Stem Cell

FLI-06 is a Notch signaling inhibitor (EC 50 = 2.3µM) that acts upstream of α-secretase and β-secretase cleavage. FLI-06 disrupts intracellular trafficking and processing of the Notch signaling pathway, inhibiting general secretion at a stage prior to exiting the endoplasmic reticulum (ER) and transforming the ER morphology from tubules to lamellae. FLI-06 for the treatment of cancer and neurodegenerative diseases.

GSK-3 inhibitor

GANT61 was able to efficiently block GLI1 as well as GLI2-induced transcription, IC50 is 5 µM.

competitive inhibitor of GSK-3β (Ser9) phosphorylation

Selective peptide inhibitor of glycogen synthase kinase-3 (GSK-3)

IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC 50 value of 180 nM.

HPI 1 is a potent GLI antagonist with an IC50 value of 1.1 μM. HPI 1 shows anti-proliferative activity. HPI 1 decreases the GLI1 mRNA expression. HPI 1 inhibits colony formation in a dose-dependent manner.

Hedgehog signaling Inhibitor

SANT-2 is a potent antagonist of Hh-signaling pathway. Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. SANT-2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers.

Hh pathway antagonist

Scrambled control peptide for use with TCS 183

Tankyrase inhibitor

TCS 2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM.

CHIR-98014 is a potent, cell-permeable inhibitor of GSK-3α and GSK-3β with IC 50 values of 0.65nM and 0.58nM, respectively.

AY 9944 dihydrochloride is a specific cholesterol biosynthesis inhibitor.

Indirubin-3'-oxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 μM, respectively; Indirubin-3'-oxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.

XAV-939 selectively inhibits β-catenin-mediated transcription.

Smo antagonist,potent and selective

Cyclopamine is a naturally occurring Hedgehog (Hh)-specific small-molecule signaling steroidal alkaloid inhibitor, causes a profound inhibition of tumor growth, has significant anti-invasive, anti-proliferative and anti-estrogenic potency in human breast cancer cells .

GSK-3β inhibitor

Wnt-C59 is a highly potent inhibitor of Porcupine (Porcn), a member of the Mboat (membrane-bound O-acyl deglycosylase) family, with an IC 50 value of 74pM, and can inhibit Wnt signaling.

GSK-3α/β inhibitor

GSK-3β inhibitor

Tideglusib is a potent, selective, and irreversible non-ATP competitive glycogen synthase kinase-3 (GSK-3) inhibitor. The IC 50 values for GSK-3βWT and GSK-3βC199A are 5nM and 60nM, respectively.