Catalog No.
Product Name
Application
Product Information
Citations
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CDK4/6 inhibitor
CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively. -
CDK12 inhibitor
CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay. -
CDK8/19 dual inhibitor
CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively. -
CDK inhibitor
Alsterpaullone (9-Nitropaullone;NSC 705701) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. -
CDC7 inhibitor
Simurosertib (TAK-931) is a selective cycle 7 (CDC7) kinase inhibitor, with an IC50<0.3 nM. -
CDK4/CDK6 inhibitor
CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor with IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively. -
CDK14 inhibitor
FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively. -
CDK9 degrader PROTAC
THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN). -
XBP1 inhibitor
Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM. -
CDK inhibitor
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. -
CDK1, CDK5, and GSK-3βinhibitor
Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively. -
GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively. -
CDK inhibitor
AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM, less potent to CDK3 and little active to CDK7. -
CDK9 inhibitor
CDK9-IN-2 is a novel cyclin-dependent kinase 9(CDK9) inhibitor. -
CDK inhibitor
NVP-LCQ195 is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM. -
CDK inhibitor
Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor. IC50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. -
CDK Inhibitor
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. -
CDK7 Inhibitor
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. -
CDK9 Inhibitor
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. -
CK1/CDK1/CDK5 Inhibitor
(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. -
CDK8 Inhibitor
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. -
CDK8 Inhibitor
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. -
CDK6/9 Inhibitor
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. -
CDK Inhibitor
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. -
CDK3 Inhibitor
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. -
CDK8/19 Inhibitor
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. -
CDK8/19 Inhibitor
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. -
CDK9/FLT3 Inhibitor
CDDD11-8 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9) and FLT3-ITD, exhibiting Ki values of 8 nM and 13 nM, respectively. This compound effectively reduces the proliferation of leukemia cell lines, particularly those associated with the FLT3-ITD mutation. CDDD11-8 serves as a valuable tool for research into targeted therapies for hematological malignancies, specifically in the study of cell cycle regulation and tyrosine kinase signaling pathways. -
FLT3/CDK5 Inhibitor
AMG 925 (HCl) is a potent dual inhibitor targeting FLT3 and CDK5, demonstrating IC50 values of 2±1 nM and 3±1 nM, respectively. This compound exhibits selectivity for these kinases, making it a valuable tool for research into hematological malignancies and cancer progression. Its oral bioavailability further enhances its utility in preclinical studies investigating therapeutic interventions for FLT3-driven malignancies and CDK5-associated diseases. -
FLT3/CDK4 Inhibitor
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. -
CDK Inhibitor
(E/Z)-SU9516 is a selective inhibitor of cyclin-dependent kinases (CDKs), primarily targeting CDK2, with an IC50 value of 22 nM. This compound also exhibits inhibitory effects on CDK1 and CDK4, with IC50 values of 40 nM and 200 nM, respectively. Its potent inhibition of CDKs makes (E/Z)-SU9516 a valuable tool for studying cell cycle regulation and therapeutic applications in cancer research. -
CDK4 Inhibitor
3-ATA is a selective inhibitor of cyclin-dependent kinase 4 (CDK4), demonstrating both neuroprotective and antitumor properties. This compound has been shown to reduce kainic acid-induced apoptosis in cerebellar granule neurons, making it a valuable tool for investigating neurodegenerative diseases. Its ability to modulate cell cycle progression and prevent neuronal death highlights its potential applications in both cancer research and neuroprotection studies. -
CDK9-Cyclin T1 PPI Inhibitor
CDK9-Cyclin T1 PPI-IN-1 is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction. This compound effectively inhibits cell proliferation in triple-negative breast cancer (TNBC) MDA-MB-231 cells with an IC50 of 0.044 μM and promotes apoptosis. Additionally, CDK9-Cyclin T1 PPI-IN-1 suppresses CDK9 transcriptional activity and diminishes the phosphorylation of RNA Polymerase II at the CTD serine 2 residue. In vivo studies further demonstrate its capability to inhibit tumor growth in a TNBC 4T1 mouse model. -
CDK Inhibitor
CDK-IN-9 is a potent cyclin-dependent kinase (CDK) inhibitor that serves as a molecular glue, promoting the interaction between CDK12 and DDB1. With an IC50 value of 4 nM for CDK2/E, CDK-IN-9 facilitates the polyubiquitination and subsequent degradation of cyclin K. Additionally, it induces apoptosis through the dephosphorylation of retinoblastoma protein and RNA polymerase II, making it a valuable tool for research in cancer biology and cell cycle regulation. -
PROTAC CDK4/6/9 Degrader
PROTAC CDK4/6/9 Degrader 1 is a targeted protein degradation agent that specifically degrades cyclin-dependent kinases CDK4, CDK6, and CDK9. This compound effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells by inducing G1 phase arrest, promoting apoptosis, and suppressing cellular migration and invasion. PROTAC CDK4/6/9 Degrader 1 serves as a valuable tool for studying the role of these kinases in TNBC and may support the development of novel therapeutic strategies aimed at this aggressive cancer subtype.
