N-[苄氧羰基]-L-色氨酰-L-ALPHA-谷氨酰-N-[(1S)-3-氟-1-(2-甲氧基-2-氧代乙基)-2-氧代丙基]-L-组胺酰胺甲基酯
- CAS号:210345-00-9
- 英文名:CASPASE-1 INHIBITOR TFA SALT
- 中文名:N-[苄氧羰基]-L-色氨酰-L-ALPHA-谷氨酰-N-[(1S)-3-氟-1-(2-甲氧基-2-氧代乙基)-2-氧代丙基]-L-组胺酰胺甲基酯
- CBNumber:CB8382359
- 分子式:C37H42FN7O10
- 分子量:763.77
- MOL File:210345-00-9.mol
- 沸点 :1129.2±65.0 °C(Predicted)
- 密度 :1.349±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :insoluble in H2O; ≥26.32 mg/mL in EtOH with ultrasonic; ≥46.33 mg/mL in DMSO
- 形态 :Powder
- 酸度系数(pKa) :11.06±0.46(Predicted)
- 颜色 :Light yellow to yellow
N-[苄氧羰基]-L-色氨酰-L-ALPHA-谷氨酰-N-[(1S)-3-氟-1-(2-甲氧基-2-氧代乙基)-2-氧代丙基]-L-组胺酰胺甲基酯性质、用途与生产工艺
- 生物活性 Z-WEHD-FMK 是一种强效具有细胞通透性可逆的 caspase-1/5 抑制剂。Z-WEHD-FMK 也抑制 cathepsin B 的活性 (IC50=6 μM)。Z-WEHD-FMK 可用于检测细胞凋亡。
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靶点
Caspase-1
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体外研究
Z-WEHD-FMK (80 μM; 9 hours) elicits a near-complete blockage of C. trachomatis -induced cleavage of golgin-84 and increases GM130 expression in cells.Z-WEHD-FMK (30 min before being exposed to E. piscicida ) effectively inhibits 0909I E. piscicida induced ZF4 cells cytotoxicity and pyroptotic morphology. And in addition, it also inhibits the cytotoxicity induced by cytosolic LPS delivery.Z-WEHD-FMK (20 μM;18-24 hours following Cr 3+ ,Ni 2+ , and Co 2+ ) significantly induces a decrease of 76% to 86% in IL-1β release with 200 to 400 ppm Cr 3+ , it also induces a decrease of 35% to 45% with 48 ppm Ni 2+ or higher, Finally, this caspase-1 inhibitor induced a decrease with 6 ppm Co 2+ , down to a level below the detection threshold, and a decrease of 40% to 48% with 12 to 24 ppm Co 2+ in bone marrow-derived macrophages (BMDM).
Western Blot Analysis
Cell Line: C. trachomatis - or mock-infected HeLa cells Concentration: 80 μM Incubation Time: 9 hours Result: Increased golgin-84 and GM130 expression. Cell Viability Assay
Cell Line: Mycoplasma free-ZF4 cells Concentration: Incubation Time: 30 min before being exposed to E. piscicida Result: Inhibited ZF4 cells cytotoxicity and pyroptotic morphology.
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