GSK3494245

Modify Date: 2024-01-09 18:56:30

GSK3494245 structure	Common Name	GSK3494245
	CAS Number	2080410-41-7	Molecular Weight	410.44
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₁H₂₃FN₆O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of GSK3494245

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].

Name	GSK3494245

Description	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].
Related Catalog	Research Areas >> Infection Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome
In Vitro	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].
In Vivo	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].
References	[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.

Molecular Formula	C₂₁H₂₃FN₆O₂
Molecular Weight	410.44

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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: GSK3494245
Price: Check
Purity: 98.0%
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DC Chemicals Limited
China
Product Name: GSK3494245
Price: $1500.0/100mg
Purity: 98.0%
Delivery: Inquiry
Contact: Tony Cao
Email: sales@dcchemicals.com

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GSK3494245

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The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.