Stem Cell

Wnt signaling inhibitor; inhibits β-catenin-transcription factor interactions

Frizzled 4 allosteric agonist; exhibits biased siginaling; preserves stemness

A synthetic peptide

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM.

KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively.

MSAB (methyl 3-{[(4-methylphenyl)sulfonyl]amino}benzoate) is a selective Wnt/β-catenin signaling inhibitor binding to β-catenin and promoting its degradation with an EC 50 of 0.583μM.

PRI-724 (C-82 prodrug, ICG-001 analog) is a first-in-class Wnt signaling modulator that inhibits the interaction between cAMP response element (CREB) binding protein and β-catenin.

RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.

I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM).

LATS-IN-1 is an inhibitor of LATS1 and LATS2 (IC 50 = 2nM for both). Lats-IN-1 inhibits core Hippo pathway kinases and activates downstream effector molecules YAP/TAZ, which translocate to the nucleus, driving expression of genes that promote cell proliferation and survival. Lats-IN-1 is primarily used to treat tissue regeneration and degenerative diseases.

Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model.

Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer.

K-975 is a potent and orally active inhibitor of YAP1/TAZ-TEAD protein-protein interaction.

FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities.

SAG-d3 is deuterium labeled SAG. SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM).

Teplinovivint is a potent wnt/β-catenin signaling pathway inhibitor.

PY-60 is a thiazole-substituted derivative with 5-phenylisoxazole as its core structure, which can potently and specifically activate the transcriptional activity of YAP (EC 50 = 1.6μM).

β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer.

VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer.

MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction.

N-Desmethylnefopam D5 hydrochloride is a deuterium labeled N-Desmethylnefopam hydrochloride.

VT103 is a selective TEAD1 protein palmitoylation inhibitor.