CDK

Cat. No.

A30629

CAS No.

1805833-75-3

Samuraciclib

Synonyms: CT7001; ICEC0942

Samuraciclib is a selective, ATP-competitive inhibitor of CDK7, exhibiting an IC50 of 41 nM. This compound demonstrates significant selectivity over CDK1, CDK2, CDK5, and CDK9, with fold selectivities of 45, 15, 230, and 30, respectively. Samuraciclib effectively inhibits the proliferation of breast cancer cell lines, with GI50 values ranging from 0.2 to 0.3 μM, indicating its potential as an effective therapeutic agent in oncology research.

Cat. No.

A30676

CAS No.

1983984-01-5

Avotaciclib trihydrochloride

Synonyms: BEY1107 trihydrochloride

Avotaciclib trihydrochloride is an orally active inhibitor of cyclin-dependent kinase 1 (CDK1). This compound has demonstrated the ability to inhibit tumor cell proliferation and induce apoptosis, making it a valuable tool for cancer research. Avotaciclib trihydrochloride is particularly relevant for studies focused on pancreatic and lung cancers.

Cat. No.

A30699

CAS No.

3002399-75-6

CDK4-IN-3

CDK4-IN-3 is a potent irreversible inhibitor of cyclin-dependent kinase 4 (CDK4), exhibiting an IC50 of 25 nM and demonstrating over 10-fold selectivity for CDK4 compared to CDK6. This compound effectively arrests the cell cycle in the G₁ phase, leading to the induction of apoptosis in tumor cells. CDK4-IN-3 is valuable for research applications focused on solid tumors, including breast and lung cancers.

Cat. No.

A30746

CAS No.

190653-73-7

CGP-74514

CGP-74514 is a potent and selective inhibitor of cyclin-dependent kinase 1 (CDK1), exhibiting an IC50 of 25 nM. By targeting the CDK1/cyclin B complex, CGP-74514 effectively halts the cell cycle at the G2/M phase and triggers apoptosis in tumor cells. This compound is particularly valuable for research focused on bladder cancer and related therapeutic applications.

Cat. No.

A30792

CAS No.

2369981-71-3

CDK9-IN-7

CDK9-IN-7 is a selective and potent inhibitor of cyclin-dependent kinase 9 (CDK9), demonstrating an IC50 of 11 nM. This compound selectively inhibits CDK9 over other cyclin-dependent kinases, such as CDK4 and CDK6, with IC50 values of 148 nM and 145 nM, respectively. CDK9-IN-7 exhibits significant antitumor activity, inducing apoptosis in non-small cell lung cancer (NSCLC) cells, arresting the cell cycle in the G2 phase, and reducing the stemness characteristics of NSCLC. It is a valuable tool for research into cancer biology and potential therapeutic applications.

Cat. No.

A30892

CAS No.

486414-35-1

AG-012986

AG-012986 is a potent pan-CDK inhibitor targeting multiple cyclin-dependent kinases including CDK1, CDK2, CDK4, CDK5, CDK6, and CDK9. It demonstrates significant biological activity with Kis of 9.2 nM for CDK4/cyclin, 44 nM for CDK1/cyclin B, and 94 nM for CDK2/cyclin A, alongside IC50 values of 4 nM for CDK9/cyclin T and 22 nM for CDK5/p35. AG-012986 effectively inhibits cell proliferation in cancer cell lines, inducing cell cycle arrest and apoptosis, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A31040

CAS No.

2677026-15-0

CDK6/PIM1-IN-1 hydrochloride

CDK6/PIM1-IN-1 hydrochloride is a potent dual inhibitor targeting CDK6 and PIM1, exhibiting IC50 values of 39 nM and 88 nM, respectively, along with significant inhibition of CDK4 (IC50=3.6 nM). This compound effectively inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 hydrochloride is a valuable tool for research investigating the role of CDK6 and PIM1 in cancer biology, particularly in the context of AML.

Cat. No.

A31101

CAS No.

2459916-56-2

CDK1/Cyc B-IN-1

CDK1/Cyc B-IN-1 is a selective inhibitor of the CDK1/cyclin B complex, demonstrating an IC50 of 97 nM. This compound effectively induces apoptosis and facilitates G2/M phase cell cycle arrest, making it a valuable tool for studying cell proliferation. CDK1/Cyc B-IN-1 exhibits broad-spectrum cytotoxic activity against various cancer cell lines, supporting its potential in cancer research applications.

Cat. No.

A31113

CAS No.

784211-09-2

RGB-286147

RGB-286147 is a selective ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and CDK-related kinases (CRKs), exhibiting IC50 values between 9 to 839 nM. This compound demonstrates minimal activity against non-CDK/CRK kinases. RGB-286147 induces apoptosis in cancer cells and shows significant anti-tumor effects, making it a valuable tool for research in cancer biology and therapeutic development targeting CDK pathways.

Cat. No.

A31329

CAS No.

2677026-14-9

CDK6/PIM1-IN-1

CDK6/PIM1-IN-1 is a potent dual inhibitor targeting CDK6 and PIM1, with IC50 values of 39 nM and 88 nM, respectively, and an additional inhibition of CDK4 at an IC50 of 3.6 nM. This reagent significantly inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 demonstrates strong anti-AML activity, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A31491

CAS No.

137254-39-8

1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC

Synonyms: PC(18:0/22:4)

1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC is a cyclin-dependent kinase (CDK) inhibitor that plays a crucial role in cancer research. This compound induces apoptosis and effectively inhibits the proliferation of a variety of cancer cell lines, making it a valuable tool for studying cancer biology and therapeutic responses. Its ability to impact CDK activity provides insights into cell cycle regulation and potential cancer treatment strategies.

Cat. No.

A31534

CAS No.

2418559-01-8

HDAC1/2 and CDK2-IN-1

HDAC1/2 and CDK2-IN-1 is a dual inhibitor targeting HDAC1, HDAC2, and CDK2, with IC50 values of 70.7 μM, 23.1 μM, and 0.80 μM, respectively. This compound effectively disrupts the cell cycle and promotes apoptosis in tumor cells, demonstrating significant in vivo antitumor activity. It is suitable for research applications focused on cancer biology and therapeutic interventions targeting histone deacetylases and cyclin-dependent kinases.

Cat. No.

A31560

CAS No.

2841473-39-8

ZLMT-12

ZLMT-12 is a potent CDK2/9 inhibitor, demonstrating IC50 values of 0.002 μM and 0.011 μM against CDK9 and CDK2, respectively. This compound is derived from tacrine and exhibits weak inhibition of acetylcholinesterase (IC50 = 19.023 μM) and butyrylcholinesterase (IC50 = 2.768 μM). ZLMT-12 is characterized by low toxicity and notable antiproliferative activity, effectively inducing apoptosis and facilitating cell cycle arrest in the S and G2/M phases. This compound serves as a valuable tool for research in cell cycle regulation and therapeutic development in cancer biology.

Cat. No.

A31632

CAS No.

3040999-70-7

CDK7-IN-30

CDK7-IN-30 is a potent CDK7 inhibitor with an IC50 value of 7.21 nM, targeting the phosphorylation of RNA Polymerase II and CDK2. This compound demonstrates significant pro-apoptotic effects and exhibits anti-cancer activity, making it a valuable tool for cancer research. Its mechanism of action offers insights into cell cycle regulation and transcriptomic processes, facilitating the exploration of therapeutic strategies in oncology.

Cat. No.

A31633

CAS No.

1628314-13-5

A-1592668

A-1592668 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), which plays a critical role in transcriptional regulation. This compound induces apoptosis in various cancer cell lines and demonstrates synergistic effects when combined with Venetoclax, effectively inhibiting the growth of Jeko-1 tumors. A-1592668 is a valuable tool for research in cancer biology and therapeutic development targeting CDK9 pathways.

Cat. No.

A31644

CAS No.

3036645-03-8

BC13

BC13 is a selective inhibitor of CDK6 and BRD4, demonstrating IC50 values of 234 nM and 36 nM, respectively. This compound exhibits notable antiproliferative effects, facilitating cell apoptosis and inducing DNA damage in various cell lines. Additionally, BC13 has been shown to elevate reactive oxygen species (ROS) levels, making it a valuable tool for research in cancer biology and therapeutic development targeting cell cycle regulation.

Cat. No.

A31716

CAS No.

2987905-95-1

HDAC1/CDK7-IN-1

HDAC1/CDK7-IN-1 is a dual inhibitor targeting HDAC1 and CDK7, exhibiting IC50 values of 893 nM and 248 nM, respectively. This compound effectively inhibits the proliferation of cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis specifically in HCT-116 cells, while also disrupting their migratory capacity. These properties make it a valuable tool for cancer research, particularly in exploring therapeutic strategies that target epigenetic regulation and cell cycle dynamics.

Cat. No.

A31886

CAS No.

2228039-87-8

Otviciclib

Otviciclib is a potent cyclin-dependent kinase (CDK) inhibitor that demonstrates significant anti-proliferative effects against various solid tumor cell lines, including HCT116, NCIH82, and DU145. This compound effectively induces cell cycle arrest in the G2/M phase and triggers apoptosis, exhibiting a favorable toxicity profile towards normal cells. Otviciclib shows broad-spectrum anticancer activity, making it a valuable tool for research applications related to colon, pancreatic, and lung cancers.

Cat. No.

A31948

CAS No.

2197029-81-3

CDK9/HDAC1/HDAC3-IN-1

CDK9/HDAC1/HDAC3-IN-1 is a dual inhibitor targeting CDK9 and HDACs. With IC50 values of 0.17 μM for CDK9, 1.73 μM for HDAC1, and 1.11 μM for HDAC3, this compound effectively disrupts the activity of these proteins. It induces cancer cell apoptosis and causes cell cycle arrest at the G2/M phase. Additionally, CDK9/HDAC1/HDAC3-IN-1 exhibits broad-spectrum anti-cancer effects, demonstrating efficacy against various malignancies, including breast, cervical, and liver cancers, as evidenced in murine TNBC MDA-MB-231 xenograft models.

Cat. No.

A31959

CAS No.

2919216-33-2

CDK2-IN-9

CDK2-IN-9 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.63 µM. This compound demonstrates significant antiproliferative activity, inducing apoptosis and causing cell cycle arrest at the S and G2/M phases. CDK2-IN-9 is suitable for research applications focused on melanoma and the exploration of CDK2's role in cell cycle regulation and cancer biology.

Cat. No.

A32054

CAS No.

186692-44-4

(Rac)-Roscovitine

Synonyms: (Rac)-Seliciclib; (Rac)-CYC202

(Rac)-Roscovitine is a selective inhibitor of cyclin-dependent kinases (CDKs), functioning by competitively binding to their active sites in place of ATP. This mechanism effectively inhibits CDK phosphorylation activity, leading to apoptosis in cancer cells. As a valuable research tool, (Rac)-Roscovitine is applicable in studies of cancer and various conditions associated with CDK dysregulation, including neurodegenerative diseases, cardiac disorders, and chronic inflammation.

Cat. No.

A32097

CAS No.

2580938-58-3

CDK/HDAC-IN-2

CDK/HDAC-IN-2 is a dual inhibitor of histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs), exhibiting IC50 values of 6.4 nM for HDAC1, 0.25 nM for HDAC2, 45 nM for HDAC3, and >1000 nM for HDAC6,8, as well as 8.63 nM for CDK1, 0.30 nM for CDK2, and >1000 nM for CDK4,6,7. This compound demonstrates significant antiproliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. CDK/HDAC-IN-2 is particularly valuable in cancer research due to its potent antitumor efficacy.

Cat. No.

A32102

CAS No.

1804127-83-0

CDK9-IN-18

CDK9-IN-18 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), effectively obstructing its phosphorylation activity. This compound demonstrates significant anticancer properties, promoting apoptosis in various cancer cell lines while exhibiting low cellular toxicity. Its mechanism of action makes CDK9-IN-18 a valuable tool for research into cancer therapeutics and the regulation of gene expression.

Cat. No.

A32109

CAS No.

2851977-85-8

ZLHQ-5f

ZLHQ-5f is a dual inhibitor of Cyclin-dependent kinase 2 (CDK2) and Topoisomerase I (Topo I), exhibiting an IC50 of 0.145 μM against CDK2/CycA2. This compound effectively induces S-phase cell cycle arrest and triggers apoptosis in HCT116 cancer cells. Its favorable safety profile supports its potential applications in cancer research and therapeutic development.

Cat. No.

A32154

CAS No.

2222285-23-4

CDK2/9-IN-1

CDK2/9-IN-1 is an orally active dual inhibitor targeting cyclin-dependent kinases CDK2 and CDK9, with IC50 values of 0.004 μM and 0.009 μM, respectively. This compound induces apoptosis through G2/M cell cycle arrest, demonstrating notable antitumor activity. CDK2/9-IN-1 is useful for research applications focused on cancer biology and the modulation of cell cycle regulation.