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MedChemExpressModel Iminostilbene -256-96-2

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Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases[1][2].
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Iminostilbene

MCE China:Iminostilbene

Brand:MedChemExpress (MCE)

Cat. No.HY-N7064

CAS:256-96-2

Purity:99.34%

Storage:4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.

In Vitro:Iminostilbene (2.5-10 μM, 30 h) inhibits LPS-induced inflammatory response, reduces PKM2 expression, and suppresses its downstream signaling pathways in RAW264.7 macrophages[2].

In Vivo:Iminostilbene (0.625 mg/kg, 1.25 mg/kg, p.o., once daily for 5 days) improved cardiac function and suppressed inflammation in the myocardial ischemia/reperfusion (MI/R) injury SD rat model[2].

IC50 & Target:COX-2 iNOS STAT3 HIF-1α

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References:

[1]. Christian P, et al. Crystallization of Carbamazepine in Proximity to Its Precursor Iminostilbene and a Silica Surface. Cryst Growth Des. 2016 May 4;16(5):2771-2778. Epub 2016 Mar 30.  [Content Brief]

[2]. Lu S, et al. Iminostilbene, a novel small-molecule modulator of PKM2, suppresses macrophage inflammation in myocardial ischemia-reperfusion injury. J Adv Res. 2020 Sep 9;29:83-94.  [Content Brief]

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