CDK

Cat. No.

A54216

CAS No.

2435721-30-3

PROTAC CDK9 degrader-2

PROTAC CDK9 degrader-2, a selective degrader of cyclin-dependent kinase 9 (CDK9), utilizes a PROTAC mechanism involving a natural product ligand, Wogonin, which targets the ubiquitin E3 ligase Cereblon (CRBN). With an IC50 of 17 μM in MCF-7 cell lines, this compound demonstrates potent activity in the degradation of CDK9, making it a valuable reagent for research applications focused on CDK9-related pathways in cancer biology and therapeutic development.

Cat. No.

A54233

CAS No.

3083777-50-5

(R)-CDK2 degrader 6

(R)-CDK2 Degrader 6 is a cereblon-based molecular glue degrader specifically targeting cyclin-dependent kinase 2 (CDK2). It functions by inducing ubiquitination and subsequent proteasomal degradation of CDK2, with a DC50 value of 27 nM. This compound is suitable for cancer research applications, providing a valuable tool for studying CDK2-related pathways and therapeutic interventions.

Cat. No.

A54239

CAS No.

2935587-90-7

PROTAC CDK9 degrader-7

PROTAC CDK9 degrader-7 is a designed degradate that specifically targets cyclin-dependent kinase 9 (CDK9). This compound facilitates the degradation of CDK9 through the proteasomal pathway, effectively reducing its cellular levels. Its biological activity makes it a valuable tool for research applications focused on investigating CDK9's role in transcription regulation and its implications in cancer therapy.

Cat. No.

A54257

CAS No.

3083777-51-6

(S)-CDK2 degrader 6

(S)-CDK2 degrader 6 selectively targets cyclin-dependent kinase 2 (CDK2) as a molecular glue degrader. With a DC50 of 166.7 nM over 24 hours, this compound effectively promotes the degradation of CDK2, thereby modulating cell cycle progression. It holds significant potential for applications in breast cancer research, enabling the exploration of therapeutic strategies that involve the regulation of CDK2 activity.

Cat. No.

A54260

CAS No.

3068546-95-9

DS17

DS17 is a molecular glue that functions as a potent degrader of cyclin K, exhibiting an EC50 value of 13 nM. This compound is pivotal for cancer research due to its ability to modulate cell cycle dynamics and influence tumor progression. Researchers can utilize DS17 to investigate the therapeutic potential of targeting cyclin K in various malignancies.

Cat. No.

A54320

CAS No.

3039540-19-4

PROTAC CDK9 degrader-11

PROTAC CDK9 degrader-11 is an orally active PROTAC degrader that specifically targets CDK9, demonstrating a DC50 value of 1.09 nM. This compound shows cytotoxicity in various small cell lung cancer cell lines with an IC50 in the nanomolar range. PROTAC CDK9 degrader-11 effectively induces cell cycle arrest at the G0/G1 phase and reduces invasion in DMS114 and DMS53 cells. Additionally, it exhibits significant antitumor efficacy in NCI-H446 xenograft mouse models, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A54326

CAS No.

1670273-47-8

[pThr3]-CDK5 Substrate

[pThr3]-CDK5 Substrate is a specific substrate for cyclin-dependent kinase 5 (CDK5), functioning primarily through phosphorylation at threonine 3. This substrate is based on the histone H1 peptide sequence, which effectively binds within the active site of CDK5. It is phosphorylated by CDK5 with a Km value of 6 µM, making it useful for studies examining CDK5 activity and regulation in various biological contexts.

Cat. No.

A54335

CAS No.

2489241-16-7

CST651

Synonyms: PROTAC CDK4/6 degrader 34

CST651 is a selective proteolysis-targeting chimera (PROTAC) degrader specifically designed to target cyclin-dependent kinases CDK4 and CDK6. This compound effectively degrades CDK4 and CDK6 in MM.1S cells, exhibiting DC50 values of 20 nM and 5.1 nM, respectively. CST651 demonstrates the ability to inhibit cancer cell proliferation and migration, making it a valuable tool for research into various cancers, including acute lymphoblastic leukemia.

Cat. No.

A54343

CAS No.

3099145-52-2

CDK2 degrader 8

CDK2 Degrader 8 is a novel chemical probe designed to target and degrade cyclin-dependent kinase 2 (CDK2). By specifically modulating CDK2 levels, it demonstrates significant anti-tumor activity, making it a valuable tool for investigating solid tumors such as breast cancer and ovarian serous cystadenocarcinoma, as well as liquid tumors like diffuse large B-cell lymphoma and acute myelogenous leukemia. CDK2 Degrader 8 facilitates research into the pathological roles of CDK2 dysregulation in cancer.

Cat. No.

A54391

CAS No.

2935587-91-8

PROTAC CDK9 degrader-6

PROTAC CDK9 degrader-6 is a proteolysis-targeting chimera (PROTAC) designed to specifically target and degrade cyclin-dependent kinase 9 (CDK9) through the ubiquitin-proteasome system. This compound effectively induces the degradation of CDK9, exhibiting DC50 values of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively. It is useful in research applications investigating the modulation of transcriptional regulation and the therapeutic potential in cancers driven by aberrant CDK9 activity.

Cat. No.

A54425

CAS No.

2994191-89-6

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.

Cat. No.

A54439

CAS No.

2541626-55-3

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.

Cat. No.

A54441

CAS No.

2935587-89-4

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.

Cat. No.

A54446

CAS No.

2488892-07-3

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.

Cat. No.

A54469

CAS No.

2411021-95-7

(R)-PROTAC CDK9 ligand-1

(R)-PROTAC CDK9 ligand-1 is a potent degrader targeting cyclin-dependent kinase 9 (CDK9), a key regulator of transcription and cell cycle progression. This compound facilitates the synthesis of PROTACs (proteolysis-targeting chimeras), which exhibit antitumor activity by promoting the degradation of CDK9. Research applications include investigations into cancer biology and therapeutic strategies aimed at modulating CDK9 levels for improved treatment outcomes.

Cat. No.

A81389

CAS No.

3094209-58-9

CDK4 degrader 1

CDK4 Degrader 1 (ML 1–71) is a molecular glue degrader that specifically targets cyclin-dependent kinase 4 (CDK4). This compound promotes the selective degradation of CDK4, leading to reduced cell proliferation and induction of cell cycle arrest in various cancer models. It serves as a valuable tool for investigating CDK4's role in tumorigenesis and for the development of targeted therapies in cancer research.

Cat. No.

A84544

CAS No.

2411021-01-5

PROTAC CDK9 degrader-4

PROTAC CDK9 degrader-4 is a potent CDK9 degradation agent that facilitates the targeted degradation of cyclin-dependent kinase 9. This compound effectively modulates transcriptional regulation by harnessing the power of PROTAC technology, leading to significant biological activity in various cellular contexts. It holds potential applications in cancer research and the study of transcriptional control mechanisms.

Cat. No.

B21941

CAS No.

3030276-48-0

PROTAC CDK2-pRb degrader-1

PROTAC CDK2-pRb degrader-1 is an orally active PROTAC that targets cyclin-dependent kinase 2 (CDK2) for degradation. This compound effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine 807/811 by promoting the ubiquitination and proteasomal degradation of CDK2. Demonstrating significant biological activity with EC50 values of 12 nM and 125 nM in human cells, PROTAC CDK2-pRb degrader-1 is particularly useful in research focused on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers, as it inhibits tumor growth and induces tumor stasis in xenograft models.