262381-84-0
中文名稱
N-[[L-TRANS-3-(ETHOXYCARBONYL)OXIRAN-2-YL]CARBONYL]-L-LEUCYL-3-(P-HYDROXYPHENYL)ETHYLAMIDE
英文名稱
N-[[L-trans-3-(Ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-leucyl-3-(p-hydroxyphenyl)ethylamide
CAS
262381-84-0
分子式
C20H28N2O6
分子量
392.45
MOL 文件
262381-84-0.mol
262381-84-0 結(jié)構(gòu)式
基本信息
中文別名
JPM 565 乙基酯 英文別名
XSC-2JPM-OEt
JPM 565-OEt
JPM 565 ethyl ester
N-[[L-trans-3-(Ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-leucyl-3-(p-hydroxyphenyl)ethylamide
(2S,3S)-3-[[[(1S)-1-[[[2-(4-Hydroxyphenyl)ethyl]amino]carbonyl]-3-methylbutyl]amino]carbonyl]-2-oxiranecarboxylic acid ethyl ester
2-Oxiranecarboxylic acid, 3-[[[(1S)-1-[[[2-(4-hydroxyphenyl)ethyl]amino]carbonyl]-3-methylbutyl]amino]carbonyl]-, ethyl ester, (2S,3S)-
物理化學(xué)性質(zhì)
儲存條件4°C, protect from light
溶解度DMSO:125.0(Max Conc. mg/mL);318.51(Max Conc. mM)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
JPM-OEt 是一種廣譜的半胱氨酸組織蛋白酶 (cysteine cathepsin) 抑制劑。JPM-OEt 在活性位點(diǎn)共價結(jié)合，并且不可逆地抑制半胱氨酸組織蛋白酶家族。具有抗腫瘤活性。體內(nèi)研究
JPM-OEt (50 mg/kg; i.p.; daily for 30 days) reduces tumor cathepsin B activity significantly.
JPM-OEt (50 mg/kg; i.p.; twice daily for 4 weeks) leads to tumor regression in the RIP1-Tag2 (RT2) mouse model of pancreatic islet cell tumorigenesis.
JPM-OEt (50 mg/kg; i.p.; daily from 63 to 98 days) causes a significant delay in the increase of tumour burden during the first 2 weeks of treatment.
| Animal Model: | Female mice of a transgenic mouse |
| Dosage: | 50 mg/kg |
| Administration: | i.p.; daily from 63 to 98 days |
| Result: | Caused a significant delay in the increase of tumour burden during the first 2 weeks of treatment. However, on days 84, 91 and 98 no significant differences between both groups could be detected. |