GSK484

GSK484 Structure
CAS No.
1652591-81-5
Chemical Name:
GSK484
Synonyms
GSK484;CS-2265;AOB6992;GTPL8577;GSK484 HCl;GSK484 >=98% (HPLC);PAD4 inhibitor GS484;PAD4 inhibitor GSK484;GSK484 (hydrochloride);GSK484 hydrochloride,GSK 484,Protein Arginine Deiminase,GSK-484,GSK-484 hydrochloride,GSK484,inhibit,Peptidylarginine Deiminase,Inhibitor
CBNumber:
CB63146499
Molecular Formula:
C27H32ClN5O3
Molecular Weight:
510.04
MOL File:
1652591-81-5.mol
Modify Date:
2024/4/17 13:57:11

GSK484 Properties

storage temp. 2-8°C
solubility DMSO:25.0(Max Conc. mg/mL);49.01(Max Conc. mM)
Ethanol:25.0(Max Conc. mg/mL);49.01(Max Conc. mM)
PBS buffer (pH 7.2):5.0(Max Conc. mg/mL);9.8(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);58.82(Max Conc. mM)
form powder
color white to beige

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338
HS Code  2933399990

GSK484 price More Price(2)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich(India) SML1658 GSK484 ≥98% (HPLC) 1652591-81-5 5MG ₹35874.05 2022-06-14 Buy
Sigma-Aldrich(India) SML1658 GSK484 ≥98% (HPLC) 1652591-81-5 25MG ₹137953.8 2022-06-14 Buy
Product number Packaging Price Buy
SML1658 5MG ₹35874.05 Buy
SML1658 25MG ₹137953.8 Buy

GSK484 Chemical Properties,Uses,Production

Description

GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme. It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils. It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC) website for more information.

Uses

GSK484 is a novel selective PAD4 inhibitor.

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

GSK484 Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 91)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
Hubei Chuchang Biotech Co., Ltd. +86-18727130788 +86-18727130788 China 109 58 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32760 60 Inquiry
Career Henan Chemica Co +86-0371-86658258 +8613203830695 China 30253 58 Inquiry
Zhejiang J&C Biological Technology Co.,Limited +1-2135480471 +1-2135480471 China 10522 58 Inquiry
InvivoChem +1-708-310-1919 +1-13798911105 United States 6393 58 Inquiry
LEAP CHEM CO., LTD. +86-852-30606658 China 24738 58 Inquiry
Nantong HI-FUTURE Biology Co., Ltd. +undefined18051384581 China 3136 58 Inquiry
Hebei Miaoyin Technology Co.,Ltd +86-17367732028 +86-17367732028 China 3582 58 Inquiry
Wuhan Topule Biopharmaceutical Co., Ltd +8618327326525 China 8474 58 Inquiry
GSK484 GSK484 (hydrochloride) CS-2265 PAD4 inhibitor GS484 GSK484 HCl ((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 GTPL8577 GSK484 >=98% (HPLC) PAD4 inhibitor GSK484 GSK484 hydrochloride,GSK 484,Protein Arginine Deiminase,GSK-484,GSK-484 hydrochloride,GSK484,inhibit,Peptidylarginine Deiminase,Inhibitor 1652591-81-5 652591-81-5 C27H31N5O3ClH