GSK484 HCl
GSK484 is a potent PAD-4 inhibitor (Protein-arginine deiminase type-4). GSK484 potently binds to the low-calcium form of PAD4 in a reversible manner (IC50 of 50 nM) and appears to be competitive with substrate. GSK484’s selectivity for PAD4 over PAD1-3 was shown in cells and also confirmed with recombinant enzymes. This probe is an inhibitor of cellular citrullination in primary neutrophils, and further phenotypic profiling has confirmed its ability to inhibit NET formation in both mouse and human neutrophils. GSK484 exhibits favourable pharmacokinetic profiles, with low-moderate clearance, and good volume of distribution and half-life in mouse and rat, and has suitable a PK profile for use as a potential in vivo tool. (http://www.thesgc.org/chemical-probes/GSK484).
For research use only. We do not sell to patients.
Chemical Information
| Name | GSK484 HCl |
|---|---|
| Iupac Chemical Name | ((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 |
| Synonyms | GSK484; GSK-484; GSK 484. |
| Molecular Formula | C27H32ClN5O3 |
| Molecular Weight | 510.035 |
| Smile | O=C(N1C[C@H](N)[C@H](O)CC1)C2=CC(OC)=C3N(C)C(C(N4CC5CC5)=CC6=C4C=CC=C6)=NC3=C2.[H]Cl |
| InChiKey | MULKOGJHUZTANI-ADMBKAPUSA-N |
| 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 |
| CAS Number | 1652591-81-5 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Chemical Structure
