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Catalog No.
Product Name
Application
Product Information
Citations
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Wnt/β-catenin signaling inhibitor
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. -
gamma secretase inhibitor
BMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor. -
Casein kinase 1ε inhibitor
PF-4800567 is a potent and selective inhibitor of casein kinase 1ε (CK1ε), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). -
GSK-3α/β inhibitor
CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. -
GSK-3α/β inhibitor
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM. -
CK1δ/ε inhibitor
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. -
YAP/TAZ inhibitor
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μμ in firefly luciferase assay. -
dual PDE7/GSK-3 inhibitor
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS). -
dyneins 1/2 inhibitor
Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. -
GSK-3β inhibitor
GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM. -
CDK1, CDK5, and GSK-3βinhibitor
Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively. -
GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively. -
γ-secretase inhibitor
MRK 560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo. -
GSK-3 inhibitor
BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity. -
Potent porcupine inhibitor
Porcn-IN-1 is potent porcupine inhibitor with an IC50 of 0.5??0.2 nM. -
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. -
GSK-3β Inhibitor
Manzamine A is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) and cyclin-dependent kinase 5 (CDK-5), with respective IC50 values of 10.2 μM and 1.5 μM. This compound exhibits significant biological activity, including antimalarial and anticancer effects, and has been shown to inhibit autophagy in pancreatic cancer cells by targeting vacuolar ATPases. Additionally, Manzamine A demonstrates potent antiviral properties against herpes simplex virus type 1 (HSV-1), making it a valuable reagent for diverse research applications in cancer, autophagy, and virology studies. -
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.
