Catalog No.
Product Name
Application
Product Information
Citations
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Aurora Kinase Inhibitor
Tripolin A is a selective non-ATP competitive inhibitor of Aurora A kinase, exhibiting IC50 values of 1.5 μM for Aurora A and 7 μM for Aurora B. This compound plays a crucial role in modulating cell cycle progression by targeting Aurora kinases, making it valuable in cancer research. Tripolin A is used to investigate the mechanisms of mitotic regulation and potential therapeutic strategies in tumor cells. -
Aurora Kinase Inhibitor
XMD-12 is a selective Aurora kinase inhibitor that demonstrates significant anti-tumor activity. It effectively enhances paclitaxel-induced cell death and exhibits high potency against Aurora A, B, and C kinases, with IC50 values of 5.6, 18.4, and 24.6 nM, respectively. This compound is valuable for research applications in cancer biology and therapy development. -
Aurora Kinases Inhibitor
Aurora kinase-IN-2 is a potent inhibitor of Aurora kinases, demonstrating IC50 values of 90 nM for Aurora A and 152 nM for Aurora B. This compound effectively induces cell cycle arrest at the G2/M phase by modulating cyclin B1 and cdc2. It is primarily utilized in cancer research to explore the role of Aurora kinases in tumorigenesis and therapeutic response. -
Aurora A Inhibitor
Aurora A Inhibitor 1 is a potent and selective inhibitor of the Aurora A kinase, which plays a crucial role in regulating cell division and has been implicated in various cancers. Overexpression of Aurora A is associated with oncogenic properties, making it an important target for cancer research. This compound is suitable for studies focusing on the therapeutic modulation of Aurora A in diverse cancer types. -
Aurora Kinase Inhibitor
Aurora kinase inhibitor-9 is a potent dual inhibitor of Aurora A and Aurora B kinases, exhibiting IC50 values of 0.093 µM and 0.09 µM, respectively. This compound demonstrates significant anti-proliferative activity across various cancer cell lines, making it a valuable tool in cancer research. Its ability to target key regulators of cell division positions it as a candidate for studies investigating mitotic disruption and the development of novel cancer therapies. -
Aurora Inhibitor
TAK-901 hydrochloride is a potent inhibitor of aurora kinases A and B, exhibiting IC50 values of 21 nM and 15 nM, respectively. This compound disrupts cell cycle progression, making it a valuable tool in cancer research and therapeutic development. Its ability to inhibit aurora kinases positions TAK-901 hydrochloride as an important reagent for studying mitotic regulation and exploring targeted cancer therapies. -
Aurora A PROTAC Degrader
PROTAC Aurora A Degrader-1 is a selective degrader that targets Aurora A, effectively forming a ternary complex with AURKA and CRBN. This compound demonstrates potent biological activity, inducing degradation of AURKA, lowering MYCN levels, and promoting DNA damage and apoptosis in cancer cells. With DC50 values of 1 nM and 2 nM in LAN5 and SMS-SAN cells, respectively, it exhibits significant antiproliferative effects and is valuable for research on neuroblastoma and small cell lung cancer. -
Aurora Kinase Inhibitor
Tripolin B is an ATP-competitive inhibitor targeting Aurora kinases, exhibiting IC50 values of 2.5 µM and 6 µM for Aurora A and Aurora B kinases, respectively. This compound has demonstrated selectivity in its inhibition profile and is primarily utilized in cellular studies to explore the roles of Aurora kinases in cell cycle regulation and cancer progression. Tripolin B can be a valuable tool in research focused on cell division and oncogenic signaling pathways. -
Aurora Kinase Inhibitor
BI 831266 is a potent and selective inhibitor of Aurora kinase B, a critical regulator of mitosis. This compound exhibits significant antitumor activity, making it valuable for cancer research. Its inhibition of Aurora B can lead to disruptions in cell division, providing insights into potential therapeutic applications for various malignancies. -
Aurora A/B Kinases Inhibitor
TY-011 is a selective inhibitor of Aurora A and B kinases, disrupting normal microtubule-kinetochore attachment. This interference results in DNA damage and apoptosis, effectively inhibiting the proliferation of human gastric cancer cells, with observed IC50 values between 0.11 and 4.49 μM across various gastric cancer cell lines. TY-011 serves as a valuable tool in the study of gastric cancer and the mechanisms underlying mitotic regulation. -
Aurora Kinase Inhibitor
OM137 is a potent Aurora Kinase inhibitor, demonstrating IC50 values of 21.7 μM for Aurora A kinase and 2.4 μM for Aurora B kinase. Additionally, OM137 affects cell cycle regulation by inhibiting Cdk1/cyclinB and Cdk5/p25, also with an approximate IC50 of 20 μM. This compound is notable for its ability to reduce spindle checkpoint-signaling proteins, such as Mad2 and BubR1, at the kinetochores of chromosomes, making it a valuable tool in cancer research and studies on mitotic regulation. -
Aurora Kinase Inhibitor
AT9283 hydrochloride is a multi-targeted kinase inhibitor that primarily targets Aurora A and Aurora B kinases, which play critical roles in cell proliferation and survival. Its inhibitory effects extend to additional kinases such as JAK2 and Abl (T315I), enhancing its potential utility in cancer research. AT9283 hydrochloride has demonstrated significant anti-tumor activity, making it a valuable tool for investigating therapeutic strategies in various malignancies. -
Aurora Kinase Inhibitor
VE-465 is a potent Aurora kinase inhibitor that promotes apoptosis in cancer cells. Its anticancer activities have been demonstrated across various tumor models, making it a valuable tool for cancer research. This compound's ability to selectively target Aurora kinases positions it as a significant candidate for investigations into tumor progression and treatment strategies. -
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 Control
Win 47338 is a control compound targeting Aurora kinases (AurA/AurB) and the mitotic kinase monopolar spindle 1 (MPS1). It serves as a crucial reference for studies involving mitotic regulation and cellular division processes. With a Ki value greater than 100 μM, it provides a baseline for evaluating the potency of other kinase inhibitors in research applications focused on cell cycle dynamics and cancer therapeutics. -
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. -
WEE1 HEMTAC Degrader
HEMTAC WEE1 degrader-1 is a HSP90-mediated degrader specifically targeting the WEE1 kinase, with an IC50 of 16.76 nM for HSP90 inhibition. This compound facilitates the ubiquitination and subsequent degradation of WEE1, effectively disrupting the G2/M cell cycle checkpoint. It demonstrates significant anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft models, making it a valuable reagent for research applications in AML therapeutics. -
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. -
G-quadruplex Ligand
G-quadruplex ligand 1 targets G-quadruplex structures in DNA, disrupting their stability. This ligand significantly enhances gene expression by altering the conformation of G-quadruplexes, making it a valuable tool for studies involving gene regulation and potential therapeutic applications. Its unique properties facilitate investigations into the roles of G-quadruplexes in cellular processes and disease mechanisms. -
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. -
G-quadruplex
PT-ttpy is a metallo-organic complex that acts as a potent ligand for G-quadruplex structures. It effectively induces telomere-related DNA damage in cancer cells by inhibiting telomerase activity and disrupting telomere functions. Additionally, PT-ttpy is associated with various chromatin abnormalities during mitosis, including the formation of chromatin bridges, ultrafine bridges (UFBs), and double-stranded breaks (DSBs). This reagent is valuable for research in cancer biology and the study of telomere dynamics. -
KRASG12D PROTAC Degrader
PROTAC K-Ras Degrader-5 is a cereblon-based PROTAC specifically designed to target KRASG12D, achieving a DC50 of less than 100 nM. This reagent facilitates the recruitment of KRASG12D to the cereblon E3 ubiquitin ligase complex, leading to its ubiquitination and proteasomal degradation. As a result, it effectively reduces pERK levels and inhibits the proliferation of cancer cells. PROTAC K-Ras Degrader-5 also enhances caspase 3/7 activity and cleaved PARP levels, indicative of apoptosis, in pancreatic cancer models. This compound is a valuable tool for researching both pancreatic and colorectal cancer. -
ROCK/ERK/GSK/AGC Inhibitor
ROCK-IN-5 (compound I-B-37) is a potent inhibitor of Rho-associated protein kinase (ROCK), as well as ERK, GSK-3, and AGC protein kinases. This compound exhibits significant biological activity in regulating cellular proliferation and has applications in researching cardiac conditions and neurodegenerative diseases. Its broad inhibitory profile makes it a valuable tool for studies aimed at understanding signaling pathways involved in various disease mechanisms. -
KRAS G12C Inhibitor
KRAS G12C-IN-76 is a selective inhibitor of the KRAS G12C mutation, a prominent driver in various cancers. This compound effectively reduces ERK phosphorylation, thereby impeding signaling pathways involved in tumor growth and proliferation. KRAS G12C-IN-76 demonstrates significant anti-cancer activity, particularly in pancreatic cancer models, making it a valuable tool for research in targeted therapies and cancer biology. -
KRas G12V Inhibitor
KRAS-IN-51 is a selective inhibitor of the KRas G12V mutant, exhibiting an IC50 of 2.9 nM. It demonstrates effective inhibition of pERK phosphorylation and shows significant anti-proliferative activity in colorectal cancer (SW620) and pancreatic cancer (MIAPaCa-2) cell lines. This compound is valuable for research focused on KRas-driven malignancies, contributing to the understanding of therapeutic strategies targeting KRas mutations. -
KRAS G12C Inhibitor
KRAS G12C Inhibitor 61 is a selective inhibitor targeting the KRAS G12C mutation. It effectively inhibits phospho-ERK 1/2 in MIA PaCa-2 cells, exhibiting an IC50 of 9 nM. This compound is valuable for research into pancreatic, colorectal, and lung cancers, contributing to studies focused on therapeutic strategies for KRAS-driven malignancies. -
KRAS(Q61H) Inhibitor
RM-046 is a selective inhibitor targeting the KRAS(Q61H) mutant, functioning through the formation of a ternary complex with cyclophilin A. This compound non-covalently binds to activated KRASQ61H, obstructing effector binding and thereby inhibiting downstream signal transduction pathways. RM-046 has demonstrated efficacy in suppressing ERK phosphorylation, stalling cancer cell proliferation, and promoting anti-tumor activity, including tumor regression in preclinical xenograft studies. It serves as a valuable tool for investigating KRASQ61H-associated malignancies. -
KRAS G12D Inhibitor
KRAS G12D-IN-27 is a selective inhibitor targeting the KRAS G12D mutant protein. It effectively inhibits ERK phosphorylation, exhibiting an IC50 of 112 nM. This compound is valuable for cancer research, particularly in studies focused on the KRAS signaling pathway and downstream effects in tumor biology. -
KRASG12C Inhibitor
KRASG12C IN-15 is a potent inhibitor of the KRASG12C mutation, functioning primarily by obstructing the SOS1-mediated GDP/GTP exchange, with an IC50 of 19 nM. It effectively inhibits ERK phosphorylation with an IC50 of 0.051 μM and demonstrates significant anti-proliferative effects on KRASG12C-mutated MIA PaCa-2 cells, with an IC50 of 0.023 μM. In vivo studies reveal that KRASG12C IN-15 exhibits notable antitumor efficacy in MIA PaCa-2 xenograft mouse models. This compound is valuable for investigating KRASG12C-associated signaling pathways and developing targeted therapies. -
ROCK2 Inhibitor
NRL-1049 dihydrochloride is a selective inhibitor of rho-associated protein kinase 2 (ROCK2), exhibiting an IC50 value of 0.59 μM. This compound demonstrates a remarkable selectivity for ROCK2 over ROCK1, with an IC50 of 26 μM, effectively inhibiting ROCK2 activity. NRL-1049 dihydrochloride has significant potential in research applications focused on the preservation of the blood-brain barrier following acute injury. -
ROCK Inhibitor
Zelasudil is a selective inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2), demonstrating significant anti-fibrotic activity. This small molecule enhances immunomodulatory responses in metastatic pancreatic tumors, promoting increased infiltration of CD8+ and CD4+ T cells while reducing FOXP3+ regulatory T cells at the tumor periphery. Zelasudil shows potential for advancing research in pancreatic ductal adenocarcinoma and related therapeutic strategies. -
ROCK/NET Inhibitor
Netarsudil functions as a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). This compound effectively reduces intraocular pressure through ROCK inhibition, promoting relaxation of trabecular meshwork cells and dilation of episcleral veins, facilitating aqueous humor outflow while simultaneously decreasing aqueous humor production via NET inhibition. Netarsudil is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma. -
ROCK2 Inhibitor
Belumosudil mesylate is a selective inhibitor of the Rho-associated kinase 2 (ROCK2), demonstrating an IC50 of 105 nM for ROCK2 and 24 µM for ROCK1. This compound exhibits significant anti-fibrotic properties, making it valuable for research in fibrosis-related pathways and diseases. Belumosudil mesylate is applicable in studies aimed at understanding the role of ROCK signaling in various physiological and pathological processes. -
ROCK Inhibitor
SAR407899 is a selective and potent ROCK inhibitor that acts competitively with ATP, exhibiting an IC50 of 135 nM for ROCK-2 and Kis of 36 nM in human and 41 nM in rat ROCK-2. This compound demonstrates stable inhibition of migrasome formation and is valuable for research into cellular migration and related processes. Its application in studies of ROCK signaling pathways may enhance the understanding of various physiological and pathological conditions. -
ROCK/NET Inhibitor
Netarsudil dimesylate is a potent inhibitor of Rho-associated kinases (ROCK I and ROCK II) and also serves as a reversible inhibitor of the norepinephrine transporter (NET). It effectively reduces intraocular pressure through ROCK inhibition, leading to the relaxation of trabecular meshwork cells and dilation of episcleral veins, which facilitates aqueous humor outflow, while simultaneously inhibiting NET to diminish aqueous humor production. This compound is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma. -
ROCK Inhibitor
Sovesudil is a potent Rho kinase (ROCK) inhibitor that functions through ATP-competitive mechanisms, exhibiting IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II. It effectively lowers intraocular pressure (IOP) while minimizing the risk of hyperemia, making it a valuable compound for ocular research and potential therapeutic applications in glaucoma treatment and other related conditions. -
ROCK Inhibitor
Verosudil is a potent Rho-associated protein kinase (ROCK) inhibitor, demonstrating robust inhibitory activity against both ROCK1 and ROCK2 with a Ki value of 2 nM. Its relatively lower selectivity for other kinases such as PKA, PKCT, MRCKA, and CAMK2A provides additional research avenues. Verosudil enhances trabecular outflow capacity, making it a valuable reagent in studies targeting intraocular pressure reduction. This compound is particularly relevant for research focused on glaucoma and ocular hypertension. -
ROCK Inhibitor
3-(4-Pyridyl)indole is a selective Rho-kinase (ROCK) inhibitor, exhibiting an IC50 value of 25 μM. This compound is known to effectively inhibit cellular blebbing and promote the dissolution of actin stress fibers, making it a valuable reagent for studying wound healing mechanisms and cytoskeletal dynamics in various biological research applications. -
ROCK Inhibitor
GSK269962A hydrochloride is a potent ROCK inhibitor that selectively targets Rho-associated coiled-coil kinase 1 (ROCK1) and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively. It exhibits significant anti-inflammatory and vasodilatory properties, making it valuable in research applications focused on vascular biology, cardiovascular diseases, and inflammatory conditions. This compound provides a useful tool for elucidating the role of ROCK signaling in various biological processes. -
ROCK Inhibitor
CAY10746 is a selective inhibitor of Rho-associated protein kinase (ROCK), demonstrating potent inhibitory activity against ROCK I and ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. This compound is particularly relevant for research into diabetic retinopathy (DR) and other conditions associated with abnormal vascular function. Its ability to modulate ROCK activity makes it a valuable tool in studying cellular pathways involved in inflammation and tissue remodeling. -
ROCK/PKC Inhibitor
(rac)-AR-13503 is a potent inhibitor of Rho-associated protein kinase (ROCK) and protein kinase C (PKC). It plays a significant role in regulating angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. Additionally, (rac)-AR-13503 has demonstrated the ability to inhibit aberrant neovascularization in the oxygen-induced retinopathy (OIR) model in mice, making it a valuable tool for research in ocular disorders and vascular biology. -
ROCK Inhibitor
Rho-Kinase-IN-2 is a selective inhibitor of Rho Kinase (ROCK) with an IC50 value of 3 nM for ROCK2. This orally active and CNS-permeable compound is significant for investigating the role of ROCK in neurodegenerative disorders, particularly Huntington's disease. Its potent inhibition of this pathway makes it a valuable tool for exploring therapeutic strategies targeting ROCK activity in relevant biological models. -
ROCK Inhibitor
Sovesudil hydrochloride is a highly selective Rho kinase (ROCK) inhibitor that competitively binds to ATP, demonstrating IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II. It effectively reduces intraocular pressure (IOP) and is noteworthy for its ability to do so without causing hyperemia. This compound is utilized in research focused on glaucoma and other ocular conditions linked to elevated IOP. -
ROCK2 Inhibitor
ROCK2-IN-6 hydrochloride is a selective inhibitor of Rho-associated protein kinase 2 (ROCK2). It modulates ROCK2 activity, making it a valuable tool for studying disorders associated with ROCK signaling, including autoimmune diseases and inflammation. This compound is ideal for research aimed at understanding the role of ROCK2 in various biological processes and therapeutic interventions. -
ROCK2 Inhibitor
ROCK2-IN-8 is an orally active inhibitor of Rho-associated protein kinase 2 (ROCK2) with an IC50 of 7.2 nM. This compound is valuable in studies investigating aqueous humor outflow in porcine eyes, as well as the phosphorylation of myosin light chain. Its specificity for ROCK2 makes it a useful tool in exploring the roles of this kinase in various biological processes. -
ROCK1 Inhibitor
GSK-25 is a potent and selective inhibitor of ROCK1, demonstrating an IC50 of 7 nM. This compound exhibits excellent selectivity against a diverse panel of 31 kinases, with over 100-fold selectivity compared to RSK1 (IC50 = 398 nM) and p70S6K (IC50 = 1 µM). GSK-25 is also characterized by its inhibitory effects on specific cytochrome P450 enzymes, with IC50 values of 2.5 µM, 5.2 µM, and 2.5 µM for CYP2C9, CYP2D6, and CYP3A4, respectively. This makes GSK-25 suitable for research applications focused on cell signaling and pharmacological studies involving the ROCK pathway. -
ROCK1 Inhibitor
ROCK1-IN-1 is a selective ROCK1 inhibitor with a Ki value of 540 nM. This compound is utilized in research focused on hypertension, glaucoma, and erectile dysfunction by modulating the Rho-associated protein kinase pathway. Its inhibition of ROCK1 activity provides insight into various physiological processes and potential therapeutic interventions for related disorders. -
ROCK2 Inhibitor
NRL-1049 is a selective inhibitor of ROCK2, demonstrating an IC50 of 0.59 µM for ROCK2 and 26 µM for ROCK1. This compound effectively reduces Lysophosphatidic acid-induced ROCK activation in endothelial cells and has shown potential in animal models by decreasing lesion volume and hemorrhagic transformation associated with cavernous angiomas. Additionally, NRL-1049 preserves the blood-brain barrier, suppresses seizure activity following brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice, making it a valuable tool for research into neurological disorders and vascular pathologies.
