Dipyrithione

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

双吡啶硫酮似乎具有新颖的细胞毒性和有效的广谱抗肿瘤活性。

Dipyrithione appears to have novel cytotoxicity and potent broad-spectrum antitumor activity.(In Vitro):Dipyrithione (20?μg/mL) shows antifungal activity with MIC values of 6.03 μM for Trichophyton rubrum.Dipyrithione (72 h) shows cytotoxic activity against 293?T cells with an IC50 value of 0.22 μM.Dipyrithione (1-5 μM; 8.5 h) inhibits LPS (100 ng/ml)-induced up-regulation of iNOS and COX-2 in RAW264.7 cells in a dose-dependent manner.Dipyrithione (1 μM; 8.5 h) suppresses LPS-induced increase of iNOS but not COX-2 mRNA level, inhibits LPS-increased NO production.Dipyrithione (3 μM; 2, 5 h) decreases phosphorylation of STAT1 induced by LPS and does not influence LPS-induced MAPK and NF-κB activation in RAW 246.7 cells.Dipyrithione (0-5 μg/mL; 48 h) shows antiproliferative activity for KB, 231, U937 and K562 cells in a dose dependent manner.Dipyrithione (2.5 μg/ml) induces apoptosis and cycle arrest at G1 phase.(In Vivo):Dipyrithione (0.2 mg/cm2; externally once daily for 10 days) shows great anti-dermatophyte activity effects in guinea pig.Dipyrithione (1, 2.5, 5 mg/kg; i.p.) shows anti-inflammatory activity in mouse. Dipyrithione (5 mg/kg; i.p.; daily for 10 days) shows anti-tumor acyivity in mouse.

Dipyrithione (20?μg/mL) shows antifungal activity with MIC values of 6.03 μM for Trichophyton rubrum.Dipyrithione (72 h) shows cytotoxic activity against 293?T cells with an IC50 value of 0.22 μM.Dipyrithione (1-5 μM; 8.5 h) inhibits LPS (100 ng/ml)-induced up-regulation of iNOS and COX-2 in RAW264.7 cells in a dose-dependent manner.Dipyrithione (1 μM; 8.5 h) suppresses LPS-induced increase of iNOS but not COX-2 mRNA level, inhibits LPS-increased NO production.Dipyrithione (3 μM; 2, 5 h) decreases phosphorylation of STAT1 induced by LPS and does not influence LPS-induced MAPK and NF-κB activation in RAW 246.7 cells.Dipyrithione (0-5 μg/mL; 48 h) shows antiproliferative activity for KB, 231, U937 and K562 cells in a dose dependent manner.Dipyrithione (2.5 μg/ml) induces apoptosis and cycle arrest at G1 phase. Western Blot Analysis Cell Line:RAW264.7 cells Concentration:1-5 μM Incubation Time:8.5 h Result:Inhibited the expression of LPS (100 ng/ml)-induced up-regulation of iNOS and COX-2 in a dose-dependent manner.Cell Proliferation Assay Cell Line:KB, 231, U937, K562 cellsConcentration:2.5 μg/ml Incubation Time:24 h Result:Induced cell cycle arrest at G1 phase with induced p21 accumulation, CyclinD1 and CyclinE1 expressions were downregulated.Apoptosis Analysis Cell Line:KB, 231, U937, K562 cells Concentration:2.5 μg/ml Incubation Time:36 h Result:Induced apoptosis by induced cleavage of caspase-9, caspase-3 and PARP.Western Blot Analysis Cell Line:RAW264.7 cells Concentration:1-5 μM Incubation Time:8.5 hResult:Inhibited the expression of LPS (100 ng/ml)-induced up-regulation of iNOS and COX-2 in a dose-dependent manner.

Dipyrithione (0.2 mg/cm2; externally once daily for 10 days) shows great anti-dermatophyte activity effects in guinea pig.Dipyrithione (1, 2.5, 5 mg/kg; i.p.) shows anti-inflammatory activity in mouse.Dipyrithione (5 mg/kg; i.p.; daily for 10 days) shows anti-tumor acyivity in mouse. Animal Model:Guinea pig (infected with Trichophyton rubrum)Dosage:0.2 mg/cm2 Administration:Externally once daily for 10 days Result:Showed normal hair growth, with no scaly skin.Animal Model:18-22g male ICR mice2 Dosage:1, 2.5, 5 mg/kg Administration:I.p.Result:Raised the survival rate from 10% to 30%, 60% and 90%, respectively.Animal Model:6 weeks, 18-20 g male ICR mice (hepatoma 22 (H22) cells)Dosage:2.5 mg/kg Administration:I.p.; daily for 10 days Result:Inhibited the growth of tumor.

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Others

Other Targets

others

Metabolic Disease

dandruff

3696-28-4

252.32

C10H8N2O2S2

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (39.63 mM)

[O-][n+]1ccccc1SSc1cccc[n+]1[O-]

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(-20℃)

With Ice Pack

≥ 2 years