Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
Smoothened Inhibitor
PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ?? 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ?? 1.4 nmol/L in cells. -
Wnt inhibitor
IWP-3 is an inhibitor of Wnt production. Blocks Wnt pathway activity in vitro ( IC?????€ = 40 nM). IWP-3 inactivates Porcupine (Porcn), a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion. Through blockade of Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC?????€ = 1.2 μM). -
YAP Inhibitor
MY-1076 is a selective inhibitor of the Yes-associated protein (YAP), which plays a critical role in various cellular processes, including cell proliferation and apoptosis. This compound promotes the degradation of YAP, leading to induced apoptosis in tumor cells. MY-1076 demonstrates potent antiproliferative effects against gastric and colorectal cancer cell lines, including MGC-803, SGC-7901, HCT-116, and KYSE450, with IC50 values of 0.019, 0.017, 0.020, and 0.044 μM, respectively. It is a valuable tool for researching YAP's role in cancer biology and potential therapeutic interventions. -
WNT Inhibitor
WNTinib is a selective WNT signaling inhibitor targeting mutated β-catenin (CTNNB1) in hepatocellular carcinoma (HCC). By effectively disrupting the oncogenic Wnt pathway, WNTinib inhibits key kinases such as KIT and MAPK, leading to the reduction of EZH2 activation. This compound is suitable for research applications focused on cancer biology and the mechanisms of liver tumorigenesis. -
CK1α Inhibitor
Casein Kinase Inhibitor A86 is a selective inhibitor of casein kinase 1α (CK1α), demonstrating potent oral bioactivity. In addition to its primary target, A86 also inhibits cyclin-dependent kinase 7 (CDK7) and cyclin-dependent kinase 9 (CDK9), contributing to its diverse pharmacological profile. This compound has been shown to induce apoptosis in leukemia cells, highlighting its potential as an anti-leukemic agent in cancer research applications. -
GSK-3β Inhibitor
GSK-3β Inhibitor 3 is a potent and selective irreversible covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), exhibiting an IC50 of 6.6 μM. This compound is instrumental in research applications related to acute promyelocytic leukemia, providing insights into GSK-3β's role in cancer signaling pathways and therapeutic strategies. Its specificity allows for detailed studies of GSK-3β inhibition effects on cellular processes and pathways involved in oncogenesis. -
Hedgehog Inhibitor
CUR61414 is a potent inhibitor of the Hedgehog signaling pathway, specifically targeting the Smoothened (Smo) protein with a Ki value of 44 nM. This small-molecule aminoproline derivative demonstrates selective activity, inducing apoptosis in cancer cells while sparing adjacent non-tumor cells. CUR61414 is valuable for research applications focused on cancer biology and therapeutic strategies aimed at manipulating Hedgehog pathway activity. -
Wnt/β-catenin Inhibitor
KWZY-11 is a potent Wnt/β-catenin inhibitor that effectively modulates the associated signaling pathway. This compound demonstrates strong biological activity by inducing DNA damage and promoting apoptosis specifically in MDA-MB-231 breast cancer cells. Its dual inhibition of PARP and CDK6 enhances its potential applications in cancer research, particularly for therapeutic strategies targeting tumor cell proliferation. -
CK2 Inhibitor
CX-5011 free base is a potent inhibitor of casein kinase 2 (CK2), targeting this serine/threonine kinase to modulate cellular signaling pathways. It also serves as a Rac-1 activator, enhancing processes such as methuosis and macropinocytosis. The compound has been shown to induce apoptosis and decrease the phosphorylation of ribosomal protein S6 (rpS6), making it a valuable tool for research applications in cancer biology and cellular metabolism. -
GLI-1 Inhibitor
GLI1-IN-1 is a potent inhibitor of GLI-1, effectively targeting the Hedgehog (HH) signaling pathway with an IC50 of 1.3 μM. This compound demonstrates significant anticancer activity, inducing apoptosis and inhibiting growth in colorectal cancer cells. GLI1-IN-1’s excellent water solubility enhances its applicability for various research studies focused on cancer biology and therapeutic interventions. -
CDK Inhibitor
5,6-Dichlorobenzimidazole riboside (DRB) functions as a selective inhibitor of several carboxyl-terminal domain kinases, notably casein kinase II and cell cycle-dependent kinases (CDKs). This nucleoside analog exhibits antitumor activity and has been shown to induce apoptosis in targeted cancer cells. Its role in modulating kinase activity makes DRB valuable for research in cancer biology and cell cycle regulation. -
γ-secretase Inhibitor
Nirogacestat dihydrobromide is a selective, noncompetitive inhibitor of γ-secretase, with a reported IC50 of 6.2 nM. This compound effectively inhibits Notch signaling, making it a valuable tool for studying Notch receptor-dependent cancers while minimizing gastrointestinal toxicity. It is particularly useful in research focused on the role of γ-secretase in cancer biology and therapeutic development. -
Selective p38α Inhibitor
AMG-548 dihydrochloride is a selective p38α inhibitor with a Ki of 0.5 nM, exhibiting moderate selectivity towards p38β (Ki = 36 nM) and over 1000-fold selectivity against p38γ and p38δ isoforms. This compound demonstrates potent inhibition of TNFα production in whole blood stimulated by LPS, with an IC50 of 3 nM. Additionally, AMG-548 dihydrochloride inhibits Wnt signaling by directly targeting Casein kinase 1 isoforms δ and ε, making it valuable for research in inflammation and signaling pathways. -
CK2 Inhibitor
(E/Z)-GO289 is a potent and selective inhibitor of casein kinase 2 (CK2) with an IC50 of 7 nM. This compound significantly extends the circadian period and demonstrates cell type-dependent inhibition of cancer cell growth, which correlates with cellular clock function. (E/Z)-GO289 is valuable for research into circadian biology and cancer therapeutics. -
CK1 Inhibitor
CKI-7 free base is a selective casein kinase 1 (CK1) inhibitor that operates through an ATP-competitive mechanism, exhibiting an IC50 of 6 μM and a Ki of 8.5 μM. In addition to its primary action on CK1, CKI-7 also inhibits Cdc7 kinase, SGK, ribosomal S6 kinase-1 (S6K1), and mitogen- and stress-activated protein kinase-1 (MSK1). This compound demonstrates minimal activity against casein kinase II and other protein kinases, making it a valuable tool for research applications focused on cell cycle regulation and signal transduction pathways. -
CSNK1α Inhibitor
BAY-204 is a selective inhibitor of casein kinase 1 alpha (CSNK1α), functioning through ATP-competitive mechanisms with an IC50 of 2 nM at 10 μM ATP and 12 nM at 1 mM ATP. This compound is primarily utilized in research focused on acute myeloid leukemia (AML), providing valuable insights into the role of CSNK1α in cancer biology and potential therapeutic interventions. -
CSNK1A1/CSNK1D Inhibitor
BAY-888 is a selective inhibitor of casein kinase 1α (CK1α/CSNK1A1) that acts through ATP-competitive mechanisms, exhibiting an IC50 of 4 nM at 10 μM ATP and 63 nM at 1 mM ATP. This compound disrupts the negative regulatory effects of CK1α on p53 and other associated signaling pathways, thereby inducing apoptosis and inhibiting tumor cell proliferation. BAY-888 has demonstrated efficacy against various cancers, including acute myeloid leukemia (AML), and is utilized in research focused on the development of anticancer therapeutics for p53 wild-type tumors and exploring mechanisms in CK1α-related signaling pathways. -
CK1 Inhibitor
CK1-IN-2 is a selective inhibitor of casein kinase 1 (CK1) with demonstrated IC50 values of 123 nM for CK1α, 19.8 nM for CK1δ, 26.8 nM for CK1ε, and 74.3 nM for p38α. This compound exhibits significant inhibition of CK1 activity, making it a valuable tool for dissecting CK1-mediated signaling pathways. CK1-IN-2 is useful in oncology and neurobiology research, particularly in studies exploring cell proliferation, apoptosis, and circadian rhythm regulation. -
CK2 Inhibitor
CK2 Inhibitor 2 targets Casein Kinase 2 (CK2) and acts as a potent, selective inhibitor with an IC50 of 0.66 nM. This compound demonstrates a high degree of selectivity for CK2, exhibiting an IC50 of 32.69 nM against Clk2. CK2 Inhibitor 2 has been shown to exert significant antiproliferative and antitumor effects, making it a valuable tool for research related to cancer biology and signal transduction. -
Casein Kinase Inhibitor
TBCA is a selective inhibitor of casein kinase II (CK2), exhibiting an IC50 of 110 nM and a Ki value of 77 nM. This compound demonstrates a significant preference for CK2 over CK1, DYRK1A, and a diverse panel of 27 other kinases. TBCA is valuable for research applications focused on studying the role of CK2 in cellular signaling and disease mechanisms. -
Casein Kinase Inhibitor
PI-828 is a dual inhibitor of phosphoinositide 3-kinase (PI3K) and casein kinase 2 (CK2), exhibiting IC50 values of 173 nM for p110α, 149 nM for CK2, and 1127 nM for CK2α2 in lipid kinase assays. This compound demonstrates significant biological activity by modulating key signaling pathways involved in cell growth and survival. PI-828 is utilized in research applications focused on cancer biology, providing insights into tumorigenesis and potential therapeutic interventions targeting these kinases. -
CSNK2A Inhibitor
CSNK2A-IN-1 is a selective inhibitor of Casein Kinase 2 Alpha (CSNK2A), a crucial regulator in various cellular processes. This compound exhibits antiviral activity and demonstrates improved selectivity compared to other kinases, such as PIM3. CSNK2A-IN-1 is relevant for research applications involving studies of viral pathogenesis and kinase signaling pathways. -
CK2α Inhibitor
CK2α-IN-1 is a selective inhibitor of casein kinase 2 alpha (CK2α) with an IC50 value of 7.0 µM and a Ki of 1.6 µM. This compound operates through a non-ATP-competitive mechanism, making it a valuable tool for investigating CK2α's role in cellular regulation. CK2α-IN-1 shows promising potential for anticancer research applications, providing insights into cancer cell proliferation and survival pathways. -
CSNK1D/CSNK1E Inhibitor
JNJ-6204 is a potent dual inhibitor of Casein Kinase 1 Delta (CSNK1D) and Casein Kinase 1 Epsilon (CSNK1E), with IC50 values of 2.3 nM and 137 nM, respectively. This compound exhibits significant brain penetration, making it a valuable tool for investigating the roles of CSNK1D and CSNK1E in cellular signaling and neurobiology. JNJ-6204 is particularly useful in the study of diseases associated with dysregulated Wnt signaling and circadian rhythm disturbances. -
CK-1δ Inhibitor
Casein kinase 1δ-IN-6 is a selective inhibitor of protein kinase CK-1δ, demonstrated by an IC50 of 23 nM. This compound exhibits neuroprotective and anti-inflammatory effects, both in vitro and in vivo, making it a valuable tool for studying neurodegenerative diseases. Its specific mechanism of action and ability to modulate CK-1δ activity position it as a promising candidate for therapeutic research. -
CK2/SRPK1 Dual Inhibitor
SRPIN803 is a dual inhibitor of casein kinase 2 (CK2) and serine/arginine-rich protein-specific kinase 1 (SRPK1), with IC50 values of 203 nM and 2.4 μM, respectively. This compound demonstrates antiangiogenic properties, making it a valuable tool for studies related to angiogenesis. SRPIN803 is particularly relevant for researching therapeutic strategies in age-related macular degeneration and other conditions influenced by vascular growth. -
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. -
CK2 Inhibitor
CK2-IN-10 is an allosteric inhibitor of casein kinase 2 (CK2), known for its role in cellular signaling and proliferation. This compound demonstrates significant potential in cancer research by inhibiting CK2 activity, which is often dysregulated in various malignancies. CK2-IN-10 can be utilized in studies focusing on cancer cell growth, survival mechanisms, and therapeutic resistance, making it a valuable tool for advancing cancer biology research. -
CK1d Inhibitor
Casein kinase 1δ-IN-3 is a selective inhibitor of casein kinase 1 delta (CK1d) with a pIC50 of 6.5376 M. This compound is instrumental in studying CK1d's role in various biological processes, including circadian rhythm regulation and signaling pathways. Its inhibitory activity makes it a valuable tool for investigating CK1d-related functions in cellular and molecular research. -
CK1/CHK1 Inhibitor
MRT00033659 is a selective inhibitor targeting casein kinase 1 (CK1) and checkpoint kinase 1 (CHK1), with IC50 values of 0.9 μM and 0.23 μM, respectively. As a pyrazolo-pyridine analogue, MRT00033659 activates the p53 signaling pathway and causes destabilization of E2F-1. This compound is valuable for research investigating cell cycle regulation, DNA damage response, and therapeutic strategies in cancer biology. -
Casein kinase 1δ Inhibitor
Casein kinase 1δ-IN-8 is an inhibitor of Casein kinase 1δ, a serine/threonine kinase implicated in various cellular processes. This compound is valuable for research into neurodegenerative disorders, including Alzheimer's disease, by elucidating the role of Casein kinase 1δ in disease pathology and potential therapeutic interventions. Its selective inhibition allows for targeted studies of kinase activity and its downstream effects in relevant biological systems. -
CK1δ Inhibitor
Casein kinase 1δ-IN-1 is a selective inhibitor of casein kinase 1δ (CK1δ), which plays a crucial role in various cellular processes. This compound exhibits significant biological activity in modulating CK1δ signaling pathways, making it a valuable tool for investigating the mechanisms underlying neurodegenerative diseases, particularly tauopathies. Researchers can utilize Casein kinase 1δ-IN-1 to explore its effects on tau phosphorylation and the potential therapeutic implications for related disorders. -
CK2 Inhibitor
CK2-IN-4 is a selective inhibitor of casein kinase 2 (CK2), with an IC50 of 8.6 µM. This compound exhibits significant potential for investigating its role in cancer progression, viral pathogenesis, and glomerulonephritis. Researchers can utilize CK2-IN-4 to study the mechanisms underlying CK2-related signaling pathways and to explore therapeutic avenues in related diseases. -
CKIα/δ Inhibitor
NCC007 is a dual inhibitor of casein kinases Iα (CKIα) and δ (CKIδ), demonstrating IC50 values of 1.8 μM and 3.6 μM, respectively. This compound is effective in modulating mammalian circadian rhythms, making it a valuable tool in chronobiology research. Its use can facilitate studies aimed at understanding the molecular mechanisms underlying circadian regulation and potential therapeutic interventions for circadian-related disorders. -
CK1δ/ε Inhibitor
SR-1277 is a potent and selective inhibitor of casein kinase 1 delta (CK1δ) and epsilon (CK1ε), demonstrating ATP-competitive inhibition with IC50 values of 49 nM and 260 nM, respectively. Additionally, it exhibits inhibitory effects on FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K, with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. SR-1277 is primarily employed in cancer research, contributing to studies investigating CK1-mediated signaling pathways and therapeutic potential. -
Casein Kinase Inhibitor
Casein Kinase II Inhibitor IV hydrochloride is a selective inhibitor of Casein Kinase II (CK2), a serine/threonine kinase involved in various cellular processes. This compound promotes differentiation in epidermal keratinocytes, making it valuable for research on skin biology and related disorders. Additionally, it can be used to explore the roles of CK2 in cell proliferation, apoptosis, and signaling pathways. -
PI3Kδ/CK1ε Inhibitor
Umbralisib tosylate is a potent and selective dual inhibitor of PI3Kδ and casein kinase-1-ε (CK1ε), exhibiting an EC50 of 22.2 nM and 6.0 μM, respectively. This compound demonstrates significant immunomodulatory effects on T cells from chronic lymphocytic leukemia (CLL) patients. Umbralisib tosylate is primarily utilized in research focused on hematological malignancies to elucidate its therapeutic potential and mechanisms of action. -
PI3Kδ/CK1ε Inhibitor
Umbralisib sulfate is a potent and selective dual inhibitor of PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. This compound demonstrates notable immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). Umbralisib sulfate is a valuable tool for research into hematological malignancies, facilitating studies on cell signaling pathways and potential therapeutic strategies. -
CK1 Inhibitor
PF-4800567 hydrochloride is a potent and selective inhibitor of casein kinase 1 (CK1), exhibiting an IC50 of 32 nM. It demonstrates over 20-fold selectivity for CK1α when compared to CK1δ, with an IC50 value of 711 nM. This compound is valuable for investigating the distinct roles of these kinases in various signaling pathways, making it an essential tool for research in cellular signaling and kinase-related studies. -
CK1δ Inhibitor
Casein kinase 1δ-IN-9 is a potent inhibitor of casein kinase 1δ (CK1δ), a key regulator in various cellular processes. This compound is particularly relevant for research focused on neurodegenerative disorders, including Alzheimer's disease, by modulating CK1δ activity. Its ability to influence signaling pathways makes it a valuable tool for investigating disease mechanisms and potential therapeutic interventions. -
Casein Kinase Inhibitor
Casein kinase 1δ-IN-20 is a selective inhibitor of casein kinase 1δ, targeting this enzyme's crucial role in various cellular processes. This compound exhibits significant biological activity relevant to the modulation of signaling pathways involved in neurodegenerative diseases, including Alzheimer's disease. Its application in research can aid in unraveling the mechanisms underlying these conditions and support the development of therapeutic strategies. -
CK1 Inhibitor
CK1δ-IN-10 is a selective inhibitor of casein kinase 1 delta (CK1δ), exhibiting an IC50 value of 0.255 μM. This compound is utilized in research applications focusing on signal transduction pathways, cell cycle regulation, and protein phosphorylation. Its ability to modulate CK1δ activity makes it a valuable tool for investigating the roles of this kinase in various cellular processes and diseases. -
Casein Kinase Inhibitor
Casein kinase 1δ-IN-21 is a potent inhibitor of casein kinase 1δ, a key regulator in various signaling pathways. By selectively targeting this kinase, it demonstrates significant potential for modulating cellular processes associated with neurodegenerative diseases, including Alzheimer's disease. This compound is valuable for research into the therapeutic mechanisms and targets of such conditions.
