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Catalog No.
Product Name
Application
Product Information
Citations
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Aurora Kinase Inhibitor
Binucleine 2 is an ATP-competitive inhibitor targeting Drosophila Aurora B kinase, displaying an inhibition constant (Ki) of 0.36 μM. This compound exhibits isoform specificity, effectively inhibiting Drosophila Aurora B in a dose-dependent manner while exhibiting minimal activity against human and Xenopus laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 is valuable for studying mitotic processes, as it induces defects in mitosis and cytokinesis in Drosophila Kc167 cells and disrupts contractile ring assembly in Drosophila S2 cells at a concentration of 40 μM, highlighting the critical role of Aurora B kinase in cell division. -
Aurora A Inhibitor
Aurora A inhibitor 4 (compound C9) is a selective inhibitor of Aurora A kinase, demonstrating a GI50 of 4.26 μM in DU 145 cells and 7.08 μM in HT-29 cells. This compound exhibits significant anti-proliferative effects, making it valuable for research focused on cell cycle regulation and cancer therapeutics. Its ability to inhibit Aurora A activity can be applied in studies investigating mitotic dysregulation in various tumor types. -
Aurora Kinase Inhibitor
Aurora B inhibitor 1 is a selective inhibitor of the Aurora B kinase, exhibiting a Ki value of <0.010 µM. This compound plays a crucial role in manipulating cell division and is instrumental in research surrounding cancer biology and therapeutic development. Its ability to inhibit Aurora B activity makes it a valuable tool for studies focused on mitotic regulation and chromosomal instability. -
Aurora A Inhibitor
Aurora A Inhibitor I is a potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 3.4 nM (Aurora A) and unusually high selectivity 1000 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases.
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Aurora Inhibitor
CCT129202 is a representative of a structurally novel series of imidazopyridine small-molecule inhibitors of Aurora kinase activity. It shows high selectivity for the Aurora kinases over a panel of other kinases tested and inhibits proliferation in multiple cultured human tumor cell lines.
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ROCK Inhibitor
GSK429286A is a cell-permeable, selective small molecule inhibitor of Rho-associated, coiled-coil containing protein kinase (ROCK). -
PLK Inhibitor
ON-01910 is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. -
Aurora inhibitor
PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3. -
CDK inhibitor
SNS-032 (BMS-387032) is a highly selective and potent inhibitor of cyclin-dependent kinases (Cdks) 2, 7, and 9, with in vitro growth inhibitory effects and ability to induce apoptosis in malignant B cells. -
Aurora inhibitor
SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1. -
ROCK inhibitor
Thiazovivin is a selective inhibitor of Rho-associated kinase (ROCK). -
osteoclastic bone resorption inhibitor
Zoledronic acid is a bisphosphonate which used to multiple myeloma and prostate cancer treament. -
CDK inhibitor
Flavopiridol HCl is an inhibitor of cyclin-dependent kinases. The (-)-cis form induces apoptosis in particular tumor cells. -
CDK Inhibitor
PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity. -
RAD51 inhibitor
Bractoppin is a potent and selective inhibitor of phosphopeptide recognition by the BRCA1 tBRCT domain. -
S-IIP inhibitor/KRASG12C Probe
ARS-1323-Alkyne is a novel KRASG12C occupancy probe. -
SOS1 Inhibitor
SOS1-IN-14 is a potent and selective inhibitor of SOS1, demonstrating an IC50 value of 3.9 nM. This orally active compound is absorbed in the intestine through a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 is primarily utilized in research on KRAS-mutated cancers, showcasing superior tumor suppression capabilities compared to alternative therapies. -
Rac1 Inhibitor
Rac1-IN-4 is a selective inhibitor of Rac1, a Rho GTPase involved in various cellular processes including cytoskeletal dynamics and cell migration. This compound effectively disrupts the signaling pathways mediated by Rac1, making it a valuable tool for studying cancer metastasis and neurodegenerative diseases. Rac1-IN-4 is utilized in research to explore the therapeutic potential of targeting Rac1 in cellular signaling and pathology. -
Ras Inhibitor
ASP2453 is a selective and orally bioavailable inhibitor targeting the KRAS G12C mutation. It functions by inhibiting the interaction between KRAS G12C and Raf mediated by Son of Sevenless (SOS), demonstrating an IC50 value of 40 nM. ASP2453 shows potential in cancer research, particularly in studies addressing KRAS-driven malignancies. -
K-Ras Inhibitor
KRpep-2d is a potent inhibitor of K-Ras, targeting the K-Ras signaling pathway known for its role in various cancers. This compound effectively reduces the proliferation of K-Ras-driven cancer cells, making it a valuable tool for cancer research. Its application can aid in the development of therapeutic strategies for K-Ras-associated malignancies. -
SOS1/KRAS Inhibitor
SAH-SOS1A TFA is a peptide-based inhibitor targeting the SOS1-KRAS protein interaction. It exhibits nanomolar affinity for both wild-type and various mutant KRAS forms, including G12D, G12V, G12C, G12S, and Q61H (EC50 = 106-175 nM). By directly disrupting nucleotide association, SAH-SOS1A TFA effectively impairs KRAS-driven cancer cell viability and inhibits the downstream ERK-MAPK phosphosignaling cascade, making it a valuable tool for research in cancer biology. -
SOS1 Inhibitor
SOS1-IN-15 is a potent SOS1 inhibitor with an IC50 value of 5 nM, designed to specifically target and inhibit SOS1 activity. Its strong inhibitory effect makes it a promising candidate for research into KRAS-driven cancers, facilitating the understanding of oncogenic signaling pathways and development of targeted therapeutic strategies. -
KRASG12C Inhibitor
RM-018 is a potent KRASG12C inhibitor that specifically targets the GTP-bound, active state of KRASG12C. This tricomplex compound effectively inhibits KRASG12C/Y96D, showcasing its potential to overcome resistance mechanisms. RM-018 is an invaluable tool for studying KRAS-related signaling pathways and developing targeted therapies in cancer research. -
Rac1/Cdc42 Inhibitor
AZA1 is a potent dual inhibitor of Rac1 and Cdc42, key regulators of cell signaling pathways. This compound has been shown to induce apoptosis in prostate cancer cells while simultaneously inhibiting their proliferation, migration, and invasion. AZA1 serves as a valuable tool for research into the molecular mechanisms of prostate cancer progression and potential therapeutic interventions. -
Cdc42 Inhibitor
MLS-573151 is a selective inhibitor of the GTPase Cdc42, exhibiting an EC50 of 2 μM. It specifically targets Cdc42 without affecting other members of the GTPase family, such as Rab2, Rab7, H-Ras, Rac1, Rac2, and wild-type RhoA. By inhibiting GTP binding to Cdc42, MLS-573151 serves as a valuable tool for studying cellular processes regulated by this signaling pathway. Its application is essential in research related to cancer and other diseases where Cdc42 plays a critical role in cell migration and proliferation. -
Rac1 Inhibitor
Z62954982 is a selective Rac1 inhibitor with an IC50 of 12 μM, demonstrating notable potency in disrupting the Rac1/Tiam1 complex. This compound effectively reduces active Rac1 levels (GTP-bound) in the cytoplasm while preserving the function of other Rho GTPases such as Cdc42 and RhoA. Z62954982 serves as a valuable tool for studies investigating Rac1-mediated signaling pathways and their role in various biological processes. -
Tyrosinase Inhibitor
Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells. -
RAS-Effector PPI Inhibitor
RAS inhibitor Abd-7 is a selective RAS-binding compound (Kd=51 nM) that disrupts RAS-effector protein-protein interactions. This inhibitor effectively interferes with RAS-dependent signaling pathways by preventing the interactions between RAS and key effectors such as PI3K, CRAF, and RALGDS, as well as mutant KRAS proteins, NRAS Q61H, and HRAS G12V. RAS inhibitor Abd-7 is valuable for research applications targeting RAS-mediated processes in cancer biology. -
KRAS(G12C) Inhibitor
BBO-8520 is a selective covalent inhibitor of the KRAS G12C mutation, effectively promoting the inactive (OFF) state of KRAS by blocking GTP binding. This compound inhibits cell proliferation and disrupts the interaction between RAS and RAF1, leading to significant impact on oncogenic signaling pathways. BBO-8520 is suitable for research applications focusing on cancer biology and therapeutic strategies targeting KRAS-driven tumors. -
Rab27a-JFC1 Inhibitor
Nexinhib20 is a selective inhibitor of the Rab27a-JFC1 interaction (IC50: 2.6 μM) and Rac-1-GTP signaling. This compound effectively inhibits neutrophil exocytosis, adhesion, and β2 integrin activation, demonstrating significant anti-inflammatory properties. Nexinhib20 is suitable for research applications focused on systemic inflammation and myocardial ischemia-reperfusion injury. -
KRas Inhibitor
Pan KRas-IN-1 is a pan KRas inhibitor that targets mutant KRas proteins, particularly effective against KRas G12C inhibitor-resistant cancer models. It exhibits potent anti-cancer activity by disrupting KRas signaling pathways, thereby inhibiting tumor cell proliferation and survival. This compound is valuable in research applications focused on overcoming resistance mechanisms in KRas-driven malignancies. -
CDK Inhibitor
(S)-CR8 is a selective inhibitor of cyclin-dependent kinases (CDKs), demonstrating potent inhibitory activity with IC50 values of 0.060 μM for CDK2/cyclin E, 0.080 μM for CDK2/cyclin A, 0.11 μM for CDK9/cyclin T, 0.12 μM for CDK5/p25, and 0.15 μM for CDK1/cyclin B. This compound effectively reduces the survival of SH-SY5Y cells, with an IC50 of 0.40 μM, making it a valuable tool for studying cell cycle regulation and potential therapeutic strategies in cancer research.
