GSK484 hydrochloride

CAS No. 1652591-81-5

GSK484 hydrochloride ( GTPL8577,AOB6992 )

Catalog No. M22058 CAS No. 1652591-81-5

GSK484 hydrochloride (GTPL8577) is a specifc and reversible peptidyl arginine deiminase 4 (PAD4) inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 142 In Stock
10MG 215 In Stock
25MG 434 In Stock
50MG 620 In Stock
100MG 884 In Stock
200MG Get Quote In Stock
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Biological Information

  • Product Name
    GSK484 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK484 hydrochloride (GTPL8577) is a specifc and reversible peptidyl arginine deiminase 4 (PAD4) inhibitor.
  • Description
    GSK484 hydrochloride (GTPL8577) is a specifc and reversible peptidyl arginine deiminase 4 (PAD4) inhibitor. It demonstrates high-affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium.GSK484 demonstrates high-affinity binding to the low-calcium form of PAD4 with IC50s of 50 nM and 250 nM in the absence of Calcium (0 mM) and Calcium (2 mM), respectively. GSK484 also inhibits PAD4 citrullination (at 0.2 mM Calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner.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 suppresses 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. 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.
  • Synonyms
    GTPL8577,AOB6992
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    PAD4
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1652591-81-5
  • Formula Weight
    510.03
  • Molecular Formula
    C27H30ClN5O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:60 mg/mL (117.64 mM; Need ultrasonic)
  • SMILES
    Cl.COC1=CC(=CC2=C1N(C)C(=N2)C1=CC2=CC=CC=C2N1CC1CC1)C(=O)N1CC[C@@H](O)[C@@H](N)C1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Lewis HD, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91.
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