Wnt Inhibitor

Salinomycin (Standard) is the analytical standard of Salinomycin. This product is intended for research and analytical applications. Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin shows selective activity against human cancer stem cells[1][2][3].

iCRT3 (Standard) is the analytical standard of iCRT3 (HY-103705). This product is intended for research and analytical applications. iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.

JW67 (Standard) is the analytical standard of JW67 (HY-108442). This product is intended for research and analytical applications. JW67 inhibits the canonical Wnt signaling with an IC₅₀ of 1.17μM. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth.

Pyrvinium pamoate (Standard) is the analytical standard of Pyrvinium pamoate. This product is intended for research and analytical applications. Pyrvinium pamoate is an FDA-approved antihelmintic agent that inhibits WNT pathway signaling.

IWP-2 (Standard) is the analytical standard of IWP-2 (HY-13912). This product is intended for research and analytical applications. IWP-2 is an inhibitor of Wnt processing and secretion with an IC₅₀ of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC₅₀ of 40 nM for the gatekeeper mutant ^M82FCK1δ.

CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC₅₀ of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1^SER727 with an IC₅₀ of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC₅₀ of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.

β-catenin modulator IIa-661 is a β-catenin modulator that modulates β-catenin activity and inhibits the activity of the Wnt/wingless (wg) signaling pathway. β-catenin modulator IIa-661 can be utilized in cancer research.

PNU-74654 (Standard) is the analytical standard of PNU-74654 (HY-101130). This product is intended for research and analytical applications. PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.

2-Hydroxyanthraquinone (Standard) is the analytical standard of 2-Hydroxyanthraquinone (HY-W012352). This product is intended for research and analytical applications. 2-Hydroxyanthraquinone is a product generated by the photochemical oxidation of Anthracene (ANT) (HY-Y0299). 2-Hydroxyanthraquinone induces ferroptosis in cardiomyocytes by depleting GSH and inhibiting GPX4, leading to cardiac developmental malformations. 2-Hydroxyanthraquinone causes damage to the cerebrovascular system and blood-brain barrier in zebrafish by downregulating the Wnt/β-catenin signaling pathway, as well as inducing inflammation and neuronal apoptosis. 2-Hydroxyanthraquinone can be used in studies related to cerebrovascular diseases and cardiotoxicity.

Cardionogen-2 is a biphasic modulator of cardiogenesis, either promoting or inhibiting heart formation depending on the stage of treatment. Cardionogen-2 inhibits Wnt/β-catenin-dependent transcription in murine embryonic stem (ES) cells and zebrafish embryos.

KYA1797K (Standard) is the analytical standard of KYA1797K (HY-101090). This product is intended for research and analytical applications. KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.

Adavivint (Standard) is the analytical standard of Adavivint (HY-109049). This product is intended for research and analytical applications. Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC₅₀ of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.

EXQ-2d is the inhibitor for tankyrase and inhibits TNKS1 and TNKS2 with an IC₅₀ of 48.8 nM and 13.8 nM (pIC₅₀=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC₅₀ of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI₅₀ of 4.9 μM and 77 μM.

CCT070535 blocks TCF-dependent transcription at the TCF level, with GI₅₀ values of 17.6 μM, 11.1 μM, 11.8 μM and 13.4 μM in HT29 (APC mutant), HCT116 (oncogenic β-catenin), SW480 (APC mutant) and SNU475 (Axin mutant) cells, respectively.

Pamidronic acid (Standard) is the analytical standard of Pamidronic acid. This product is intended for research and analytical applications. Pamidronic acid, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronic acid can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.

Murrayafoline A (Standard) is the analytical standard of Murrayafoline A (HY-W100287). This product is intended for research and analytical applications. Murrayafoline A is a carbazole alkaloid that can be extracted from Murraya tetramera. Murrayafoline A directly targets Specificity protein 1 (Sp1), thereby inhibiting NF-κB and MAPK signaling pathways. Murrayafoline a induces a G0/G1-phase arrest in platelet-derived growth factor (PDGF)-stimulated vascular smooth muscle cells. Murrayafoline A attenuates the Wnt/β-catenin pathway by promoting the degradation of intracellular β-catenin proteins. Murrayafoline A enhances the contraction of rat ventricular myocytes and L-type calcium current by activating protein kinase C. Murrayafoline A inhibits LPS (HY-D1056)-induced neuroinflammation in vivo. Murrayafoline A can be used for the study of inflammation, vascular complications and colon cancer.

Sapanisertib (INK-128; MLN0128; TAK-228) phosphate is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib phosphate directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib phosphate is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.