STAT Inhibitor

Nitidine (chloride) (Standard) is the analytical standard of Nitidine (chloride). This product is intended for research and analytical applications. Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.

Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34⁺ stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors.

Cycloguanil hydrochloride (Standard) is the analytical standard of Cycloguanil hydrochloride (HY-12784A). This product is intended for research and analytical applications. Cycloguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC₅₀ of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil hydrochloride inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.

Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.

Phellodendrine chloride (Standard) is the analytical standard of Phellodendrine chloride (HY-N0735). Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

(E/Z)-OSM-SMI-10B a derivative of OSM-SMI-10. (E/Z)-OSM-SMI-10B significantly reduces OSM-induced STAT3 phosphorylation in cancer cells upon co-incubation with OSM (Oncostatin M).

STAT3-IN-23 (PY*LKTK) is a potent STAT3 inhibitor.

Brevilin A (Standard) is the analytical standard of Brevilin A. This product is intended for research and analytical applications. Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC₅₀= 10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy.

SHP2 inhibitor LY6 (LY6) is a selective SHP2 inhibitor with an IC₅₀ of 9.8 μM, showing 7-fold selectivity over SHP1. SHP2 inhibitor LY6 inhibits SHP2-mediated cell signaling pathways and suppresses cell proliferation. SHP2 inhibitor LY6 elicits induces apoptosis and G2/M cell cycle arrest in lung cancer cells. SHP2 inhibitor LY6 can be used for the research of B cell acute lymphoblastic leukemia, acute myeloid leukemia, and lung cancer.

Scutellarin (Standard) is the analytical standard of Scutellarin. This product is intended for research and analytical applications. Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC₅₀s of 26 μM, 253 μM and 136 μM, respectively.

Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active.

Tyk2-IN-23 is a potent, orally active, selective TYK2 inhibitor (IC₅₀ = 18 nM), exhibiting more than > 70-fold selectivity over JAK1/2/3 isoforms. Tyk2-IN-23 potently inhibits p-STAT3 in TYK2-dependent signaling activated by IFN-α and IL-10. Tyk2-IN-23 potently inhibits IFN-α-induced STAT1 phosphorylation in H9 cells. Tyk2-IN-23 can be used for the study of alopecia areata and allergic Rhinitis.

PROTAC ALK degrader-4 is a ALK PROTAC degrader with a DC₅₀ of 445.25 nM. PROTAC ALK degrader-4 induces concentration- and time-dependent degradation of EML4-ALK, as well as concentration-dependent degradation of ALK^F1174L. PROTAC ALK degrader-4 downregulates 390 proteins in NCI-H3122 cells, including the targets of ceritinib (ALK, IGF-1R) and downstream molecules ERK1/2 and STAT3. PROTAC ALK degrader-4 exerts antiproliferative activity in ALK-positive cancer cells. ALK degrader-4 can be used in studies related to lung adenocarcinoma.

FAM-Danvatirsen is a FAM-labeled Danvatirsen (HY-145729). Danvatirsen is an antisense oligonucleotide targeting STAT3 that can be used in the study of cancer.

JAK1-IN-16 (compound 4l) is an inhibitor of JAK1/STAT3 and effectively downregulates TLR4 protein expression..

Thienodolin (MJ 286A) is an alkaloid that has been found in S. albogriseolus. Thienodolin inhibits nitric oxide production in LPS (HY-D1056)-stimulated RAW 264.7 murine macrophage cells with an IC₅₀ value of 17.2 μM. Thienodolin suppresses iNOS, blocks the degradation of IκBα, attenuates NF-κB p65 accumulation in the nucleus, and reduces the phosphorylation level of STAT1 at Tyr701. Thienodolin can be used for the study of inflammation.

AS2863619 GMP is AS2863619 (HY-126675) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AS2863619 is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 targets Stat5a-CDK8/19 to promote the differentiation of CD4⁺ T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 can be applied to research in related fields such as periodontitis-induced bone defects.

WZ-2-033 is a potent STAT3 inhibitor. WZ-2-033 inhibits MDA-MB-231, HCC70, and MDA-MB231-4175 cells proliferation, colony survival, migration, and invasion with IC₅₀s of 0.7, 1.3, and 1.3 μM, respectively.

NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity.

mTOR/STAT3-IN-1 is a dual mTOR/STAT3 inhibitor. mTOR/STAT3-IN-1 exhibits potent mTOR inhibitory activity and moderate STAT3 inhibitory activity, while exerting cell type-dependent antiproliferative and senolytic activities in human cell lines. mTOR/STAT3-IN-1 can be used in the research of glioblastoma and aging-related diseases.