GSK3494245

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GSK3494245

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2080410-41-7

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议

产品介绍

GSK3494245 (DDD01305143) 是一种有效的、具有口服活性的、选择性的可在夹在 β4 和 β5 亚基之间的位点结合寄生虫蛋白酶体 (proteasome) 的糜蛋白酶样活性抑制剂(对于 WT L.donovani蛋白酶体IC50=0.16μM)。GSK3494245 适度抑制人蛋白酶体的糜蛋白酶样活性 (IC50: 26S=13 µM；富集的 THP-1 提取物 IC50=40 µM)。GSK3494245 具有良好的生物安全特性。

Cas No.	2080410-41-7
别名	DDD01305143?
分子式	C21H23FN6O2
分子量	410.44
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties[1][2]. GSK3494245 shows EC50 value of 5.7 μM in L. donovani intramacrophage assay, where the amastigotes are cultured in differentiated THP-1 cells. GSK3494245 demonstrates good selectivity over mammalian cell growth inhibition (THP-1 cells; EC50 >50 μM)[1].GSK3494245 (DDD01305143) shows pEC50s of 6.5 and 5.8 against axenic amastigote and ld InMac, respectively. Ld InMac is the intramacrophage assay carried out in THP-1 cells with L. donovani amastigote[2]. GSK3494245 (25 mg/kg; orally twice a day for 10 consecutive days) elicits a >95% reduction of parasite load in Infected mice (L. donovani, LV9)[1]. [1]. Wyllie S, et al. Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition. Proc Natl Acad Sci U S A. 2019;116(19):9318-9323. [2]. Thomas MG, et al. Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis. J Med Chem. 2019;62(3):1180-1202.