化合物AS101 T6761
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Product IntroductionBioactivity英文名: Ossirene描述: Ossirene (AS101) 是一种免疫调节抑制剂，是一种新型 IL-1beta 转化酶抑制剂，可用于自身免疫性疾病和某些恶性肿瘤。它通过抑制
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Product Introduction
Bioactivity
英文名: Ossirene
描述: Ossirene (AS101) 是一种免疫调节抑制剂，是一种新型 IL-1beta 转化酶抑制剂，可用于自身免疫性疾病和某些恶性肿瘤。它通过抑制IL-10消除 STAT3 的磷酸化，有效抑制Caspase-1。
细胞实验: In vitro, PBMCs were first treated with various concentrations of AS101, and after 1 h SAC (10-3 v/v) was added. After 24 h, supernatants were collected and evaluated for cytokine content. (Only for Reference)
体外活性: Treatment of caspase-1 (interleukin-1 [IL-1] converting enzyme [ICE]) with AS101 inhibits its enzymatic activity in a dose-dependent manner. Moreover, AS101 treatment causes a significant reduction in the active form of IL-18 and IL-1 in peripheral blood mononuclear cells (PBMC) and in human HaCat keratinocytes. The inhibitory effect of AS101 does not involve nitric oxide (NO) or interferon- (IFN- ), two possible regulators of IL-18 production, and does not occur at the mRNA level. It may exert effects through a posttranscriptional mechanism[1]. AS101 induced SIRT1 expression in a dose dependent manner in three different cell lines, HEK293, HL-60 and Rin-5f. Incubation of HEK293 and HL-60 cell lines with AS101 (0.1-2.5μg/ml) resulted in a dose dependent reduction in PPARγ protein expression relative to the control cells, and the reduction of PPARγ expression is in parallel to increased SIRT1 expression[2].
体内活性: AS101 downregulates IL-18 and IL-1 serum levels in a mouse model of lipopolysaccharide (LPS)-induced sepsis, resulting in increased survival. It has also been shown to be protective against lethal and sublethal effects of irradiation and chemotherapy. In a model of cecal ligation and puncture (CLP)-induced sepsis in mice, AS101 also exerted beneficial effects[1]. AS101 treated rats showed a large increase in SIRT1 protein levels in the liver and kidney extracts of rats treated with AS101. AS101 prevents development of insulin resistance in vivo. AS101 affects SIRT1 related metabolic pathways by changing the insulin levels. AS101 treatment prevents hyperglycemia associated with T2D(type 2 diabetes) and some of the symptoms of the disease in the HFD(high fat diet)+STZ(Streptozotocin) rat model[2].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 5.63 mg/mL (18.03 mM)
关键字: RPE | NFκB | Caspase | Inhibitor | inhibit | diseases | immunomodulatory | AS-101 | autoimmune | malignancies | Ossirene | tellurium | AS 101 | IL-6 | IL-8 | p65 | Interleukin Related | STAT3 | phosphorylation
相关产品: Y-320 | GIBH-130 | Aucubin | Deacetylasperulosidic Acid | Isotetrandrine | XYLOBIOSE | Shizukaol B | Skullcapflavone I | Menthone | SP4206
相关库: Drug Repurposing Compound Library | Cytokine Inhibitor Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Apoptosis Compound Library | Orally Active Compound Library | Protease Inhibitor Library | Bioactive Compound Library
Bioactivity
英文名: Ossirene
描述: Ossirene (AS101) 是一种免疫调节抑制剂，是一种新型 IL-1beta 转化酶抑制剂，可用于自身免疫性疾病和某些恶性肿瘤。它通过抑制IL-10消除 STAT3 的磷酸化，有效抑制Caspase-1。
细胞实验: In vitro, PBMCs were first treated with various concentrations of AS101, and after 1 h SAC (10-3 v/v) was added. After 24 h, supernatants were collected and evaluated for cytokine content. (Only for Reference)
体外活性: Treatment of caspase-1 (interleukin-1 [IL-1] converting enzyme [ICE]) with AS101 inhibits its enzymatic activity in a dose-dependent manner. Moreover, AS101 treatment causes a significant reduction in the active form of IL-18 and IL-1 in peripheral blood mononuclear cells (PBMC) and in human HaCat keratinocytes. The inhibitory effect of AS101 does not involve nitric oxide (NO) or interferon- (IFN- ), two possible regulators of IL-18 production, and does not occur at the mRNA level. It may exert effects through a posttranscriptional mechanism[1]. AS101 induced SIRT1 expression in a dose dependent manner in three different cell lines, HEK293, HL-60 and Rin-5f. Incubation of HEK293 and HL-60 cell lines with AS101 (0.1-2.5μg/ml) resulted in a dose dependent reduction in PPARγ protein expression relative to the control cells, and the reduction of PPARγ expression is in parallel to increased SIRT1 expression[2].
体内活性: AS101 downregulates IL-18 and IL-1 serum levels in a mouse model of lipopolysaccharide (LPS)-induced sepsis, resulting in increased survival. It has also been shown to be protective against lethal and sublethal effects of irradiation and chemotherapy. In a model of cecal ligation and puncture (CLP)-induced sepsis in mice, AS101 also exerted beneficial effects[1]. AS101 treated rats showed a large increase in SIRT1 protein levels in the liver and kidney extracts of rats treated with AS101. AS101 prevents development of insulin resistance in vivo. AS101 affects SIRT1 related metabolic pathways by changing the insulin levels. AS101 treatment prevents hyperglycemia associated with T2D(type 2 diabetes) and some of the symptoms of the disease in the HFD(high fat diet)+STZ(Streptozotocin) rat model[2].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 5.63 mg/mL (18.03 mM)
关键字: RPE | NFκB | Caspase | Inhibitor | inhibit | diseases | immunomodulatory | AS-101 | autoimmune | malignancies | Ossirene | tellurium | AS 101 | IL-6 | IL-8 | p65 | Interleukin Related | STAT3 | phosphorylation
相关产品: Y-320 | GIBH-130 | Aucubin | Deacetylasperulosidic Acid | Isotetrandrine | XYLOBIOSE | Shizukaol B | Skullcapflavone I | Menthone | SP4206
相关库: Drug Repurposing Compound Library | Cytokine Inhibitor Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Apoptosis Compound Library | Orally Active Compound Library | Protease Inhibitor Library | Bioactive Compound Library
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