Identification | Back Directory | [Name]
N-[[L-trans-3-(Ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-leucyl-3-(p-hydroxyphenyl)ethylamide | [CAS]
262381-84-0 | [Synonyms]
XSC-2 JPM-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)- | [Molecular Formula]
C20H28N2O6 | [MDL Number]
MFCD16660940 | [MOL File]
262381-84-0.mol | [Molecular Weight]
392.45 |
Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO:125.0(Max Conc. mg/mL);318.51(Max Conc. mM) | [form ]
Solid | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity[1][2]. | [in vivo]
JPM-OEt (50 mg/kg; i.p.; daily for 30 days) reduces tumor cathepsin B activity significantly[1].
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[2].
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[3]. Animal Model: | Female mice of a transgenic mouse[3] | 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.
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| [References]
[1] Withana NP, et al. Cathepsin B inhibition limits bone metastasis in breast cancer. Cancer Res. 2012 Mar 1;72(5):1199-209. DOI:10.1158/0008-5472.CAN-11-2759 [2] Bell-McGuinn KM, et al. Inhibition of cysteine cathepsin protease activity enhances chemotherapy regimens by decreasing tumor growth and invasiveness in a mouse model of multistage cancer. Cancer Res. 2007 Aug 1;67(15):7378-85. DOI:10.1158/0008-5472.CAN-07-0602 [3] Schurigt U, et al. Trial of the cysteine cathepsin inhibitor JPM-OEt on early and advanced mammary cancer stages in the MMTV-PyMT-transgenic mouse model. Biol Chem. 2008 Aug;389(8):1067-74. DOI:10.1515/BC.2008.115 |
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Company Name: |
Shanghai Ennopharm Co., Ltd.
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Tel: |
+86 (21) 6435-5022 |
Website: |
m.approvedhomemanagement.com/ShowSupplierProductsList13640/0.htm |
Company Name: |
Alabiotech Inc.
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Tel: |
001-619-354-5251 |
Website: |
www.alabiotech-e.com |
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