Catalog No.
Product Name
Application
Product Information
Citations
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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. -
G-quadruplex DNA Fluorescent Binder
N-Methylmesoporphyrin IX (NMM) is a potent fluorescent binder that targets G-quadruplex DNA, making it an effective probe for studying Aβ fibrillation. It serves as both an in situ inhibitor and an ex situ monitor of Aβ amyloidogenesis in vitro and within cellular contexts. NMM exhibits high sensitivity to G-quadruplex structures while showing negligible response to duplexes, triplexes, and single-stranded DNA. Additionally, it remains nonfluorescent in monomeric Aβ environments, producing strong fluorescence upon interaction with Aβ aggregates. -
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. -
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/CDK5 Inhibitor
(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. -
CDK9 Autophagic Degrader
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. -
CDK4/6 Inhibitor
Palbociclib hydrochloride is a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6, with IC50 values of 11 nM and 16 nM, respectively. This compound demonstrates significant anti-proliferative activity, effectively inducing cell cycle arrest in malignant cells. Palbociclib hydrochloride is utilized in research focused on HR-positive and HER2-negative breast cancer as well as hepatocellular carcinoma, making it a valuable tool for understanding tumor biology and therapeutic responses. -
CDK7 Inhibitor
YKL-5-124 is a selective and irreversible inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound exhibits over 100-fold selectivity for CDK7 compared to CDK9 and CDK2 and has negligible activity against CDK12 and CDK13. YKL-5-124 effectively induces cell-cycle arrest, inhibits E2F-driven transcription, and has a limited impact on the phosphorylation status of RNA polymerase II, making it a valuable tool for research in cell cycle regulation and transcriptional control. -
CDK Inhibitor
Romaciclib monohydrochloride is a selective CDK inhibitor that targets CDK8 and CDK19. This compound exhibits potent inhibition of CDK8/CycC and CDK19/CycC kinase activities with IC50 values of 4.4 nM and 10.4 nM, respectively. Additionally, it weakly inhibits CDK9 with an IC50 of 1070 nM, while having no significant activity against other CDK isoforms. Romaciclib monohydrochloride is known to inhibit the phosphorylation of STAT1 at S727 and STAT5 at S726, demonstrating potential anti-tumor activity valuable for cancer research applications. -
CDK9 Inhibitor
KB-0742 dihydrochloride is a selective and orally bioactive inhibitor of CDK9, exhibiting an IC50 of 6 nM for the CDK9/cyclin T1 complex. This compound demonstrates over 50-fold selectivity for CDK9 compared to other CDK kinases, making it a valuable tool for precision research. KB-0742 dihydrochloride possesses strong anti-tumor activity, facilitating investigations into its efficacy in cancer biology and therapeutic applications. -
CDK4/6 Inhibitor
Dalpiciclib is a highly selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), demonstrating IC50 values of 12.4 nM and 9.9 nM, respectively. This orally active compound exhibits significant antitumor activity, particularly in breast cancer and esophageal squamous cell carcinoma. Dalpiciclib is utilized in research applications focused on tumor suppression and cell cycle regulation. -
WEE1 Inhibitor
Zedoresertib, a potent WEE1 inhibitor, exhibits an IC50 value of 0.8 nM and effectively inhibits phospho-CDC2. By abrogating the G2 checkpoint, Zedoresertib enhances the sensitivity of cancer cells to DNA-damaging agents, making it a valuable tool for anticancer research. This compound is essential for studies investigating cell cycle regulation and therapeutic strategies in oncology. -
Cyclin K Degrader
HQ461 is a molecular glue that facilitates the interaction between CDK12 and DDB1, leading to the targeted degradation of cyclin K. This degradation impairs CDK12 function, which in turn results in reduced phosphorylation of CDK12 substrates, downregulation of DNA damage response genes, and induces apoptosis in affected cells. HQ461 is a valuable tool for research applications focused on the modulation of cell cycle regulation and the DNA damage response pathway. -
CDK9 Inhibitor
KB-0742 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 6 nM for the CDK9/cyclin T1 complex. With over 50-fold selectivity against other CDK kinases, KB-0742 demonstrates significant anti-tumor activity. This compound is particularly valuable for research involving transcriptional regulation, cancer biology, and therapeutic strategies targeting CDK9-associated pathways. -
CDK4/6 Inhibitor
Dalpiciclib hydrochloride is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), with IC50 values of 12.4 nM and 9.9 nM, respectively. This compound exhibits significant antitumor activity, particularly in the context of breast cancer and esophageal squamous cell carcinoma. Dalpiciclib hydrochloride is valuable for research focused on cell cycle regulation and cancer therapeutics. -
PTEFb/CDK9 Inhibitor
Atuveciclib is a highly selective oral inhibitor of PTEFb/CDK9, demonstrating potent activity with an IC50 of 13 nM against the CDK9/CycT1 complex. This compound effectively disrupts transcriptional regulation, making it a valuable tool in cancer research and studies related to transcriptional control. Atuveciclib may be employed in investigations aimed at understanding the roles of CDK9 in various diseases, including cancer and other pathologies linked to aberrant transcriptional activity. -
CDK5 Inhibitor
GFB-12811 is a highly selective inhibitor of cyclin-dependent kinase 5 (CDK5) with an IC50 of 2.3 nM. Its potent action allows for effective modulation of CDK5 activity, making it a valuable tool for studying neurodegenerative diseases and related signaling pathways. This compound is suitable for research investigating the role of CDK5 in neuronal function and pathology. -
CDK4/6 Inhibitor
Abemaciclib metabolite M20 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). This compound exhibits potent anti-proliferative activity in various cancer cell lines, contributing to its potential use in cancer therapy. Research applications include studying cell cycle regulation and exploring therapeutic strategies for tumors driven by CDK4/6 activity. -
CDK2/5 Inhibitor
CDK5 inhibitor 20-223 is a potent inhibitor of cyclin-dependent kinases 2 and 5, exhibiting IC50 values of 6.0 nM and 8.8 nM, respectively. This compound demonstrates significant anti-colorectal cancer activity, making it a valuable tool for research in cancer biology and therapeutic development. Its selective inhibition of CDK2 and CDK5 provides insights into their roles in cell cycle regulation and oncogenesis. -
CCND1/CDK4 PROTAC Degrader
CPD-39 is a potent heterobifunctional PROTAC degrader that targets CCND1 and CDK4. This compound effectively induces the degradation of these proteins, demonstrating significant anti-proliferative activity. CPD-39 is intended for research applications focusing on the modulation of cell cycle regulation and cancer therapeutics. -
CDK4/6 Inhibitor
Abemaciclib metabolite M18 hydrochloride functions as a CDK4/6 inhibitor, exhibiting significant antitumor activity. This compound has been utilized in the design of PROTAC (Proteolysis Targeting Chimera) CDK4/6 degraders in conjunction with a CRBN ligand. Its role in targeted protein degradation research makes it a valuable tool for investigating cell cycle regulation and cancer therapeutics. -
CDK12 Inhibitor
CDK12-IN-2 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a nanomolar potency with an IC50 value of 52 nM. This compound also demonstrates inhibitory activity against CDK13, its closest homologue, but maintains strong selectivity for CDK12 over other kinases such as CDK2, CDK7, CDK8, and CDK9. CDK12-IN-2 effectively inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II, making it a valuable chemical probe for functional studies in cancer biology and transcription regulation. -
CDK5 Inhibitor
CDK5-IN-3 is a highly selective inhibitor of CDK5, demonstrating IC50 values of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. This compound is valuable for investigations into the role of CDK5 in cellular processes and is particularly relevant for research focused on autosomal dominant polycystic kidney disease (ADPKD). Its potency and specificity make CDK5-IN-3 an essential tool for elucidating the molecular mechanisms underlying CDK5-related pathologies. -
CDK2 Inhibitor
GW8510 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) that also targets ribonucleotide reductase M2 (RRM2). This compound demonstrates significant neuroprotective effects and possesses anticancer properties. It is utilized in scientific research to explore mechanisms of cell proliferation and apoptosis in various cancer models, making it a valuable tool for studying the role of CDK2 in cancer and neurodegenerative diseases. -
CDK2 Molecular Glue Degrader
CDK2 degrader 6 is a potent CDK2 molecular glue degrader that functions through binding to cereblon and CDK2, leading to the ubiquitination and proteasomal degradation of CDK2. With a DC50 of 46.5 nM, it effectively modulates the cell cycle and reduces proliferation in breast cancer cells. Additionally, CDK2 degrader 6 demonstrates in vivo antitumor activity in gastric cancer mouse models, making it a valuable tool for research into breast and gastric cancers. -
CDK Inhibitor
DS96432529 is a potent CDK8 inhibitor that exhibits bone anabolic properties. This compound selectively inhibits cyclin-dependent kinase 8, leading to enhanced bone formation and potential therapeutic applications in osteoporosis and other bone-related disorders. Its oral bioavailability makes it a valuable tool for in vivo studies focusing on bone metabolism and development. -
CDK2 Inhibitor
CDK2-IN-23 is a highly potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.29 nM. This compound demonstrates significant pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models, making it a valuable tool in cancer research. Its selectivity and potency provide a promising avenue for studying CDK2's role in tumorigenesis and evaluating therapeutic strategies in oncology. -
CDK9 Inhibitor
CDK9 inhibitor HH1 selectively targets cyclin-dependent kinase 9 (CDK9), a key regulator of transcriptional control. This compound effectively inhibits CDK9 activity, leading to decreased transcription of oncogenes associated with cancer progression. HH1 serves as a valuable reagent for investigating therapeutic strategies in cancer research and studying the role of CDK9 in gene expression regulation. -
CDK Inhibitor
JH-XVI-178 is a potent and selective inhibitor targeting cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 1 nM and 2 nM, respectively. This compound exhibits low clearance rates and moderate oral pharmacokinetic characteristics, making it suitable for in vivo studies. JH-XVI-178 is valuable for research in transcriptional regulation and cancer biology, particularly in contexts where CDK8 and CDK19 play critical roles in oncogenic signaling pathways. -
CDK12/13 Inhibitor
MFH290 is a selective covalent inhibitor of cyclin-dependent kinases 12 and 13 (CDK12/13). By forming a covalent bond with Cys-1039 of CDK12, MFH290 effectively inhibits the phosphorylation of serine-2 in the C-terminal domain of RNA polymerase II, thus modulating transcriptional regulation. This compound is primarily utilized in cancer research to explore therapeutic strategies targeting CDK12/13-related pathways. -
CDK7 Inhibitor
YKL-5-124 TFA is a selective and irreversible inhibitor of Cyclin-dependent kinase 7 (CDK7), with IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound demonstrates over 100-fold selectivity for CDK7 compared to CDK9 and CDK2, and it shows no activity against CDK12 and CDK13. YKL-5-124 TFA effectively induces cell-cycle arrest, inhibits E2F-driven gene expression, and has minimal impact on RNA polymerase II phosphorylation, making it a valuable tool for research in cancer biology and transcription regulation. -
CDK12/13 Covalent Inhibitor
BSJ-01-175 is a potent covalent inhibitor of CDK12 and CDK13, targeting cyclin-dependent kinases involved in cell cycle regulation. This compound exhibits strong selectivity and effectively inhibits RNA polymerase II phosphorylation, leading to the downregulation of CDK12-targeted genes in cancer cells. BSJ-01-175 is valuable for research in cancer biology and therapeutic development aimed at CDK-mediated signaling pathways. -
CDK Inhibitor
2,4,6-Trihydroxybenzoic acid is a specific inhibitor of cyclin-dependent kinases (CDKs). It exhibits significant anti-proliferative activity, making it a valuable tool for cancer research. This compound is utilized in studies aimed at elucidating the role of CDKs in cell cycle regulation and tumorigenesis.
