p-stat3

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

ZX-29 is a potent and selective inhibitor of ALK with IC50 values of 2.1 nM, 1.3 nM, and 3.9 nM for ALK, ALK [L1196M], and ALK [G1202R] mutations, respectively. It also induces protective autophagy and exhibits antitumor effects.

1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea is a a derivative of the multiple tyrosine kinase inhibitor sorafenib. 1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea potently inhibits the phosphorylation of STAT3 by blocking STAT3 phosphorylation and activation, and induces apoptosis in hepatocellular carcinoma cell lines[1].

SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects.

WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).

JAK1/STAT3-IN-1 (compound 4f) functions as an anti-atopic dermatitis (AD) agent by inhibiting the JAK1/STAT3 signaling pathway. It has an IC50 value of 2.17 μM for inhibiting NO production. Additionally, JAK1/STAT3-IN-1 improves skin conditions in AD-like mice by reducing inflammatory infiltration, suppressing the expression of p-JAK1/JAK1 and p-STAT3/STAT3, and alleviating the hyperimmune response induced by MC903 (Calcipotriol).

Brefeldin A 4-O-nicotinate (CHNQD-01228) is a dual inhibitor of Arf1 and BMX proteins with an IC50 value of 0.22 μM for T24 cell proliferation. It also suppresses T24 cell migration and colony formation in a dose-dependent manner, induces G1 phase arrest, and triggers apoptosis. By targeting BMX proteins, it inhibits the AKT/p-AKT and STAT3/p-STAT3 signaling pathways, while also inhibiting Arf1 proteins to eliminate bladder cancer stem cells and activate antitumor immunity, thus exhibiting anticancer activity. Brefeldin A 4-O-nicotinate is applicable in research related to bladder cancer.

JAK2-IN-13 is a potent and orally active JAK2 inhibitor with an IC50 of 54.7 nM. It downregulates the expression of p-STAT3 and p-STAT5 and exhibits good bioavailability. JAK2-IN-13 effectively suppresses recombinant human erythropoietin-induced extramedullary erythropoiesis as well as polycythemia vera. It is used in the study of myeloproliferative neoplasms.

STAT3-IN-51 is a STAT3 inhibitor that binds directly to the SH2 domain of STAT3. This compound induces apoptosis, ferroptosis, and immunogenic cell death (ICD), enhancing antitumor immunity. It suppresses STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling, while prompting reactive oxygen species (ROS) generation, decreasing Bcl-2 expression, disrupting mitochondrial functions, inhibiting GPX4 activity, and promoting lipid peroxidation. STAT3-IN-51 is applicable in research on colorectal cancer, breast adenocarcinoma, non-small cell lung cancer (NSCLC), and cisplatin-resistant lung adenocarcinoma.

P-gp-IN-36 is a potent P-glycoprotein (P-gp) inhibitor with an EC50 of approximately 1 μM. It effectively inhibits the efflux function of P-gp, reversing P-gp-mediated multidrug resistance in cancer cells. Additionally, P-gp-IN-36 suppresses STAT3 phosphorylation and reduces overall STAT3 expression levels, sensitizing P-gp-expressing cancer cells to conventional cytotoxic drugs. This compound is useful in the study of multidrug-resistant cancers.

Solamargine (δ-Solanigrine) is a major steroidal alkaloid glycoside extracted from a traditional Chinese medicine herb, Solanum nigrum L. (SNL); has been shown to inhibit growth and induce apoptosis of various cancer cells.

Nifuroxazide-D4 is intended for use as an internal standard for the quantification of nifuroxazide by GC- or LC-MS. Nifuroxazide (T1563) is a nitrofuran antibiotic. It is active against strains of the enteropathogenic bacteria C. jejuni, Salmonella, Y. enterocolitica, Shigella, and E. coli. It inhibits quorum sensing and virulence factor production in P. aeruginosa. Nifuroxazide (T1563) inhibits STAT3 activity in a reporter assay and decreases viability of U266 and INA-6 myeloma cells, which have constitutive STAT3 phosphorylation, with EC50 values of approximately 4.5 µM for both. It also decreases viability, migration, and invasion of, and induces apoptosis in, MCF-7, 4T1, and MDA-MB-231 breast cancer cells. Nifuroxazide (T1563) reduces tumor growth and prevents pulmonary metastasis in a 4T1 murine mammary carcinoma model. It also reduces diarrhea, weight loss, and colon inflammation in a rat model of acetic acid-induced ulcerative colitis.

MMT3-72 is a weak JAK1 inhibitor with superior efficacy and reduced p-STAT3 in DSS-induced colitis [1].

SBT-100 is a human monoclonal antibody (mAb) that targets STAT3. It inhibits IL-6-mediated nuclear translocation of P-STAT3 in HEp-2 and PANC-1 cells and demonstrates tumor growth inhibition in MDA-MB-231.

Garcinone D (Standard) is a reference standard for research and analysis in studies involving Garcinone D. Garcinone D shows significant cytotoxicity against the CEM-SS cell line, with IC(50) value of 3.2 microg/ml; it exhibits dose-dependent enzyme-based microsomal aromatase inhibitory activity. Garcinone D inhibits p65 activation with IC50 values of 3.2 microM.

Theleganbanin B is a p-terphenyl derivative discovered in the mushroom (Thelephora ganbajun). It inhibits the production of TNF-α, IL-6, and IL-1β in BV-2 microglial cells induced by LPS. Theleganbanin B also suppresses the phosphorylation of JAK2/STAT3 and holds potential for neurodegenerative disease research.

2-Hydroxy-3-methylanthraquinone is a natural anthraquinone derivative that exhibits cytotoxic and pro-apoptotic activity against various tumor cells. It modulates SRC-related signaling and the activity of the IL-6/JAK2/STAT3 pathway, and induces a decrease in mitochondrial membrane potential and Caspase-3-dependent apoptosis. It can also influence MAPK-related signaling pathways, including the phosphorylation levels of p38MAPK and ERK1/2. 2-Hydroxy-3-methylanthraquinone is also commonly used in research related to anthraquinone chemistry, redox properties, and the pharmacological activity of natural products.

Cinnamtannin D1 is an orally active polyphenolic compound that modulates the Th17/Treg cell balance by inhibiting AHR expression. It reduces apoptosis and ROS in INS-1 cells and primary cultured mouse islets induced by Palmitic acid (PA). Cinnamtannin D1 mitigates Th17 cell differentiation by downregulating p-STAT3/RORγt and enhances Treg cell differentiation by upregulating p-STAT5/Foxp3. In a collagen-induced arthritis (CIA) mouse model, it demonstrates excellent anti-arthritic efficacy. Cinnamtannin D1 is applicable for rheumatoid arthritis (RA) research.

Garcinone D shows significant cytotoxicity against the CEM-SS cell line, with IC(50) value of 3.2 microg/ml; it exhibits dose-dependent enzyme-based microsomal aromatase inhibitory activity. Garcinone D inhibits p65 activation with IC50 values of 3.2 micr

(R)-Reticuline is a natural alkaloid that can be catalyzed by the microsomal P-450 system in plants and animals for conversion to Salutaridine, which is involved in endogenous morphine synthesis. The isomer of (R)-Reticuline is Reticuline. Reticuline inhibits the JAK2/STAT3 and NF-κB signaling pathways, and also inhibits the mRNA expression of TNF-α and IL-6, with anti-inflammatory effects.