Wnt Inhibitor

Halofenate, structurally akin to clofibrate, was evaluated in hypertriglyceridemic patients over 6-week periods in a controlled, double-blind crossover trial. It effectively reduced serum triglycerides by 50%, with minimal impact on serum cholesterol levels. Additionally, it lowered serum uric acid by 30% and exhibited uricosuric effects independent of glomerular filtration rate. Halofenate was associated with a significant increase in plasma thyroxine (T4), accompanied by a decrease in protein-bound iodine and T4 by column. In vitro studies confirmed its ability to displace T4 from thyroid-binding proteins, suggesting a thyroxine-displacing effect, which could influence thyroid function in vivo.

Triptonide (Standard) is the analytical standard of Triptonide. This product is intended for research and analytical applications. Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC₅₀ of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects.

PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC₅₀ of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer.

Lonchocarpin (Lonchocarpine) is a Wnt/β-catenin signaling pathway inhibitor. The IC₅₀ of Lonchocarpin in SW480 pBAR/Renilla cells is 4 μM. Acting downstream of β-catenin stabilization, Lonchocarpin inhibits β-catenin nuclear localization and TCF-mediated transcription, as well as the proliferation and migration of colorectal cancer cells. Lonchocarpin enhances Nrf2/ARE-mediated antioxidant responses in primary astrocytes via AMPK and JNK-related signaling, reduces H₂O₂-induced ROS production, and increases the expression of HO-1, NQO1 and MnSOD. Lonchocarpin can be used in research on colorectal cancer and oxidative stress.

Dalbinol is a rotenoid compound. Dalbinol can inhibit Wnt/β-catenin signaling pathway and promote β-catenin degradation. Dalbinol inhibits tumor cells proliferation and induces apoptosis. Dalbinol has antitumor activity.

8BTC (compound 4w) is a potent covalent Notum inhibitor with IC₅₀ of 2.5 nM.

Notum-IN-1 (compound 6b) is an orally active, selective and brain penetrant inhibitor of Notum. Notum-IN-1 blocks the Wnt signaling in vivo in mouse.

PM54 is an antitumor agent with activity across multiple cancer types. PM54 acts as a transcription and WNT/β-catenin signaling pathway inhibitor. PM54 suppresses oncogenic transcriptional programs, and key malignant pathways, while inducing DNA double-strand breaks, S-phase cell cycle arrest and apoptosis. PM54 enhances innate immune recognition, remodels the tumor microenvironment. PM54 exhibits antitumor activity as monotherapy or in combination in xenograft models. PM54 is applicable to research on various cancers and advanced solid tumors.

TNIK-IN-10 (Compound N15) is a TNIK inhibitor with an IC₅₀ of 0.49 nM against human TNIK. TNIK-IN-10 inhibits the enzymatic activity of TNIK, downregulates the expression of Wnt pathway target genes c-Myc and AXIN2, and reduces the protein expression of LRP5 and LRP6. TNIK-IN-10 induces apoptosis. TNIK-IN-10 exhibits anticancer activity against colorectal cancer. TNIK-IN-10 can be used in the research of colorectal cancer.

UAB116 is a Liver X Receptor (LXR)/Retinoid X Receptor (RXR) agonist. UAB116 can decreases metastatic phenotype in hepatoblastoma by inhibiting the Wnt/β-Catenin pathway via upregulation of TRIM29. UAB116 can reduce proliferation, stemness and invasiveness of metastatic hepatoblastoma cells.

Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity.

Nigericin (sodium salt) (Standard) is the analytical standard of Nigericin (sodium salt). This product is intended for research and analytical applications. Nigericin sodium salt is an antibiotic derived from Streptomyces hygroscopicus that act as a K⁺/H⁺ ionophore, promoting K⁺/H⁺ exchange across mitochondrial membranes. Nigericin sodium salt is a NLRP3 activator. Nigericin sodium salt shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin sodium salt induces pyroptosis through caspase 1/GSDMD in TNBC.

WZU-13 is an inhibitor for Carboxylesterase (CES). WZU-13 inhibits 77% CES activity at a dose of 100 μM.

p53 DUBTAC modulator-1 (Compound A1) is a p53 Y220C DUBTAC modulator (K_d = 12.09 µM). p53 DUBTAC modulator-1 effectively reactivates and deubiquitinates mutant p53 Y220C. p53 DUBTAC modulator-1 upregulates p53 Y220C protein levels. p53 DUBTAC modulator-1 induces Apoptosis, reduces Bcl-2, inhibits Wnt signaling. p53 DUBTAC modulator-1 has anti-cancer activity against liver cancer.

IWR-1 (IWR-1-endo) (GMP) is the IWR-1 (HY-12238) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. IWR-1 (IWR-1-endo) is a tankyrase inhibitor targeting Wnt/β-catenin (IC₅₀ = 180 nM). IWR-1 compromises critical steps of the canonical Wnt signaling, namely translocation of β-catenin to the nucleus and subsequent TCF/LEF activation and expression of Wnt/β-catenin downstream targets. IWR-1 promotes β-catenin phosphorylation by promoting stability of Axin-scaffolded destruction complexes. IWR-1 can be studied in research for anti-tumor purposes, and diseases such as osteosarcoma, colorectal cancer and psoriasis.

Y-99 is a PORCN inhibitor with an IC₅₀ of 155.4 nM against the Wnt/β-catenin signaling pathway. Y-99 inhibits the expression of p-LRP6, β-catenin, and c-Myc.

AZ1366 is an orally active tankyrase inhibitor. AZ1366 stabilizes Axin2, reduces NuMA levels, disrupts the interaction between tankyrase and NuMA, induces G2/M phase arrest, inhibits the Wnt pathway, and downregulates the expression of β-catenin-dependent genes. AZ1366 inhibits tumor growth in colorectal cancer xenograft models. AZ1366 synergistically inhibits the proliferation of non-small cell lung cancer cells, improves tumor control and significantly prolongs survival in orthotopic non-small cell lung cancer mouse models. AZ1366 is applicable to research related to colorectal cancer and non-small cell lung cancer.

Porcn-IN-2 (Example 107) is a Wnt inhibitor, with an IC₅₀ value of 0.05 nM. Porcn-IN-2 can be used for research of cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia, etc.

NLS-StAx-h is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC₅₀ of 1.4 μM. NLS-StAx-h efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h shows anti-proliferation of cancer cells.

Antiproliferative agent-76 (Compound II-2) is an 8-sulfonamidoquinoline derivative and a selective anticancer agent. Antiproliferative agent-76 blocks the NF-κB and WNT signaling pathways. Antiproliferative agent-76 promotes cancer cell Apoptosis. Antiproliferative agent-76 exhibits anticancer activity against colorectal cancer and leukemia.