GSK484

SIGMA/SML1658 - ≥98% (HPLC)

Synonym: ((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 hydrochloride; AOB6992; GSK 484; GSK-484 hydrochloride; GTPL8577

CAS Number: 1652591-81-5
Empirical Formula (Hill Notation): C₂₇H₃₁N₅O₃ · HCl
Molecular Weight: 510.03
Linear Formula: C₂₇H₃₁N₅O₃ · HCl
Product Type: Chemical

Catalog Number	PKG Qty.	Price


45-SML1658-5MG	5 mg	$355.00 1/EA	Add To Favorites
45-SML1658-25MG	25 mg	$1380.00 1/EA	Add To Favorites

Properties
Descriptions
Safety Info.
Basic Data

assay	≥98% (HPLC)
color	white to beige
form	powder
InChI	1S/C27H31N5O3.ClH/c1-30-25-20(11-18(13-24(25)35-2)27(34)31-10-9-23(33)19(28)15-31)29-26(30)22-12-17-5-3-4-6-21(17)32(22)14-16-7-8-16;/h3-6,11-13,16,19,23,33H,7-10,14-15,28H2,1-2H3;1H/t19-,23+;/m0./s1
InChI key	MULKOGJHUZTANI-ADMBKAPUSA-N
Quality Level	100
SMILES string	[H]Cl.CN1C(C2=CC(C=CC=C3)=C3N2CC4CC4)=NC5=C1C(OC)=CC(C(N6C[C@H](N)[C@H](O)CC6)=O)=C5
solubility	H₂O: 2 mg/mL, clear (warmed)
storage temp.	2-8°C

Biochem/physiol Actions:	GSK484 is a potent selective reversible inhibitor of protein arginine deiminase PAD4, an enzyme believed to play a role in granulocyte and macrophage development leading to inflammation and immune response, and overexpressed in many tumors. GSK484 has IC₅₀ values of 50 nM without calcium and 250 nM in the presence of 2 mM calcium. GSK484 showed minimal off-target activity tested against 50 other proteins with no activation across HDACs 1–11 even at 100 μM. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is reordered to form a β-hairpin. For full characterization details, please visit the GSK484 probe summary on the Structural Genomics Consortium (SGC) website. To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
Features and Benefits:	GSK484 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC .
Features and Benefits:	This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm .
Other Notes:	GSK484 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK484 probe summary on the Chemical Probes Portal website.
Packaging:	5, 25 mg in glass bottle

RIDADR	NONH for all modes of transport
WGK Germany	WGK 3
Flash Point(F)	Not applicable
Flash Point(C)	Not applicable

Purity	≥98% (HPLC)
Storage Temp.	2-8°C
UNSPSC	12352200

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