STAT3 Activator

Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury

Butyzamide is an orally active activator of Mpl, a thrombopoietin (TPO) receptor. Butyzamide increases the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. Butyzamide increases the level of platelets in mouse xenotransplantation assay.

Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.

Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis.

Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC₅₀ for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer.

YMU1 is a selective inhibitor of human thymidylate kinase (hTMPK) with an IC₅₀ of 610 nM. YMU1 inhibits tumor proliferation.

Zoniporide hydrochloride hydrate (CP-597396 hydrochloride hydrate) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide hydrochloride hydrate reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide hydrochloride hydrate is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

Secretoneurin, rat is a 33-amino acid neuropeptide produced by proteolytic processing of chromogranin II, widely distributed in the central and peripheral nervous systems, and its release is calcium-dependent. Secretoneurin, rat modulates the activities of caspase-3, caspase-1, the NLRP3 inflammasome, IGF-1R, VEGFR1, VEGFR2, FGFR3, AMPK, ERK1/2/MAPK, and Jak2/Stat3 pathways. Secretoneurin, rat regulates neuronal apoptosis, synaptic structure, inflammation, neurogenesis, angiogenesis, oxidative stress, cardiomyocyte hypertrophy, dopamine release, and cell migration and proliferation. Secretoneurin, rat is used in studies of global cerebral ischemia, myocardial infarction, stroke, and cardiac hypertrophy.

Fulipiftide (PSP 29-mer) is a short peptide derived from pigment epithelium-derived factor (PEDF). Fulipiftide induces the phosphorylation of ERK2 and STAT3, enriches tendon stem/progenitor cell markers, maintains cell stemness, promotes colony formation and niche expansion, and drives cell infiltration into injured tendons. Fulipiftide promotes the oriented formation of collagen fibers, regulates collagen deposition, and reduces inflammatory cell infiltration and neovascularization. Fulipiftide can be used in studies related to acute tendon injury.

Eflepedocokin alfa is a recombinant fusion protein. Eflepedocokin alfa consists of human IL-22 fused to human IgG2-Fc domain. Eflepedocokin alfa leads to the activation of IL-22/IL-22R-mediated signal transduction pathways as well as STAT3. Eflepedocokin alfa plays a role in immune response and bacterial infection, enhancing intestinal barrier function, intestinal immunity, and tissue repair.

Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC₅₀ of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer.

Polygalaxanthone III is a representative xanthone component of Polygala tenuifolia. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1, with an IC₅₀ of 50.56 μM. Polygalaxanthone III repairs skin damage induced by M. furfur via activating STAT3 phosphorylation and exerts anti-inflammatory effects. Polygalaxanthone III can be used for research on M. furfur-related skin damage.

Zoniporide (CP-597396) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

Mocravimod (KRP-203 free base) is a sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod significantly lowered the concentration of reactive oxygen species (ROS), prevented mitochondrial permeability transition pore opening, boosted mitochondrial membrane potential (MMP), and increased phosphorylation of AKT, EKR, GSK-3β, JAK2, and STAT3. Mocravimod retains T cell effector function. Mocravimod can be used for the study of acute myelogenous leukemia, diabetes and Myocardial Ischemia-Reperfusion Injury (MIRI).

OSM-SMI-8 is an oncostatin M (OSM) inhibitor with a pK_i of 44.82 nM against human targets. OSM-SMI-8 inhibits the activation of STAT3, JNK, ERK 42/44 and AKT signaling pathways induced by OSM. OSM-SMI-8 is applicable to research related to cancer metastasis and Crohn's disease.

(E/Z)-OSM-SMI-8 ((E/Z)-NSC642624) is the racemate of OSM-SMI-8 (HY-148693). OSM-SMI-8 is an oncostatin M (OSM) inhibitor with a pK_i of 44.82 nM against human targets. OSM-SMI-8 inhibits the activation of STAT3, JNK, ERK 42/44 and AKT signaling pathways induced by OSM. OSM-SMI-8 is applicable to research related to cancer metastasis and Crohn's disease.

JAK2 activator 1 is an orally active and selective JAK2 activator derived from Proanthocyanidin A1 (HY-N2344) (EC₅₀ = 64 nM). JAK2 activator 1 directly binds to JAK2, triggers conformational changes, and achieves allosteric activation of the JAK2/STAT3 signaling pathway. JAK2 activator 1 promotes hematopoietic recovery in chemotherapy-induced myelosuppression by protecting hematopoietic stem cells from Carboplatin (HY-17393)-induced damage. JAK2 activator 1 does not promote the proliferation of A549, HepG2, or CaCo2 tumor cells, nor does it attenuate the antitumor effect of Carboplatin. JAK2 activator 1 can be used in research related to cancer chemotherapy-induced myelosuppression.

Zoniporide mesylate (CP-597396 mesylate) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide mesylate reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide mesylate is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

Zoniporide hydrochloride (CP-597396 hydrochloride) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide hydrochloride reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide hydrochloride is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

Zoniporide dihydrochloride (CP-597396 dihydrochloride) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide dihydrochloride reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide dihydrochloride is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.