 exhibits significant biological activity by inducing apoptosis in tumor cells, arresting the cell cycle, and selectively inhibiting the proliferation of colorectal cancer cells with TP53 mutations or belonging to the CMS4 molecular subtype. Additionally, NCT02 demonstrates potential in suppressing tumor growth in both in vitro and in vivo models.

    2 mg
    $50.00
    5 mg
    $100.00
    All 6 sizes
  • CPD-10
    Cat. No.
    A30620

    CPD-10

    CPD-10 is a targeted CCND1 and CDK4 PROTAC degrader that effectively promotes the degradation of these proteins. Exhibiting significant anti-proliferative activity, CPD-10 induces apoptosis in cancer cell lines. It decreases the expression levels of cyclin D1, cyclin D3, CDK4, and phosphorylated Rb at serines 5807 and 811 in a dose-dependent manner, making it a valuable tool for research in cancer biology and therapeutic applications targeting cell cycle regulation.

    1 mg
    $480.00
    5 mg
    $1,230.00
    All 5 sizes
  • HEMTAC CDK4/6 degrader 1
    Cat. No.
    A30747

    HEMTAC CDK4/6 degrader 1

    HEMTAC CDK4/6 degrader 1 is a PROTAC designed to target CDK4 and CDK6 through a dual-ligand approach involving HSP90. This compound effectively induces the degradation of CDK4/6 in B16F10 melanoma cells, leading to cell cycle arrest at the G0/G1 phase and subsequent apoptosis. It serves as a vital tool for cancer research, particularly in elucidating mechanisms of CDK4/6 regulation and their role in tumor progression. Additionally, HEMTAC CDK4/6 degrader 1 features an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds for advanced applications in chemical biology.

    5 mg
    $615.00
    10 mg
    $1,010.00
    All 4 sizes
  • LL-K9-3
    Cat. No.
    A30989

    LL-K9-3

    LL-K9-3 is a small-molecule degrader specifically targeting the CDK9-cyclin T1 complex. This compound exhibits significant anti-proliferative and pro-apoptotic activities, effectively inhibiting downstream signaling pathways associated with CDK9 and androgen receptor (AR). LL-K9-3 is particularly relevant for research involving oncogenic transcriptional programs driven by AR and Myc, making it a valuable tool in cancer studies.

    1 mg
    $265.00
    5 mg
    $765.00
    All 2 sizes
  • LA-CB1
    Cat. No.
    A31180

    LA-CB1

    LA-CB1 is a CDK4/6 degrader that promotes the degradation of cyclin-dependent kinases 4 and 6 through the ubiquitin-proteasome pathway. This action disrupts the CDK4/6-Cyclin D1-Rb-E2F signaling axis, leading to G0/G1 cell cycle arrest and apoptosis. LA-CB1 demonstrates potent anti-proliferative effects against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In models of triple-negative breast cancer, LA-CB1 significantly inhibits tumor growth in a dose-dependent manner, making it a valuable compound for research in breast cancer therapeutics.

    5 mg
    $330.00
    10 mg
    $545.00
    All 4 sizes
  • PROTAC CDK4/6/9 degrader 1
    Cat. No.
    A32667

    PROTAC CDK4/6/9 degrader 1

    PROTAC CDK4/6/9 Degrader 1 is a targeted protein degradation agent that specifically degrades cyclin-dependent kinases CDK4, CDK6, and CDK9. This compound effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells by inducing G1 phase arrest, promoting apoptosis, and suppressing cellular migration and invasion. PROTAC CDK4/6/9 Degrader 1 serves as a valuable tool for studying the role of these kinases in TNBC and may support the development of novel therapeutic strategies aimed at this aggressive cancer subtype.

    Out of stock

    All 3 sizes
  • PROTAC CDK9 degrader-12
    Cat. No.
    A38459

    PROTAC CDK9 degrader-12

    PROTAC CDK9 degrader-12 is a selective CDK9 degrader that utilizes the E3 ubiquitin ligase-mediated proteasomal pathway for the degradation of CDK9, exhibiting a DC50 of 23 nM. This compound effectively inhibits CDK9-mediated transcriptional elongation of HIV-1, subsequently reducing HIV-1 RNA synthesis. PROTAC CDK9 degrader-12 is designed for research applications focused on HIV-1 infection and the study of transcriptional regulation.

    Out of stock

    All 3 sizes
  • TR-213
    Cat. No.
    A38460

    TR-213

    TR-213 is a potent molecular glue degrader that specifically targets Cyclin K (CDK). At a concentration of 1 μM, TR-213 demonstrates a significant inhibition of CDK12 and Cyclin levels, leading to decreases of 91% and 56%, respectively. This compound effectively inhibits RNA polymerase II activity and modulates alternative polyadenylation (APA), making it a valuable tool for cancer research and investigations into CDK-related pathways.

    Out of stock

    All 3 sizes
  • CDK9 autophagic degrader 1
    Cat. No.
    A46129

    CDK9 autophagic degrader 1

    CDK9 autophagic degrader 1 is a selective autophagic degrader targeting cyclin-dependent kinase 9 (CDK9). This compound effectively degrades CDK9, leading to a significant reduction in associated Cyclin T1 levels. Demonstrating over 80% inhibition of CDK9 at a concentration of 100 nM, this reagent serves as a valuable tool for research applications focused on transcriptional regulation and cancer biology.

    Out of stock

    All 3 sizes
  • KI-CDK9d-32
    Cat. No.
    A53679

    KI-CDK9d-32

    KI-CDK9d-32 is a selective and potent degrader designed to target CDK9 through a PROTAC mechanism (DC50: 0.89 nM). It facilitates the ubiquitination and subsequent degradation of CDK9, effectively inhibiting the MYC signaling pathway and disrupting nucleolar homeostasis. This compound demonstrates significant anticancer activity, particularly against acute lymphoblastic leukemia and pancreatic cancer, making it a valuable tool for research in cancer biology and therapeutic development.

    1 mg
    $360.00
    5 mg
    $900.00
    All 5 sizes
  • HQ461
    Cat. No.
    A54134

    HQ461

    HQ461 is a molecular glue that facilitates the interaction between CDK12 and DDB1, leading to the targeted degradation of cyclin K. This degradation impairs CDK12 function, which in turn results in reduced phosphorylation of CDK12 substrates, downregulation of DNA damage response genes, and induces apoptosis in affected cells. HQ461 is a valuable tool for research applications focused on the modulation of cell cycle regulation and the DNA damage response pathway.

    1 mg
    $30.00
    2 mg
    $45.00
    All 8 sizes
  • CPD-39
    Cat. No.
    A54145

    CPD-39

    CPD-39 is a potent heterobifunctional PROTAC degrader that targets CCND1 and CDK4. This compound effectively induces the degradation of these proteins, demonstrating significant anti-proliferative activity. CPD-39 is intended for research applications focusing on the modulation of cell cycle regulation and cancer therapeutics.

    5 mg
    $575.00
    10 mg
    $945.00
    All 4 sizes
  • CDK2 degrader 6
    Cat. No.
    A54150

    CDK2 degrader 6

    CDK2 degrader 6 is a potent CDK2 molecular glue degrader that functions through binding to cereblon and CDK2, leading to the ubiquitination and proteasomal degradation of CDK2. With a DC50 of 46.5 nM, it effectively modulates the cell cycle and reduces proliferation in breast cancer cells. Additionally, CDK2 degrader 6 demonstrates in vivo antitumor activity in gastric cancer mouse models, making it a valuable tool for research into breast and gastric cancers.

    1 mg
    $705.00
    5 mg
    $1,805.00
    All 3 sizes
  • CDK2 degrader 3
    Cat. No.
    A54164

    CDK2 degrader 3

    CDK2 Degrader 3 is a selective degrader of cyclin-dependent kinase 2 (CDK2) that promotes degradation of the target protein. This compound induces G1 cell cycle arrest specifically in CCNE1-amplified cancer cells, making it a valuable tool for studying cell cycle regulation. CDK2 Degrader 3 is particularly relevant for research applications related to breast cancer.

    1 mg
    $1,480.00
    5 mg
    $3,115.00
    All 2 sizes
  • JWZ-5-13
    Cat. No.
    A54165

    JWZ-5-13

    JWZ-5-13 is a potent CDK7 PROTAC degrader that selectively targets cyclin-dependent kinase 7 for ubiquitin-proteasome system-mediated degradation. It exhibits significant antiproliferative effects on various cancer cell lines, making it an essential tool for studying pathways involved in malignancies such as ovarian cancer, diffuse large B-cell lymphoma, acute T-lymphoblastic leukemia, and non-small cell lung cancer. This compound facilitates the exploration of targeted protein degradation in cancer biology, offering insights into therapeutic strategies.

    5 mg
    $715.00
    10 mg
    $1,170.00
    All 5 sizes
  • TMX-2172
    Cat. No.
    A54174

    TMX-2172

    TMX-2172 is a selective bivalent PROTAC that targets CDK2 and CDK5, inducing their proteasomal degradation with IC50 values of 6.5 nM and 6.8 nM, respectively. This compound demonstrates notable selectivity for CDK2 and CDK5, while sparing other cyclin-dependent kinases such as CDK1, CDK4, CDK6, CDK7, and CDK9. TMX-2172 effectively inhibits the enzymatic activity of CDK2 and CDK5, leading to a reduction in ASCL1 protein levels, induction of cancer cell death, and antiproliferative effects. This reagent is applicable in research focused on ovarian cancer and small cell lung cancer.

    1 mg
    $495.00
    5 mg
    $1,010.00
    All 5 sizes
  • BSJ-5-63
    Cat. No.
    A54175

    BSJ-5-63

    BSJ-5-63 is a potent PROTAC degrader targeting CDK12, CDK7, and CDK9. It effectively reduces protein expression levels of these kinases as well as RNAPII and Cyclin K, resulting in decreased mRNA expression of BRCA1 and BRCA2. This compound exhibits significant anticancer activity and is particularly relevant for research focused on prostate cancer.

    5 mg
    $160.00
    10 mg
    $230.00
    All 5 sizes
  • CDK2 degrader 5
    Cat. No.
    A54177

    CDK2 degrader 5

    CDK2 Degrader 5 is a targeted degrader for cyclin-dependent kinase 2 (CDK2), achieving a maximum degradation (Dmax) of over 50% and up to 80% in the HiBiT Assay. This compound is integral for probing CDK2's role in cell cycle regulation and cancer biology, making it a valuable tool for researchers investigating therapeutic strategies in oncology. Its selective degradation mechanism allows for a deeper understanding of CDK2 functions in various cellular contexts.

    1 mg
    $70.00
    5 mg
    $180.00
    All 6 sizes
  • ZLC491
    Cat. No.
    A54184

    ZLC491

    ZLC491 is a PROTAC degrader that selectively targets CDK12 and CDK13, utilizing cereblon- and proteasome-dependent mechanisms for degradation. This compound effectively inhibits the transcription and expression of long genes, particularly those involved in DNA damage response pathways. ZLC491 demonstrates anti-proliferative effects in various triple-negative breast cancer cell lines, making it a valuable tool for research into targeted therapies for this aggressive cancer subtype.

    5 mg
    $295.00
    10 mg
    $505.00
    All 5 sizes
  • CDK2 degrader 7
    Cat. No.
    A54188

    CDK2 degrader 7

    CDK2 Degrader 7 is an orally active compound that targets cyclin-dependent kinase 2 (CDK2) for selective degradation. It exhibits effective biological activity with DC50 values of 13 nM in MKN1 cells and 17 nM in TOV21G cells, leading to G1 phase arrest in MKN1 cells. Additionally, CDK2 Degrader 7 demonstrates efficacy in achieving tumor stasis in xenograft models of HCC1569 with CCNE1 amplification. This reagent is valuable for investigating the therapeutic potential in CCNE1-amplified cancers.

    1 mg
    $260.00
    5 mg
    $670.00
    All 5 sizes
  • CDK2 degrader 2
    Cat. No.
    A54195

    CDK2 degrader 2

    CDK2 Degrader 2 is a potent PROTAC targeting cyclin-dependent kinase 2 (CDK2), facilitating its degradation in MKN1 cells with a DC50 value of less than 100 nM. This compound employs a novel design, integrating a ligand for the target protein along with a linker and a ligand for the E3 ligase cereblon (CRBN). CDK2 Degrader 2 is valuable for research applications focused on the regulation of cell cycle progression and the exploration of targeted protein degradation mechanisms.

    1 mg
    $1,105.00
    5 mg
    $2,460.00
    All 3 sizes
  • CDK2 degrader 4
    Cat. No.
    A54198

    CDK2 degrader 4

    CDK2 Degrader 4 is a selective degrader that targets cyclin-dependent kinase 2 (CDK2). This compound promotes the degradation of CDK2, thereby inhibiting its activity in cell cycle regulation. CDK2 Degrader 4 is significant for cancer research, providing insights into CDK2's role in tumor growth and proliferation. Its application can aid in the development of targeted therapies for CDK2-dependent malignancies.

    1 mg
    $415.00
    5 mg
    $1,065.00
    All 4 sizes
  • PROTAC CDK9 degrader-9
    Cat. No.
    A54207

    PROTAC CDK9 degrader-9

    PROTAC CDK9 degrader-9 is a selective and potent degrader designed to target cyclin-dependent kinase 9 (CDK9) via PROTAC technology. This compound facilitates the targeted degradation of CDK9, thereby modulating transcriptional regulation and influencing cell proliferation. It is particularly useful in anti-cancer research, where the inhibition of CDK9 can lead to suppression of oncogenic pathways.

    1 mg
    $415.00
    5 mg
    $1,065.00
    All 5 sizes

Items 26-50 of 67

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