ChemicalBook > CAS DataBase List > GSK484

GSK484

Product Name
GSK484
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, PAD4 inhibitor
CBNumber
CB63146499
Molecular Formula
C27H32ClN5O3
Formula Weight
510.04
MOL File
1652591-81-5.mol
More
Less

GSK484 Property

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
Water Solubility 
H2O: 2mg/mL, clear (warmed)
InChIKey
MULKOGJHUZTANI-JEGYXLSDNA-N
SMILES
C(C1CC1)N1C2=CC=CC=C2C=C1C1=NC2=CC(C(N3CC[C@@H](O)[C@@H](N)C3)=O)=CC(OC)=C2N1C.Cl |&1:22,24,r|
More
Less

Safety

HS Code 
2933399990
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1658
Product name
GSK484
Purity
≥98% (HPLC)
Packaging
5MG
Price
$365
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1658
Product name
GSK484
Purity
≥98% (HPLC)
Packaging
25MG
Price
$1420
Updated
2025/07/31
Cayman Chemical
Product number
17488
Product name
GSK484 (hydrochloride)
Purity
≥95%
Packaging
500μg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
17488
Product name
GSK484 (hydrochloride)
Purity
≥95%
Packaging
1mg
Price
$68
Updated
2024/03/01
Cayman Chemical
Product number
17488
Product name
GSK484 (hydrochloride)
Purity
≥95%
Packaging
5mg
Price
$283
Updated
2024/03/01
More
Less

GSK484 Chemical Properties,Usage,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.

in vivo

To address whether PAD4 inhibition can suppress cancer-associated kidney injury, MMTV-PyMT mice are treated with the PAD4 inhibitor GSK484 at 4 mg/kg daily for one week. This dose suppress the elevated number of neutrophils undergoing NETosis in peripheral blood in mice with cancer. In parallel, the total protein level in urine from MMTV-PyMT mice is significantly reduced compared with untreated tumor-bearing mice, further supporting an improved functional status of the kidneys after GSK484 treatment. Administration of GSK484 at a dose of 4 mg/kg daily during one week reverts signs of kidney dysfunction in tumor-bearing mice to the same extent as DNase I treatment, without any detectable signs of toxicity[2].

References

[1] HUW D LEWIS. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation[J]. Nature chemical biology, 2015, 11 3: 189-191. DOI: 10.1038/nchembio.1735
[2] MARINA LI. A Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma.[J]. Molecular Cancer Therapeutics, 2020, 19 7: 1530-1538. DOI: 10.1158/1535-7163.mct-19-1020
[3] YEBIN ZHOU. Evidence for a direct link between PAD4-mediated citrullination and the oxidative burst in human neutrophils.[J]. Scientific Reports, 2018: 15228. DOI: 10.1038/s41598-018-33385-z

GSK484 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

GSK484 Suppliers

China 113 India 1 United States 8 Global 122
Changzhou Borl Biotechnology Co.,LTD
Tel
13606124132;13656121842
Email
luyan0021@163.com
Country
China
ProdList
235
Advantage
58
Hubei Chuchang Chemical Co., Ltd
Tel
18 15623560702
Email
info@chuchangbiotech.com
Country
China
ProdList
162
Advantage
58
Beijing Ouhe Technology Co., Ltd
Tel
010-010-82967028 13522913783
Fax
+86-10-82967029
Email
2355560935@qq.com
Country
China
ProdList
12000
Advantage
60
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Shanghai Macklin Biochemical Co.,Ltd.
Tel
15221275939
Fax
021-50706099
Email
shenlinxing@macklin.cn
Country
China
ProdList
15873
Advantage
55
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51395
Advantage
80
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2989
Advantage
58
More
Less

View Lastest Price from GSK484 manufacturers

Hubei Chuchang Biotech Co., Ltd.
Product
GSK484 (hydrochloride) 1652591-81-5
Price
US $0.00-0.00/mg
Min. Order
1mg
Purity
98%
Supply Ability
100G
Release date
2024-04-17

1652591-81-5, GSK484Related Search:

GSK J4 HCl GSK 2334470 GSK2982772 GSK2636771 Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]- GSK778 N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide RET Kinase inhibitor 1 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide GSK583 GSK369796 GSK461364 GSK547 GSK-467 GSK481 GSK-3326595 GSK864 S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide

  • 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
  • ((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 , GSK484 HCl
  • GSK484, PAD4 inhibitor
  • GSK484 hydrochloride, 10 mM in DMSO
  • GSK-484 hydrochloride (GSK484)
  • (3S,4R)-3-amino-1-({2-[1-(cyclopropylmethyl)indol-2-yl]-7-methoxy-1-methyl-1,3-benzodiazol-5-yl}carbonyl)piperidin-4-ol hydrochloride - [AC77953]
  • 1652591-81-5
  • 652591-81-5
  • C27H31N5O3ClH