CDK

Cat. No.

A33725

CAS No.

2762296-44-4

FLT3/CDK4-IN-1

FLT3/CDK4-IN-1 is a highly selective, orally active dual inhibitor targeting FLT3 and CDK4, demonstrating IC50 values of 11 nM and 7 nM, respectively. This compound exhibits significant antiproliferative activity against specific cancer cell lines and shows promising antitumor effects in vivo. FLT3/CDK4-IN-1 is suitable for research applications focused on cancer biology, particularly in exploring pathways associated with leukemias and solid tumors.

Cat. No.

A34677

CAS No.

2924036-87-1

SHP2/CDK4-IN-1

SHP2/CDK4-IN-1 is a potent dual inhibitor of SHP2 and CDK4, exhibiting IC50 values of 4.3 nM and 18.2 nM, respectively. This compound effectively induces G0/G1 phase cell cycle arrest, thereby inhibiting the proliferation of triple-negative breast cancer (TNBC) cell lines. In preclinical studies, SHP2/CDK4-IN-1 demonstrated significant antitumor efficacy in the EMT6 syngeneic mouse model, making it a valuable tool for research on TNBC.

Cat. No.

A34730

CAS No.

443798-47-8

K00546

K00546 is a highly selective inhibitor of cyclin-dependent kinases CDK1 and CDK2, exhibiting IC50 values of 0.6 nM and 0.5 nM, respectively, for CDK1/cyclin B and CDK2/cyclin A complexes. In addition, K00546 effectively inhibits CDC2-like kinases CLK1 and CLK3, with IC50 values of 8.9 nM and 29.2 nM, respectively. This compound is valuable for research focused on cell cycle regulation and the mechanistic study of kinase activity in cancer biology.

Cat. No.

A34764

CAS No.

388627-21-2

GW297361

GW297361 is an oxindole compound identified as a cyclin-dependent kinase (CDK) inhibitor with a selective action on Pho85 in cellular systems. It demonstrates significant inhibitory effects on yeast Cdk1 and Pho85, exhibiting IC50 values of 20 nM and 400 nM, respectively. This compound is valuable for research applications focused on cell cycle regulation and the study of kinase signaling pathways.

Cat. No.

A35073

CAS No.

2172559-91-8

ML 315 hydrochloride

ML 315 hydrochloride is a selective dual inhibitor targeting cyclin-dependent kinases (CDKs) and dual-specificity tyrosine-regulated kinases (DYRKs), exhibiting IC50 values of 68 nM and 282 nM, respectively. This compound is utilized in research focused on cancer and neurological diseases, providing insights into cell cycle regulation and neurodegenerative pathways. ML 315's potent inhibitory action makes it a valuable tool for studying therapeutic strategies in these critical areas.

Cat. No.

A35075

CAS No.

1364123-68-1

(R)-(+)-O-Demethylbuchenavianine

(R)-(+)-O-Demethylbuchenavianine is a selective inhibitor of Cyclin-dependent kinases (CDKs), specifically targeting CDK1 and CDK5 with IC50 values of 1.1 and 0.95 μM, respectively. Additionally, it shows inhibitory activity against glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1), and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), though with IC50 values greater than 10 μM. This compound is important for research focused on cell cycle regulation, cancer therapeutics, and neurodegenerative diseases.

Cat. No.

A35076

CAS No.

1440251-53-5

ML 315

ML 315 is a selective dual inhibitor of cyclin-dependent kinases (CDK) and dual-specificity tyrosine phosphorylation-regulated kinase (DYRK), exhibiting IC50 values of 68 nM and 282 nM, respectively. It demonstrates significant biological activity in modulating cell cycle progression and neuronal signaling pathways. This compound has applications in cancer research and the study of neurological diseases, facilitating insights into therapeutic targets within these areas.

Cat. No.

A35865

CAS No.

17413-38-6

Aristolochic acid D

Synonyms: Aristolochic acid-IVa

Aristolochic acid D is a selective inhibitor of PDE2 with an IC50 of 4.673 μM and CDK2 with an IC50 of 25 μM, derived from Aristolochia indica L. This compound demonstrates significant anti-inflammatory properties while exhibiting a non-carcinogenic and non-nephrotoxic profile. Aristolochic acid D is valuable for research applications focused on inflammation and tumor-related diseases, offering insights into therapeutic strategies.

Cat. No.

A36113

CAS No.

3068529-24-5

CDK6/9-IN-2

CDK6/9-IN-2 is a potent dual inhibitor of cyclin-dependent kinases CDK6 and CDK9, with reported IC50 values of 15 nM and 22 nM, respectively. This compound exhibits selectivity for CDK2, CDK8, and CDK11. CDK6/9-IN-2 effectively inhibits the proliferation of HaCaT cells stimulated by IFN-γ and TNF-α, while also suppressing the STAT3 signaling pathway and the expression of inflammatory factors. Its ability to alleviate psoriatic dermatitis makes CDK6/9-IN-2 valuable for research in psoriasis and related inflammatory conditions.

Cat. No.

A36199

CAS No.

2832887-40-6

M5N36

M5N36 is a selective inhibitor of Cdc25C, exhibiting IC50 values of 0.15 µM, 0.19 µM, and 0.06 µM for Cdc25A, Cdc25B, and Cdc25C, respectively. This compound demonstrates significant anti-proliferative activity and enhances the phosphorylation of CDK1 and CDK2. M5N36 is valuable for research applications targeting cell cycle regulation and cancer biology.

Cat. No.

A36239

CAS No.

134271-74-2

CDC25B-IN-2

CDC25B-IN-2 is a selective inhibitor of the cdc25B phosphatase, which plays a crucial role in regulating cell cycle progression. This compound demonstrates significant inhibitory activity, making it valuable for investigating the molecular mechanisms governing cell cycle regulation and oncogenesis. CDC25B-IN-2 is ideal for research applications focused on cancer biology and therapeutic development targeting cell cycle dysregulation.

Cat. No.

A36279

CAS No.

6541-19-1

6,7-Dichloroquinoline-5,8-dione

6,7-Dichloroquinoline-5,8-dione is a selective inhibitor of CDC25B2, demonstrating an IC50 value of 4.6 µM. This compound is valuable for investigating the role of CDC25B2 in cell cycle regulation and its implications in cancer research. Its inhibitory activity may facilitate studies aimed at understanding cancer mechanisms and developing targeted therapeutic strategies.

Cat. No.

A36507

CAS No.

2241300-50-3

AS2863619 free base

AS2863619 free base is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 0.61 nM and 4.28 nM, respectively. This compound drives the conversion of antigen-specific effector and memory T cells into Foxp3+ regulatory T (Treg) cells, thereby offering potential therapeutic approaches for various immunological conditions. The inhibition of CDK8/19 by AS2863619 enhances STAT5 activation, leading to the upregulation of the Foxp3 gene and promoting Treg cell development.

Cat. No.

A36518

CAS No.

155179-21-8

Vanicoside B

Vanicoside B is a potent inhibitor of cyclin-dependent kinase 8 (CDK8), derived from the herb Persicaria dissitiflora. This compound demonstrates significant anti-tumor activity by disrupting CDK8-mediated signaling pathways and reducing the levels of proteins associated with epithelial-mesenchymal transition. As a result, Vanicoside B induces cell cycle arrest and apoptosis, making it a valuable reagent for cancer research and therapeutic investigations targeting CDK8 pathways.

Cat. No.

A36612

CAS No.

3024381-54-9

CDK8/19-IN-2

CDK8/19-IN-2 is a potent and orally active inhibitor of cyclin-dependent kinases 8 and 19, exhibiting IC50 values of 2.08 nM and 2.49 nM, respectively. This compound is crucial for research focusing on acute myeloid leukemia (AML), breast cancer, and lymphoma, where inhibition of CDK8 and CDK19 can influence tumor proliferation and survival. Its selectivity and efficacy make it a valuable tool in studying the role of these kinases in various oncogenic pathways.

Cat. No.

A36623

CAS No.

1860885-61-5

CDK8-IN-16

CDK8-IN-16 is a potent dual inhibitor of cyclin-dependent kinases 8 and 19, demonstrating IC50 values of 5.1 nM and 5.6 nM, respectively. This compound effectively inhibits phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cells and modulates the WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cells. CDK8-IN-16 exhibits favorable pharmacokinetic properties, including an oral bioavailability of 57% in rat models, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A36888

CAS No.

1241675-76-2

(R)-DRF053 dihydrochloride

(R)-DRF053 dihydrochloride is a selective inhibitor of casein kinases 1 (CK1), CDK1/cyclin B, and CDK5/p25, exhibiting IC50 values of 14 nM, 220 nM, and 80 nM, respectively. This compound effectively inhibits the CK1-mediated generation of amyloid-beta in cellular models, making it valuable for research into neurodegenerative diseases and cellular signaling pathways. Its specificity and potency position it as a suitable reagent for investigating the roles of these kinases in various biological processes.

Cat. No.

A37028

CAS No.

1358201-44-1

P162-0948

P162-0948 is a selective inhibitor of Cyclin-Dependent Kinase 8 (CDK8), demonstrating an IC50 value of 50.4 nM. This compound effectively reduces cell migration and downregulates the expression of epithelial-mesenchymal transition (EMT)-related proteins in A549 human alveolar epithelial cells. Additionally, P162-0948 inhibits Smad phosphorylation, indicating its potential to disrupt the TGF-β/Smad signaling pathway. This makes P162-0948 a valuable tool for research focused on pulmonary fibrosis and related pathways.

Cat. No.

A37069

CAS No.

2839338-28-0

CDK8-IN-11

CDK8-IN-11 is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8), displaying an IC50 value of 46 nM. This compound effectively inhibits the WNT/β-catenin signaling pathway, making it a valuable tool for investigating the molecular mechanisms underlying oncogenesis. CDK8-IN-11 is primarily utilized in research related to colon cancer, contributing to the development of targeted therapeutic strategies.

Cat. No.

A37415

CAS No.

3065284-87-6

LCI133

LCI133 is a selective multikinase inhibitor targeting CDK4, CDK6, CDK9, and AURKA/B, exhibiting nanomolar potency (IC50 values of 4.7 nM, 10.2 nM, 4.1 nM, 2.8 nM, and 10.6 nM, respectively). It effectively induces S/G2 cell-cycle arrest and promotes significant apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. Additionally, LCI133 demonstrates notable antitumor efficacy in preclinical models, particularly in BE(2)-C neuroblastoma xenograft studies, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A37601

CAS No.

87302-58-7

DCB-3503

DCB-3503 is an allosteric modulator targeting heat shock cognate protein HSC70, functioning as an inhibitor of Cyclin D1. By allosterically modulating the ATPase and chaperone activities of HSC70, DCB-3503 effectively inhibits the translation of Cyclin D1. This compound holds potential for research applications focused on malignancies characterized by elevated Cyclin D1 expression, such as hepatocellular carcinoma and breast cancer.

Cat. No.

A37762

CAS No.

2766124-39-2

Q901

Synonyms: CDK7-IN-21

Q901 is a potent and selective CDK7 inhibitor, exhibiting an IC50 of 10 nM. It effectively disrupts the activity of MYC and E2F, making it a valuable tool for studying cellular mechanisms in various cancer types, including colon and lung cancer. This compound is suitable for research applications focused on cancer biology and therapeutic development targeting CDK7.

Cat. No.

A37848

CAS No.

1113044-49-7

FIT-039

FIT-039 is a selective CDK9 inhibitor that acts as an ATP-competitive antagonist, exhibiting an IC50 of 5.8 μM against the CDK9/cyclin T1 complex. This compound demonstrates potent antiviral activity, effectively inhibiting the replication of various viruses, including HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human cytomegalovirus (CMV). FIT-039 is particularly notable for its potential in addressing drug-resistant strains of HSV and other DNA viruses in research applications.

Cat. No.

A40631

CAS No.

667463-82-3

Indirubin-3′-oxime

Synonyms: IDR3O; I3O

Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation.

Cat. No.

A41192

CAS No.

2410402-88-7

CDK2-IN-12

CDK2-IN-12 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 11.6 μM. This compound also inhibits human carbonic anhydrase isoforms I, II, IX, and XII, with respective KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 demonstrates notable anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development.