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GSK484

GSK484 Structure
GSK484
  • CAS No.1652591-81-5
  • Chemical Name:GSK484
  • CBNumber:CB63146499
  • Molecular Formula:C27H32ClN5O3
  • Formula Weight:510.04
  • MOL File:1652591-81-5.mol
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|
  • UNSPSC Code 51111800
  • NACRES NA.77
Safety
  • HS Code  :2933399990
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P305+P351+P338
GSK484 Price More Price(2)
  • Brand: Sigma-Aldrich(India)
  • Product number: SML1658
  • Product name : GSK484
  • Purity: ≥98% (HPLC)
  • Packaging: 5MG
  • Price: ₹35874.05
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: SML1658
  • Product name : GSK484
  • Purity: ≥98% (HPLC)
  • Packaging: 25MG
  • Price: ₹137953.8
  • Updated: 2022/06/14
  • Buy: Buy

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].

GSK484 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK484 Suppliers
Global(106)Suppliers
  • Supplier：
    Career Henan Chemica Co
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  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：
  • Email：support@targetmol.com
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GSK484 Spectrum
1652591-81-5, GSK484Related Search:
  • 化学试剂
  • 药靶配体
  • 小分子API
  • 生化试剂
  • 抑制剂
  • C27H31N5O3ClH
  • 652591-81-5
  • GSK484盐酸盐,10 MM DMSO 溶液
  • GSK484,PAD4抑制剂
  • GSK485 HYDROCHLORIDE
  • GSK484,可逆的PAD4抑制剂
  • ((3S,4R)-3-氨基-4-羟基哌啶-1-基)(2-(1-(环丙基甲基)-1H-吲哚-2-基)-7-甲氧基-1-甲基-1H-苯并[D]咪唑-5-基)甲酮盐酸盐
  • GSK484盐酸盐
  • 1652591-81-5
  • GSK484 hydrochloride, 10 mM in DMSO
  • GSK484, PAD4 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 hydrochloride,GSK 484,Protein Arginine Deiminase,GSK-484,GSK-484 hydrochloride,GSK484,inhibit,Peptidylarginine Deiminase,Inhibitor
  • PAD4 inhibitor GSK484
  • GSK484 >=98% (HPLC)
  • GTPL8577
  • AOB6992
  • ((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
  • PAD4 inhibitor GS484
  • CS-2265
  • GSK484 (hydrochloride)
  • GSK484

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