GSK484|1652591-81-5--Shanghai xingMo Biotechnology

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Description

GSK484 is a potent PAD-4 inhibitor (Protein-arginine deiminase type-4). GSK484 potently binds to the low-calcium form of PAD4 in a reversible manner (IC50 of 50 nM) and appears to be competitive with substrate. GSK484’s selectivity for PAD4 over PAD1-3 was shown in cells and also confirmed with recombinant enzymes. This probe is an inhibitor of cellular citrullination in primary neutrophils, and further phenotypic profiling has confirmed its ability to inhibit NET formation in both mouse and human neutrophils. GSK484 exhibits favourable pharmacokinetic profiles, with low-moderate clearance, and good volume of distribution and half-life in mouse and rat, and has suitable a PK profile for use as a potential in vivo tool.

Chemical Structure

Chemical Name

((3S,4R)-3-amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone

SMILES Code

O[C@@H]1CCN(C[C@@H]1N)C(C2=CC3=C(C(OC)=C2)N(C)C(C4=CC5=C(N4CC6CC6)C=CC=C5)=N3)=O

Theoretical Analysis

XingMo Cat#:XM127
Product Name:GSK484
Synonyms:GSK484; GSK-484; GSK 484.
CAS#:1652591-81-5
Chemical Formula:C₂₇H₃₁N₅O₃
Exact Mass:473.2427
Molecular Weight:473.577

Technical Data

Appearance: solid powder

Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
Solubility: Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly.

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).

WARNING: This product is for research use only, not for human or veterinary use

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