GSK484 hydrochloride - ≥98%, high purity , CAS No.1652591-81-5

  • ≥98%
Item Number
G276185
Grouped product items
SKUSizeAvailabilityPrice Qty
G276185-1mg
1mg
In stock
$45.90
G276185-5mg
5mg
In stock
$187.90
G276185-10mg
10mg
In stock
$286.90
G276185-25mg
25mg
In stock
$583.90
G276185-50mg
50mg
In stock
$1,051.90

Potent, reversible inhibitor of PAD4

Basic Description

SynonymsPharmakon1600-01500687 | [(3S,4R)-3-amino-4-hydroxypiperidin-1-yl]-[2-[1-(cyclopropylmethyl)indol-2-yl]-7-methoxy-1-methylbenzimidazol-5-yl]methanone;hydrochloride | GSK484 | AKOS037643581 | (3S,4R)-3-amino-1-({2-[1-(cyclopropylmethyl)indol-2-yl]-7-methox
Specifications & Purity≥98%
Biochemical and Physiological MechanismsPotent and reversible inhibitor of PAD4 (Protein Arginine Deiminase 4) (IC 50 = 50 nM). Selective for PAD4 over PAD1-3. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is re-ordered to form
Storage TempStore at -20°C,Desiccated
Shipped InIce chest + Ice pads
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -80°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

 product description:

GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.


Associated Targets(Human)

ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Pubchem Sid488202420
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488202420
IUPAC Name [(3S,4R)-3-amino-4-hydroxypiperidin-1-yl]-[2-[1-(cyclopropylmethyl)indol-2-yl]-7-methoxy-1-methylbenzimidazol-5-yl]methanone;hydrochloride
INCHI InChI=1S/C27H31N5O3.ClH/c1-30-25-20(11-18(13-24(25)35-2)27(34)31-10-9-23(33)19(28)15-31)29-26(30)22-12-17-5-3-4-6-21(17)32(22)14-16-7-8-16;/h3-6,11-13,16,19,23,33H,7-10,14-15,28H2,1-2H3;1H/t19-,23+;/m0./s1
InChi Key MULKOGJHUZTANI-ADMBKAPUSA-N
Canonical SMILES CN1C2=C(C=C(C=C2OC)C(=O)N3CCC(C(C3)N)O)N=C1C4=CC5=CC=CC=C5N4CC6CC6.Cl
Isomeric SMILES CN1C2=C(C=C(C=C2OC)C(=O)N3CC[C@H]([C@H](C3)N)O)N=C1C4=CC5=CC=CC=C5N4CC6CC6.Cl
PubChem CID 86340151
Molecular Weight 510.03

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

10 results found

Lot NumberCertificate TypeDateItem
B2301805Certificate of AnalysisApr 11, 2024 G276185
B2301814Certificate of AnalysisMar 07, 2024 G276185
B2301924Certificate of AnalysisMar 07, 2024 G276185
B2301755Certificate of AnalysisFeb 01, 2024 G276185
B2301785Certificate of AnalysisFeb 01, 2024 G276185
B2301741Certificate of AnalysisNov 08, 2023 G276185
B2301780Certificate of AnalysisNov 08, 2023 G276185
B2301804Certificate of AnalysisNov 08, 2023 G276185
B2301806Certificate of AnalysisNov 08, 2023 G276185
B2301817Certificate of AnalysisNov 08, 2023 G276185

Chemical and Physical Properties

SolubilitySoluble in DMSO to 50 mM

Safety and Hazards(GHS)

RIDADR NONHforallmodesoftransport

Related Documents

References

1. Xia X et al..  (2022)  Neutrophil extracellular traps promote metastasis in gastric cancer patients with postoperative abdominal infectious complications..  Nat Commun,  13  (1017).  [PMID:35197446]

Solution Calculators