CDK

Cat. No.

A54271

CAS No.

1831842-69-3

Palbociclib dihydrochloride

Synonyms: PD-0332991 dihydrochloride

Palbociclib dihydrochloride is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6) with IC50 values of 11 nM and 16 nM, respectively. This compound exhibits significant anti-proliferative effects and induces cell cycle arrest in various cancer cell lines. It is particularly relevant for research applications in hormone receptor-positive and HER2-negative breast cancer, as well as hepatocellular carcinoma, providing insights into tumor growth regulation and potential therapeutic strategies.

Cat. No.

A54272

CAS No.

2757498-64-7

Palbociclib orotate

Synonyms: PD 0332991 orotate

Palbociclib orotate is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), demonstrating IC50 values of 11 nM and 16 nM, respectively. This compound exhibits significant anti-proliferative activity, effectively inducing cell cycle arrest in cancer cells. Palbociclib orotate is primarily utilized in research focused on HR-positive and HER2-negative breast cancer as well as hepatocellular carcinoma, making it a valuable tool for understanding therapeutic strategies in these malignancies.

Cat. No.

A54273

CAS No.

3032997-20-6

CDK1-IN-5

CDK1-IN-5 is a selective inhibitor of cyclin-dependent kinase 1 (CDK1), demonstrating IC50 values of 42.19 nM for CDK1, 188.71 nM for CDK2, and 354.15 nM for CDK5. By targeting CDK1, this compound effectively disrupts cell cycle progression and inhibits the growth of cancer cells. CDK1-IN-5 is valuable for research applications focused on cancer biology and therapeutic strategies against tumor proliferation.

Cat. No.

A54274

CAS No.

2202767-78-8

Cimpuciclib

Cimpuciclib is a selective inhibitor of cyclin-dependent kinase 4 (CDK4), exhibiting an IC50 value of 0.49 nM. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research. Its inhibition of CDK4 disrupts cell cycle progression, thus providing insights into therapeutic strategies for tumors driven by CDK4 dysregulation.

Cat. No.

A54276

CAS No.

3032997-12-6

CDK1-IN-3

CDK1-IN-3 is a selective inhibitor of Cyclin-dependent kinase 1 (CDK1), exhibiting IC50 values of 36.8 nM, 305.17 nM, and 369.37 nM for CDK1, CDK2, and CDK5, respectively. This compound effectively disrupts the cell cycle, leading to inhibition of cancer cell proliferation. CDK1-IN-3 is valuable for research applications targeting cancer biology and therapeutic development in oncology.

Cat. No.

A54277

CAS No.

2531743-46-9

GDC-4198

Synonyms: RGT-419B

GDC-4198 is an orally active inhibitor of cyclin-dependent kinases 4 and 2 (CDK4/2), exhibiting selective activity against kinases such as CDK6, CDK9, and GSK3β. By inhibiting cyclin-CDK complexes, GDC-4198 effectively blocks the phosphorylation of retinoblastoma protein (pRb), thus halting the cell cycle progression from the G1 to S phase. This compound is a valuable tool for investigating various cancers, particularly breast cancer (especially hormone receptor-positive, HER2-negative), lung cancer, and colorectal cancer.

Cat. No.

A54278

CAS No.

2326428-24-2

CDK7-IN-2 hydrochloride hydrate

CDK7-IN-2 hydrochloride hydrate is a selective inhibitor of cyclin-dependent kinase 7 (CDK7). This compound demonstrates significant anti-cancer activity by inhibiting CDK7, which is crucial for cell cycle regulation and transcriptional control. CDK7-IN-2 is primarily used in cancer research to explore its therapeutic potential in various malignancies and to investigate CDK-driven signaling pathways.

Cat. No.

A54279

CAS No.

1883548-83-1

BS-181 dihydrochloride

BS-181 dihydrochloride is a highly selective inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 of 21 nM, showcasing superior potency compared to alternative compounds. It also exhibits moderate inhibition against CDK2, CDK5, and CDK9, with IC50 values of 880 nM, 3000 nM, and 4200 nM, respectively. BS-181 dihydrochloride has demonstrated the ability to inhibit the growth of various cancer cell lines (IC50 range of 11.5 μM to 37.3 μM) and to induce apoptosis. This compound is valuable for research applications focused on cancer therapies targeting CDK pathways.

Cat. No.

A54280

CAS No.

2366237-37-6

CDK4/6-IN-3

CDK4/6-IN-3 is a potent inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6), demonstrating Ki values of less than 0.3 nM and 2.2 nM, respectively. This compound also exhibits inhibitory activity against CDK1 with a Ki of 110 nM. Its ability to penetrate the blood-brain barrier makes CDK4/6-IN-3 a valuable candidate for research into glioblastoma therapies and other malignancies driven by dysregulated cell cycle progression.

Cat. No.

A54282

CAS No.

2246956-84-1

CDK9-IN-9

CDK9-IN-9 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 1.8 nM. This compound also demonstrates some activity against CDK2, with an IC50 of 155 nM. CDK9-IN-9 has been shown to possess anti-cancer properties, making it a valuable tool for research applications focused on cancer biology and therapeutic development targeting transcriptional regulation mechanisms.

Cat. No.

A54284

CAS No.

2414896-32-3

CDK7-IN-11

CDK7-IN-11 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating a high inhibitory activity with an IC50 value of 4.2 nM. This compound is suitable for in-depth research into diseases linked to CDK7 activity, providing valuable insights into its role in cell cycle regulation and transcriptional control. CDK7-IN-11 can aid in the exploration of therapeutic strategies targeting CDK7 in various malignancies and other pathological conditions.

Cat. No.

A54285

CAS No.

2737262-24-5

CDK9-IN-29

CDK9-IN-29 is a highly selective inhibitor of Cyclin-dependent kinase 9 (CDK9) with an IC50 value of 3.20 nM. This compound effectively hinders cell proliferation and promotes apoptosis in various cellular models. CDK9-IN-29 is suitable for research focused on cancer biology, particularly studies investigating transcriptional regulation and cell cycle dynamics.

Cat. No.

A54286

CAS No.

1983984-11-7

Tanuxiciclib trihydrochloride

Tanuxiciclib trihydrochloride is a potent inhibitor of cyclin-dependent kinases (CDKs), which play a crucial role in cell cycle regulation. By selectively targeting CDK activity, this compound exhibits significant potential in impeding tumor cell proliferation. It is particularly valuable for research applications in cancer biology and therapeutic development, aiding in the exploration of CDK-related pathways and their implications in oncogenesis.

Cat. No.

A54287

CAS No.

920113-02-6

Riviciclib

Synonyms: P276-00 free base

Riviciclib is a potent cyclin-dependent kinase (CDK) inhibitor that selectively targets CDK9-cyclin T1, CDK4-cyclin D1, and CDK1-cyclin B, exhibiting IC50 values of 20 nM, 63 nM, and 79 nM, respectively. This compound demonstrates significant antitumor activity, especially in cisplatin-resistant cancer cells. Riviciclib is useful for research applications focused on cell cycle regulation, cancer therapy, and the development of resistance to chemotherapeutics.

Cat. No.

A54288

CAS No.

1402057-87-7

Cdc7-IN-3

Cdc7-IN-3 is a selective inhibitor of the Cdc7 kinase, a serine-threonine protein kinase crucial for the initiation of DNA replication during the cell cycle. This compound demonstrates potent inhibitory activity against Cdc7, making it a valuable tool for studying cell proliferation and checkpoint control mechanisms. It is suitable for research applications involving cancer biology and the exploration of therapeutic strategies that target DNA replication processes.

Cat. No.

A54289

CAS No.

2414373-55-8

CDK6/9-IN-1

CDK6/9-IN-1 is a dual inhibitor of cyclin-dependent kinases 6 and 9, exhibiting IC50 values of 40.5 nM and 39.5 nM for CDK6 and CDK9, respectively. This compound demonstrates significant anti-proliferative activity, making it a valuable tool for studying cell cycle regulation and transcriptional control in various cancer models. It is particularly applicable in research focused on the therapeutic targeting of CDK pathways in oncogenesis.

Cat. No.

A54290

CAS No.

2397678-18-9

Tibremciclib

Tibremciclib is a selective inhibitor of cyclin-dependent kinase 4 (CDK4), exhibiting significant antineoplastic activity. By blocking CDK4 activity, it disrupts cell cycle progression and promotes apoptosis in cancer cells. Tibremciclib is primarily utilized in cancer research and therapeutic applications, focusing on targeting tumors driven by aberrant CDK4 signaling.

Cat. No.

A54291

CAS No.

1780390-76-2

Senexin A hydrochloride

Senexin A hydrochloride is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), with an IC50 of 280 nM for CDK8. It specifically targets and inhibits p21-induced transcription, while sparing other biological functions of p21. In addition, Senexin A hydrochloride effectively suppresses CMV-GFP induction and the p21 stimulatory activity of NF-κB-dependent promoters, making it a valuable tool for studying transcriptional regulation and cell signaling pathways.

Cat. No.

A54292

CAS No.

1402059-17-9

Cdc7-IN-7

Cdc7-IN-7 is a potent inhibitor of the Cdc7 kinase, a serine-threonine protein kinase critical for the initiation of DNA replication during the cell cycle. By selectively targeting Cdc7, this compound demonstrates significant potential in inhibiting cellular proliferation and tumor growth. Research applications include studies on cell cycle regulation, cancer biology, and potential therapeutic strategies in oncology.

Cat. No.

A54293

CAS No.

2845096-18-4

QR-6401

QR-6401 is a selective macrocyclic inhibitor of cyclin-dependent kinase 2 (CDK2), demonstrating an IC50 of 0.37 nM for CDK2/E1 and exhibiting varying activity against other CDKs. This compound shows potent antitumor efficacy in an OVCAR3 ovarian cancer xenograft model. QR-6401 is valuable for research into cancer mechanisms and potential therapeutic approaches targeting CDK2.

Cat. No.

A54294

CAS No.

2378710-04-2

CDK7-IN-6

CDK7-IN-6 is a potent and selective inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating an IC50 of less than 100 nM. This compound exhibits over 200-fold selectivity for CDK7 compared to CDK1, CDK2, and CDK5. CDK7-IN-6 is valuable for cancer research, providing a tool for investigating the role of CDK7 in cell cycle regulation and potential therapeutic strategies.

Cat. No.

A54296

CAS No.

1459216-10-4

AGM-130

AGM-130 is a selective cyclin-dependent kinase (CDK) inhibitor that interferes with cell cycle progression. It has demonstrated significant antitumor activity, making it a valuable tool for cancer research. This compound can be utilized in studies aimed at understanding CDK modulation and its potential therapeutic implications in oncology.

Cat. No.

A54297

CAS No.

2765676-32-0

CDK7-IN-16

CDK7-IN-16 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating potent activity with an IC50 range of 1 to 10 nM. This compound is primarily utilized in cancer research, particularly in studies focused on malignancies characterized by transcriptional dysregulation. Its ability to modulate CDK7 activity makes it a valuable tool for investigating therapeutic strategies in oncology.

Cat. No.

A54298

CAS No.

2415156-27-1

CDK8-IN-6

CDK8-IN-6 is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) with a Kd of 13 nM. This compound exhibits significant cytotoxic effects on various cancer cell lines, including MOLM-13, OCI-AML3, MV4-11, NRK, and H9c2, with IC50 values ranging from 7.5 to 25 µM. CDK8-IN-6 holds promise for advancing research in acute myeloid leukemia (AML) and related cancer studies, making it a valuable tool for investigating CDK8's role in tumorigenesis.

Cat. No.

A54299

CAS No.

2577288-83-4

CDK4/9-IN-1

CDK4/9-IN-1 is a selective dual inhibitor of cyclin-dependent kinases 4 and 9, exhibiting IC50 values of 23 nM for CDK4 and 12 nM for CDK9. This compound demonstrates significant potential in the study of cancer biology, particularly in elucidating the role of CDK4 and CDK9 in the cell cycle and transcription regulation. Researchers may utilize CDK4/9-IN-1 to investigate therapeutic strategies targeting these kinases in various cancer models.