CDK

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.

A38459

CAS No.

3052648-82-2

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.

Cat. No.

A38460

CAS No.

2980502-40-5

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.

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.

Cat. No.

A41204

CAS No.

2410402-75-2

Carbonic anhydrase inhibitor 14

Carbonic anhydrase inhibitor 14 is a potent inhibitor of carbonic anhydrases (CAs), exhibiting Ki values of 1203 nM for hCA I, 99.7 nM for hCA II, 9.4 nM for hCA IX, and 27.7 nM for hCA XII. Additionally, it effectively inhibits cyclin-dependent kinase 2 (CDK2) with an IC50 of 20.3 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications targeting both CA and CDK2 pathways.

Cat. No.

A41241

CAS No.

2410402-82-1

CDK2-IN-11

CDK2-IN-11 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), demonstrating an IC50 of 6.4 μM. With inhibitory constant (KI) values of 23.4 nM, 56.3 nM, and 44.3 nM for human carbonic anhydrases II, IX, and XII, respectively, it exhibits significant enzyme inhibition. CDK2-IN-11 is primarily utilized in anticancer research, making it a valuable tool for studies targeting cell cycle regulation and tumor progression.

Cat. No.

A42468

CAS No.

437982-89-3

(S)-PHA533533

(S)-PHA533533 is an inhibitor of cyclin-dependent kinases CDK2 and CDK5, demonstrating blood-brain barrier permeability with IC50 values of 37 nM and 55 nM, respectively. This compound effectively restores UBE3A expression by downregulating UBE3A-ATS, thereby alleviating the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 is a valuable tool for research applications related to Angelman syndrome and offers insights into therapeutic strategies for this genetic disorder.

Cat. No.

A44077

CAS No.

2733575-91-0

Tagtociclib hydrate

Synonyms: PF-07104091 hydrate

Tagtociclib hydrate is a potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2) and glycogen synthase kinase 3 beta (GSK3β), displaying inhibition constants of 1.16 nM and 537.81 nM, respectively. This compound demonstrates significant anti-tumor activity, particularly in cancers characterized by cyclin E1 amplification. Tagtociclib hydrate serves as a valuable research tool for studying cell cycle regulation and therapeutic strategies targeting kinase pathways in cancer biology.

Cat. No.

A44081

CAS No.

113411-17-9

DIF-3

DIF-3 is a potent cyclin D1 inhibitor that promotes the degradation of cyclin D1 and c-Myc by activating GSK-3β. This compound suppresses Wnt/β-catenin signaling pathway-associated proteins, leading to the induction of reactive oxygen species (ROS) and autophagy. Additionally, DIF-3 has demonstrated the ability to inhibit the growth of Trypanosoma cruzi in HT1080 cells, showcasing its antitumor properties in both in vitro and in vivo settings. Its multifaceted mechanism positions DIF-3 as a valuable tool for cancer research and cellular biology studies.

Cat. No.

A44091

CAS No.

844442-32-6

SGC-CDKL5/GSK3

SGC-CDKL5/GSK3 is a selective inhibitor targeting CDKL5 and GSK3α/β. This compound demonstrates potent inhibition, with IC50 values of 4.6 nM for CDKL5, 24 nM for GSK3β, and 9.5 nM for GSK3α, as assessed by the NanoBRET assay. Its specificity and efficacy make it a valuable tool for investigating central nervous system diseases and related biological pathways.

Cat. No.

A44100

CAS No.

1042735-18-1

ABC1183

ABC1183 is a selective dual inhibitor targeting GSK3 and CDK9, effectively inhibiting GSK3β, GSK3α, and CDK9/cyclin T1 with IC50 values of 657 nM, 327 nM, and 321 nM, respectively. This compound exhibits notable anti-inflammatory and anti-tumor activities, making it a valuable tool for cancer research and inflammation-related studies. Its ability to modulate critical signaling pathways positions ABC1183 as a promising candidate for further investigation in therapeutic applications.

Cat. No.

A44103

CAS No.

395074-72-3

GSK-3/CDK5/CDK2-IN-1

GSK-3/CDK5/CDK2-IN-1 is a potent inhibitor targeting GSK-3, CDK5, and CDK2. This imidazole derivative has demonstrated effectiveness in modulating pathways relevant to tumorigenesis and neurodegenerative disorders. Its ability to inhibit these kinases makes it a valuable tool for investigating mechanisms underlying cancer proliferation and neurodegeneration.

Cat. No.

A44111

CAS No.

2227279-83-4

GSK-3 inhibitor 4

GSK-3 Inhibitor 4 is a potent inhibitor of Glycogen Synthase Kinase 3 (GSK-3), Cyclin-Dependent Kinase 2 (CDK2), and Cyclin-Dependent Kinase 5 (CDK5), demonstrating IC50 values of 0.56 nM for GSK-3β, 0.45 nM for GSK-3α, 0.47 μM for CDK2, and 0.68 μM for CDK5. This compound effectively attenuates the phosphorylation of Tau protein, making it a valuable tool for investigating mechanisms underlying Alzheimer's disease. Its oral bioavailability and ability to penetrate the blood-brain barrier further enhance its utility in neuropharmacological research.

Cat. No.

A44117

CAS No.

2613307-67-6

CDK8-IN-12

CDK8-IN-12 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting a potent Ki value of 14 nM. This compound also demonstrates off-target activity against GSK-3α, GSK-3β, and PCK-θ with Ki values of 13 nM, 4 nM, and 109 nM, respectively. CDK8-IN-12 has been shown to exert significant anti-proliferative effects on MV4-11 cancer cells, making it a valuable tool for research in oncology and the exploration of CDK8-related pathways in cancer progression.

Cat. No.

A44129

CAS No.

1212711-91-5

CDK5-IN-4

CDK5-IN-4 is a potent multikinase type-II inhibitor primarily targeting cyclin-dependent kinase 5 (CDK5), with an IC50 of 9.8 μM. Additionally, it exhibits inhibitory activity against GSK-3α and GSK-3β with IC50 values of 0.98 μM and 4.00 μM, as well as CDK9 and CDK2, with IC50 values of 1.76 μM and 6.24 μM, respectively. This compound is particularly relevant for research on glioblastoma and may aid in understanding its molecular mechanisms.

Cat. No.

A44141

CAS No.

3034210-97-1

CDK7-IN-20

CDK7-IN-20 is a highly potent and selective irreversible inhibitor of cyclin-dependent kinase 7 (CDK7), exhibiting an IC50 value of 4 nM. Demonstrating over 206-fold selectivity for CDK7 compared to CDK1, CDK2, CDK3, CDK5, CDK6, CDK9, and CDK12, CDK7-IN-20 is a valuable tool for studying the role of CDK7 in cellular processes. Its potential applications extend to researching autosomal dominant polycystic kidney disease (ADPKD) and other related pathologies.

Cat. No.

A44157

CAS No.

496864-15-4

Aloisine RP106

Aloisine RP106 is a potent inhibitor of cyclin-dependent kinases (CDKs) Cdk1/cyclin B and Cdk5/p25, as well as glycogen synthase kinase 3 (GSK3), with IC50 values of 0.70 µM, 1.5 µM, and 0.92 µM, respectively. This compound is valuable for research applications targeting cell cycle regulation and neurodegenerative diseases, where CDK and GSK3 activity contribute to pathological processes. Researchers can utilize Aloisine RP106 to investigate the role of these kinases in various biological contexts including cancer and neurobiology.

Cat. No.

A44163

CAS No.

748142-06-5

UNC10112785

UNC10112785 is a potent inhibitor of serine/threonine kinases, specifically targeting GSK-3β, CDK-2, and CDK-4 with IC50 values of 0.031 μM, 0.016 μM, and 1.99 μM, respectively. This compound exhibits significant biological activity that positions it as a valuable tool in the study of type 2 diabetes. Its ability to modulate key pathways involved in metabolic regulation makes it an essential reagent for researchers investigating therapeutic interventions in diabetic conditions.

Cat. No.

A46129

CAS No.

3066836-42-5

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.