Catalog No.
Product Name
Application
Product Information
Citations
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CHK2 Inhibitor
CCT241533 dihydrochloride is a highly selective ATP-competitive inhibitor of CHK2, exhibiting an IC50 of 3 nM and a Ki of 1.16 nM. This compound has significant potential in cancer research due to its ability to modulate DNA damage responses and cell cycle regulation. It is particularly valuable for studies investigating the role of CHK2 in tumor biology and therapeutic sensitivity. -
CHK1 Inhibitor
CHK1-IN-13 is a selective checkpoint kinase 1 (CHK1) inhibitor with an IC50 range of 10-50 nM. This compound exhibits significant anticancer activity, making it a valuable tool for research focused on various cancers, including breast, ovarian, and prostate cancers. Its role in modulating the cell cycle checkpoint pathways provides insights into the mechanisms of cancer cell proliferation and therapeutic resistance. -
CHK1 Inhibitor
CHK1-IN-14 is a potent CHK1 inhibitor that selectively disrupts checkpoint kinase 1 activity. This compound is primarily utilized in research focused on understanding mechanisms of resistance to chemotherapy and radiotherapy in cancer cells. Its application provides valuable insights into potential therapeutic strategies aimed at improving the efficacy of cancer treatments. -
Dual Wee1/Chk1 Inhibitor
DB07006 is a potent dual inhibitor targeting Wee1 and Chk1 kinases. It exhibits ATP-competitive inhibition, with IC50 values of 0.030 μM for Wee1 and 0.018 μM for Chk1. This compound effectively abrogates the G2/M checkpoint when used in conjunction with DNA-damaging agents in cellular models, making it a valuable tool for cancer research and therapeutic strategies aimed at enhancing the efficacy of DNA-damage response inhibitors. -
Checkpoint Kinase (Chk) Inhibitor
(S)-CCT245737 is a selective inhibitor of checkpoint kinase 1 (CHK1), primarily targeting cell cycle regulation. This compound exhibits potent inhibitory activity, making it a valuable tool for studying the role of CHK1 in DNA damage response and replication stress. Its applications extend to cancer research, particularly in investigating therapeutic strategies for tumors with defective DNA repair mechanisms. -
Chk Inhibitor
XL-844 is an inhibitor of checkpoint kinases Chk1 and Chk2, leading to the induction of apoptosis in tumor cells by disrupting cell cycle arrest. Additionally, XL-844 demonstrates inhibitory effects on vascular endothelial growth factor receptors VEGFR1 and VEGFR3. This compound is primarily applied in anti-cancer research to explore its potential in enhancing therapeutic efficacy against various malignancies. -
Chk1 Inhibitor
CHK1-IN-8 is a selective Chk1 inhibitor with an IC50 value of less than 10 nM for human Chk1. This compound is valuable for investigating the role of Chk1 in cell cycle regulation and DNA damage response mechanisms in cancer research. Its potent inhibition of Chk1 makes it a useful tool for exploring therapeutic strategies in cancer treatment. -
Chk2 Inhibitor
PV1162 is a selective Chk2 inhibitor that functions by preventing ATP binding to Chk2, specifically targeting the gatekeeper-dependent hydrophobic pocket situated behind the ATP-binding site. With an IC50 of 0.29 nM, PV1162 effectively inhibits the phosphorylation activity of Chk2. This compound demonstrates significant potential for research applications in cancer therapy, particularly in the study of checkpoint regulation and tumor progression. -
Checkpoint Kinase (Chk) Inhibitor
CHK-IN-1 is a selective inhibitor of checkpoint kinases CHK1 and CHK2, which play crucial roles in the DNA damage response and cell cycle regulation. This compound exhibits anti-proliferative activity, making it a valuable tool for cancer research and therapeutic studies targeting tumor cell growth and survival. Its ability to regulate cellular checkpoint pathways provides a basis for exploring its efficacy in combination therapies and enhancing the understanding of cancer cell biology. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-3 is a selective dual inhibitor targeting bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). This compound effectively inhibits BRD4-BD1, PLK1, and BRDT-BD1, exhibiting IC50 values of 0.059 µM, 0.127 µM, and 0.245 µM, respectively. PLK1/BRD4-IN-3 can be employed in research applications focused on cancer biology, particularly in studies investigating cell proliferation and transcriptional regulation. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-2 is a dual inhibitor targeting both Polo-like kinase 1 (PLK1) and the bromodomain of BRD4, with an IC50 of 40 nM and 28 nM, respectively. This compound is valuable for research into cancer therapeutics and epigenetic regulation, demonstrating potential in studies focused on cell proliferation and transcriptional control. Its ability to simultaneously inhibit these key oncogenic pathways positions PLK1/BRD4-IN-2 as a crucial tool for advancing cancer research and drug discovery initiatives. -
CDK/GSK3β/JNK Inhibitor
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. -
RAS/RAS-RAF Inhibitor
RAS/RAS-RAF-IN-1 is a potent inhibitor targeting the RAS and RAS-RAF signaling pathways. With a dissociation constant (KD) in the range of 5.0 μM to 15 μM for cyclophilin A (CYPA), this compound demonstrates significant binding affinity. RAS/RAS-RAF-IN-1 exhibits notable antitumor activity, making it a valuable tool for cancer research and therapeutic development. -
Ras-Raf Inhibitor
Cyclorasin 9A5 is an 11-residue cyclic peptide that acts as an orthosteric inhibitor of the Ras-Raf protein interaction, exhibiting an IC50 of 120 nM. This compound is valuable for studying the Ras signaling pathway's involvement in various cancers and cellular processes. Its cell-permeable nature allows for effective in vitro and in vivo applications in cancer research and drug development targeting Ras-dependent pathways. -
pan-KRAS PROTAC Degrader
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment. -
PDE6δ-KRas Inhibitor
Deltasonamide 1 is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a dissociation constant (KD) of 203 pM. This compound effectively disrupts the function of the KRas signaling pathway, making it a valuable tool for investigating tumor biology and related therapeutic strategies. Deltasonamide 1 holds promise for advancing research in cancer treatment and understanding related pathophysiological mechanisms. -
KRAS Inhibitor
Deltarasin hydrochloride is a potent inhibitor of the interaction between KRAS and PDEδ, exhibiting a binding affinity (Kd) of 38 nM for purified PDEδ. This compound is crucial for research applications focused on targeting KRAS-driven oncogenesis, primarily in cancer studies. By disrupting this interaction, Deltarasin hydrochloride facilitates investigations into therapeutic strategies aimed at KRAS mutations and their downstream signaling pathways. -
PDE6δ-KRas Inhibitor
Deltasonamide 1 TFA is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a binding affinity with a KD of 203 pM. This compound is valuable in research focused on cancer biology, particularly in the study of tumor progression and metastasis. Its ability to disrupt the PDE6δ-KRas axis makes it a useful tool for investigating the underlying mechanisms of KRas-driven malignancies. -
PLK1/p38γ Inhibitor
PLK1/p38γ-IN-1 is a multitarget inhibitor that selectively targets PLK1 and p38γ kinases. This compound has demonstrated the ability to inhibit cell proliferation in human hepatocellular carcinoma and hepatoblastoma cell lines in vitro. PLK1/p38γ-IN-1 is valuable for research focused on cancer biology and the modulation of cell cycle pathways. -
KRAS G12C Inhibitor
KRAS G12C-IN-78 is a selective inhibitor targeting the KRAS G12C mutant protein, binding to both inactive and active states. This compound effectively inhibits ERK1/2 phosphorylation and promotes covalent adduct formation with endogenous KRAS G12C, leading to the suppression of MAPK pathway gene expression and reduced cellular proliferation in KRAS G12C mutant cells. KRAS G12C-IN-78 is suitable for studying KRAS G12C mutant solid tumors, such as pancreatic ductal adenocarcinoma and non-small cell lung cancer. -
Akt/ROCK Inhibitor
Akt/ROCK-IN-1 is a potent dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively. This compound demonstrates significant antitumor activity, particularly in neuroblastoma models. It serves as a valuable tool for research into cancer biology and therapeutic development. -
KRAS-PDEδ Inhibitor
NHTD is a selective inhibitor of KRAS-PDEδ, targeting the prenyl-binding pocket of PDEδ and modulating the cellular localization of KRAS. This action effectively inhibits the proliferation of KRAS-mutant cancer cells and promotes apoptosis. NHTD is a valuable tool for investigations into KRAS-driven non-small cell lung cancer (NSCLC) and related oncology research. -
CDK2/GSK3β Inhibitor
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. -
PLK2 Inhibitor
8012-3246 is a selective inhibitor of Polo-like kinase 2 (PLK2) with an IC50 of 774.5 nM. This compound effectively suppresses the phosphorylation of GSK3β, demonstrating its potential role in cellular signaling modulation. Additionally, 8012-3246 exhibits significant anticancer activity, particularly against colorectal cancer, making it a valuable tool for cancer research applications focusing on PLK2-related pathways. -
Cyclin D1 Inhibitor
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. -
CDKL5/GSK3 Inhibitor
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. -
GSK3/CDK9 Inhibitor
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. -
GSK-3/CDK5/CDK2 Inhibitor
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. -
GSK-3/CDK2/CDK5 Inhibitor
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. -
CDK8 Inhibitor
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. -
CDK/GSK-3 Inhibitor
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. -
CDK7 Inhibitor
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. -
CDK/GSK3 Inhibitor
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. -
GSK-3β/CDK-2/CDK-4 Inhibitor
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. -
CDK inhibitor
BMS-265246 is a potent new pyra- zolopyridine inhibitor of cdk2/cyclin E and cdk1/cyclin B, as well as cdk4/cyclin D. -
Aurora Kinase B/C inhibitor
GSK1070916 is a potent Aurora B/C kinase inhibitor (with IC50 of 3.5 nM/6.5 nM) with broad antitumor activity in tissue culture cells and human tumor xenograft models.
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Aurora A/B Kinase inhibitor
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1. -
multi-kinase inhibitor
Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. -
CDK inhibitor
AT7519 is an inhibitor of multiple cyclin-dependent kinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. -
ROCK inhibitor
Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM. -
CDK336 Inhibitor
Pseudolaric Acid A is a diterpene acid isolated from Pseudolarix kaempferi, has antifungal, cytotoxic and antifertile activities.
