210345-00-9

中文名称 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

英文名称 CASPASE-1 INHIBITOR TFA SALT

CAS 210345-00-9

分子式 C37H42FN7O10

分子量 763.77

MOL 文件 210345-00-9.mol

210345-00-9 结构式

基本信息物理化学性质图谱信息常见问题列表

基本信息

中文别名

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

英文别名

Z-WEHD-FMK-TFA
CASPASE-1 INHIBITOR TFA SALT
Caspase-1/ICE Inhibitor Z-WEHD-FMK
Z-TRP-GLU(OME)-HIS-ASP(OME)-FMK-TFA
Z-WE(OME)HD(OME)-FMK
Z-TRP-GLU(OME)-HIS-ASP(OME)-FMK
Z-TRP-GLU(OME)-HIS-ASP(OME)-FLUOROMETHYLKETONE
N-[(Phenylmethoxy)carbonyl]-L-tryptophyl-L-alpha-glutamyl-N-[(1S)-3-fluoro-1-(2-methoxy-2-oxoethyl)-2-oxopropyl]-L-histidinamide methyl ester
L-Histidinamide, N-[(phenylmethoxy)carbonyl]-L-tryptophyl-L-α-glutamyl-N-[(1S)-3-fluoro-1-(2-methoxy-2-oxoethyl)-2-oxopropyl]-, methyl ester (9CI)

物理化学性质

沸点1129.2±65.0 °C(Predicted)

密度1.349±0.06 g/cm3(Predicted)

储存条件-20°C储存

溶解度insoluble in H2O; ≥26.32 mg/mL in EtOH with ultrasonic; ≥46.33 mg/mL in DMSO

酸度系数(pKa)11.06±0.46(Predicted)

形态粉末

颜色Light yellow to yellow

图谱信息

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(210345-00-9)质谱(MS)

常见问题列表

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。

靶点

Caspase-1

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.