Catalog No.S4743 Synonyms: Vogonin
Molecular Weight(MW): 284.26
Wogonin, a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibits N-acetyltransferase.
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Effect of Wogonin on the translocation and transcriptional activity of NFATc1. U2OS cells stably transfected with EGFP-NFATc1, RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. The IN Cell™ Analyzer 1000 was used to observe the translocation of NFATc1. (A) DMSO was used as a control. RANKL (100 ng/ml) significantly stimulated the translocation of NFATc1; Wogonin (5 mM) significantly decreased the translocation of NFATc1 induced by RANKL (magnification, x200). (B) Statistics showed that Wogonin could decrease the translocation of NFATc1 into the nucleus induced by RANKL in a concentration-dependent manner. RAW264.7 cells were transfected with pGL3-promoter-NFATc1-RE, and then RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. (C) RANKL significantly increased the transcriptional activity of NFATc1 and Wogonin decreased the transcriptional activity of NFATc1 induced by RANKL in a concentration-dependent manner. n=3; *P<0.05 and ***P<0.001 compared with the RANKL group. NAFTc1, nuclear factor of activated T cells c1; EGFP, enhanced green fluorescent protein; DMSO, dimethylsulfoxide, RANKL, receptor activator of nuclear factor κB ligand; RE, response element.
Exp Ther Med, 2015, 10(3):1066-1070. Wogonin purchased from Selleck.
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|Description||Wogonin, a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibits N-acetyltransferase.|
Wogonin inhibits PMA-induced COX-2 gene expression by inhibiting c-Jun expression and AP-1 activation in A549 cells. Wogonin is an inhibitor of cyclin-dependent kinase 9 (CDK9) and block phosphorylation of the carboxy-terminal domain of RNA polymerase II at Ser. Thus, it reduces RNA synthesis and subsequently rapid downregulation of the short-lived anti-apoptotic protein myeloid cell leukemia 1 (Mcl-1) resulting in apoptosis induction in cancer cells. Wogonin directly binds to CDK9, presumably to the ATP-binding pocketa and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity. Wogonin preferentially inhibits CDK9 in malignant compared with normal lymphocytes. Wogonin is a also potent anti-oxidant capable to scavenge •O2− . Wogonin significantly inhibits the translocation of NFATc1 from the cytoplasm to the nucleus and its transcriptional activation activity. It also significantly inhibits osteoclast differentiation and decreases the transcription of osteoclast‑associated immunoglobulin‑like receptor, tartrate‑resistant acid phosphatase and calcitonin receptor. Wogonin Inhibits N-acetyltransferase Activity.
|In vivo||Wogonin suppresses growth of human cancer xenografts in vivo. At doses lethal to tumor cells, wogonin shows no or little toxicity for normal cells and had also no obvious toxicity in animals. Wogonin could induce apoptosis in murine sarcoma S180 thereby inhibiting the tumor growth both in vitro and in vivo. An intraperitoneal injection of 200 mg/kg Wogonin could completely inhibit leukemia and CEM cells.|
|In vitro||DMSO||56 mg/mL (197.0 mM)|
|Ethanol||3 mg/mL (10.55 mM)|
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