STAT Modulator

Fezakinumab (ILV 094) is an anti-IL-22 monoclonal antibody. Fezakinumab inhibits IL-22 signal transduction, and regulates the JAK1/STAT3 pathway as well as apoptotic proteins. Fezakinumab alleviates airway remodeling, alveolar enlargement and inflammatory cell infiltration in lung tissues. Fezakinumab reduces the levels of neutrophils, lymphocytes, eosinophils and macrophages in lung tissues. Fezakinumab can be used in the research of chronic obstructive pulmonary disease and skin diseases.

Medrysone (HMS; 6α-Methyl-11β-hydroxyprogesterone) is a STAT6 modulator and M2 macrophage polarization inducer. Medrysone enhances IL-4-triggered STAT6 activation, upregulates the expression of M2 markers, and promotes the secretion of VEGF and CCL2. Medrysone also enhances the pro-migratory activity of M2-like macrophages toward endothelial cells. By regulating macrophage polarization and related repair pathways, Medrysone significantly promotes corneal wound repair in a rat mechanical injury model. Medrysone can be used for research related to corneal injury.

AX-202 is a humanized IgG4 monoclonal antibody targeting S100A4. AX-202 neutralizes the activity of S100A4. AX-202 effectively reverses established fibrosis and reduces inflammation and fibrosis-related biomarkers in a mouse model of skin fibrosis. AX-202 is applicable for the research of fibrotic and inflammatory diseases.

PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a K_d value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research.

Bellidifolin is an orally active compound with antiproliferative, anti-inflammatory and antioxidant properties. Bellidifolin modulates key signaling pathways including STAT3, PI3K-Akt, mTOR and BRD4, and inhibits the viral protein R (Vpr). Bellidifolin induces cell cycle arrest and apoptosis, exerts significant antifibrotic effects, and protects the heart, liver and nervous system. Bellidifolin is applicable to the research of various diseases such as lung cancer, non-alcoholic fatty liver disease, myocardial hypertrophy and ischemic cranial nerve injury.

JAK2-IN-10 is a selective JAK2 V617F inhibitor with an IC₅₀ value of ≤10 nM. JAK2-IN-10 can be used for the research of myeloproliferative neoplasms and other related diseases.

XMU-MP-2 is a selective BRK/PTK6 inhibitor with an IC₅₀ of 5.4 nM. XMU-MP-2 inhibits the proliferation of BRK-positive breast cancer cells and induces apoptosis. XMU-MP-2 is applicable to breast cancer-related research.

Physalin D is isolated from the aerial parts of Physalis angulate. Physalin D displays considerable cytotoxicity against several cancer cell lines, showing IC₅₀ values in the range of d 0.28 to 2.43 microg/mL. Physalin D has the potential for the cancer disease.

TS-IN-5 (Compound 15) is a thymidylate synthase (TS) inhibitor. TS-IN-5 induces Apoptosis by modulating Bax, BCL-2, PI3K, and STAT1 proteins. TS-IN-5 shows antitumor effects against liver, breast and colon cancers.

STAT6 modulator-3 (compound 37) is a STAT6 modulator with an IC₅₀ value less than 300 nM. STAT6 modulator-3 can be used in the research of cancer and inflammatory.

MEAP (2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine) is a NEDD9-STAT3 modulator. MEAP disrupts NEDD9-STAT3 interaction, driving STAT3 Y705 dephosphorylation. MEAP induces G₂/M phase arrest. MEAP can be used for the research of anaplastic thyroid cancer.

Pabgraminone C (IM502) is a Fungal metabolite and PI3Kγ inhibitor with an IC₅₀ of 61.7 nM against PI3Kγ. Pabgraminone C shifts the STAT signaling pathway in cells from an immunosuppressive STAT3/STAT6-dominant profile to an immunostimulatory STAT1/STAT2-dominant profile, driving cells toward a pro-inflammatory phenotype. Pabgraminone C reprograms cells from an immunosuppressive state to an immunostimulatory state, reversing their suppressive effect on anti-tumor immunity. Pabgraminone C inhibits established tumor growth and metastasis across multiple cancer types. Pabgraminone C overcomes resistance to PD-1 checkpoint blockade strategies. Pabgraminone C can be used in research related to liver cancer, melanoma, and colorectal cancer.

DM243 is an EPAC1 activator and STAT3 modulator with an pIC₅₀ of 4.769 for EPAC1. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts.

(trans)-STAT6-IN-13 (Compound 95) is a STAT6 inhibitor with IC₅₀ values of ≤300 nM. (trans)-STAT6-IN-13 has weak inhibitory for STAT3. (trans)-STAT6-IN-13 can be used for the researches of cancer, inflammation and immunology.

Anticancer agent 259 (Compound 3g) is a Telmisartan (HY-13955)-based cell death modulator, that interfers with the STAT5 signaling pathway, enhances the sensitivity of drug-resistant cells to Imatinib (HY-15463) with SC₅₀ of 1.5 μM.

Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .

PTPN2/1-IN-4 (Compound WS35) is an orally active, dual-functional inhibitor of PTPN1 and PTPN2 with IC₅₀s of 12.8 and 5.8 nM for PTPN1 and PTPN2, respectively. PTPN2/1-IN-4 modulates the IFNγ-JAK-STAT signaling pathway and significantly augments CD8+ T-cell tumor infiltration. PTPN2/1-IN-4 has potent anticancer activity, robustly inhibiting tumor growth both as a monotherapy and in combination with an anti-PD-1 antibody in B16-OVA syngeneic mouse models.

anti-TNBC agent-7 (Compound 13c) possesses anticancer activity, serving as a molecular probe to recognize and regulate the signal transduction of the USP21/JAK2/STAT3 axis, exhibiting nanomolar-level cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC).

Medrysone (Standard) is the analytical standard of Medrysone. This product is intended for research and analytical applications. Medrysone (HMS; 6α-Methyl-11β-hydroxyprogesterone) is a STAT6 modulator and M2 macrophage polarization inducer. Medrysone enhances IL-4-triggered STAT6 activation, upregulates the expression of M2 markers, and promotes the secretion of VEGF and CCL2. Medrysone also enhances the pro-migratory activity of M2-like macrophages toward endothelial cells. By regulating macrophage polarization and related repair pathways, Medrysone significantly promotes corneal wound repair in a rat mechanical injury model. Medrysone can be used for research related to corneal injury.