Catalog No.
Product Name
Application
Product Information
Product Citation
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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). -
Smoothened inhibitor
BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity.- Valérian Pasche, .et al. , Parasit Vectors, 2018, 11: 298 PMID: 29764454
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GLI antagonist
GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.- Cheng Zhou, .et al. , Cell Death Dis, 2021, Mar 3;12(3):231 PMID: 33658491
- Hui Liang, .et al. , Sci Rep, 2017, 7: 40361 PMID: 28098170
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Notch inhibitor
LY3039478 is a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested. -
PKA, PKG, Casein Kinase I and II inhibitor
A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM). -
SMO agonist
SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 uM).- Mark van den Hurk, .et al. , NPJ Parkinsons Dis, 2022, Oct 18;8(1):134 PMID: 36258029
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gamma-secretase inhibitor
Flurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID). - Prodigiosin (Prodigiosine) is a secondary metabolite of Symbiotic bacteria, with anti-fungal and anti-cancer activity.
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GSK-3 inhibitor
AR-A 014418 is a selective glycogen synthase kinase 3 (GSK-3) inhibitor (IC50 = 104 nM). Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 μM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices.- Chia-Hui Huang, .et al. , Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
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β-Catenin/Tcf Inhibitor
FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities. -
Gamma-secretase inhibitor
FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.- Tan YJ, .et al. , Future Med Chem, 2018, Sep 1;10(17):2039-2057 PMID: 30066578
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Smoothened inhibitor
PF-04449913 is a potent and orally bioavailable inhibitor of smoothened. -
sFRP-1 inhibitor
WAY-316606 is a small molecule inhibitors of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. -
CK2 inhibitor
TTP 22 is a high affinity, casein kinase 2 (CK2) inhibitor (IC50= 0.1uM, Ki= 40nM). In addition, TTP 22 shows selectivity for CK2 over JNK3, ROCK1, and MET (inhibitory effects displayed at greater than 10 uM). TTP 22 is highly conserved serine/threonine protein kinase that is also involved in cell proliferation, cell differentiation and apoptosis. -
GSK-3β inhibitor
1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25. -
beta-catenin inhibitor
BC2059 is an orally bioavailable and potent beta-catenin inhibitor.- Ji-Hye Jung, .et al. , Stem Cells Dev, 2016, Jul 1; 25(13): 1006-1019 PMID: 27188501
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gamma-secretase modulator
gamma-secretase modulator 3 is a gamma-secretase modulator. - Salinomycin is an antibacterial and coccidiostat ionophore therapeutic drug.
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Gamma-secretase modulator
Compound W is a γ-secretase inhibitor that has been shown to lower the levels of secreted Aβ42 and Nβ25. -
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. - Cardiogenol C hydrochloride is a potent and cell permeable inducer of embryonic stem cell differentiation in cardiomyocytes displaying an Ec50 of 100nm.
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Wnt agonist 1
Wnt agonist 1 is a cell-permeable Wnt signaling activator. It nduces beta-catenin and TCF-dependent transcriptional activity with EC50 value of 0.7 uM.- Zhao-Hui Chen, .et al. , Breast Cancer Res, 2023, 25: 22 PMID: 36829181
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CBP/beta-catenin antagonist
PRI-724 is the second-generation, potent and specific inhibitor of CBP/β-Catenin complex, and a modulator of the β-Catenin dependent canonical Wnt signaling pathway in cancer stem cells.
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Peptide 17 is a inhibitor of this YAP-TEAD protein-protein interaction which has potential usage in treatment of YAP-involved cancers with IC50 of 25nM.
- Alexander Howard, .et al. , Exp Dermatol, 2022, Oct;31(10):1477-1499 PMID: 35913427
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PKG inhibitor
Rp-8-Br-PET-cGMPS is metabolically stable, competitive inhibitor of cGKI (Ki = 30 nM) and cGKII (cGMP-dependent protein kinase G) and blocks cGMP-gated retinal type ion channels (IC50 = 25 μM). -
PKG/PKA inhibitor
cGMP Dependent Kinase Inhibitor Peptid is a specific cGKI (cyclic GMP-dependent protein kinase) inhibitor. Data indicates that it does not block cyclic GMP-dependent protein kinase phosphorylation of intact histones and has been used to study Plasmodium falciparum. -
Wnt pathway activator
WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate; with EC50 of 0.63 uM in TCF-Luciferase assay.