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 |
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10MG | 215 | In Stock |
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25MG | 434 | In Stock |
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50MG | 620 | In Stock |
|
100MG | 884 | In Stock |
|
200MG | Get Quote | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameGSK484 hydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionGSK484 hydrochloride (GTPL8577) is a specifc and reversible peptidyl arginine deiminase 4 (PAD4) inhibitor.
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DescriptionGSK484 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.
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SynonymsGTPL8577,AOB6992
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PathwayOthers
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TargetOther Targets
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RecptorPAD4
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Research Area——
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Indication——
Chemical Information
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CAS Number1652591-81-5
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Formula Weight510.03
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Molecular FormulaC27H30ClN5O3
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Purity>98% (HPLC)
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SolubilityDMSO:60 mg/mL (117.64 mM; Need ultrasonic)
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SMILESCl.COC1=CC(=CC2=C1N(C)C(=N2)C1=CC2=CC=CC=C2N1CC1CC1)C(=O)N1CC[C@@H](O)[C@@H](N)C1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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