GSK2795039 | CAS# 1415925-18-6 | NOX2 Inhibitor

MedKoo Cat#: 565076 | Name: GSK2795039

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK2795039 is the first small molecule NADPH oxidase 2 (NOX2) inhibitor.

Chemical Structure

GSK2795039

CAS#1415925-18-6

Theoretical Analysis

MedKoo Cat#: 565076

Name: GSK2795039

CAS#: 1415925-18-6

Chemical Formula: C23H26N6O2S

Exact Mass: 450.1838

Molecular Weight: 450.56

Elemental Analysis: C, 61.31; H, 5.82; N, 18.65; O, 7.10; S, 7.12

Price and Availability

Size	Price	Availability
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,350.00	Ready to ship
500mg	USD 2,950.00	Ready to ship

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Related CAS #

No Data

Synonym

GSK-2795039; GSK 2795039; GSK2795039

IUPAC/Chemical Name

N-(1-Isopropyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamide

InChi Key

FMWVTCZKCXPKFW-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H26N6O2S/c1-15(2)29-14-18(17-6-5-16-8-11-27(3)20(16)13-17)22-19(7-10-24-23(22)29)26-32(30,31)21-9-12-28(4)25-21/h5-7,9-10,12-15H,8,11H2,1-4H3,(H,24,26)

SMILES Code

O=S(C1=NN(C)C=C1)(NC2=C3C(N(C(C)C)C=C3C4=CC5=C(C=C4)CCN5C)=NC=C2)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

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.

Storage Condition

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

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A23T04K25

QC Data

View QC data: current batch, Lot#A23T04K25

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

GSK2795039 is a NADPH oxidase 2 (NOX2) inhibitor with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption.

In vitro activity:

GSK2795039 inhibited both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. It inhibited NOX2 in an NADPH competitive manner and was selective over other NOX isoforms, xanthine oxidase, and endothelial nitric oxide synthase enzymes. Reference: Antioxid Redox Signal. 2015 Aug 10;23(5):358-74. https://pubmed.ncbi.nlm.nih.gov/26135714/

In vivo activity:

Treatment with GSK2795039 significantly improved the neurological function score 72 hours after collagenase injection (P < 0.05 or P < 0.01; Figure 8E–G) and alleviated brain edema, both 24 and 72 hours after collagenase injection (P < 0.01 or P < 0.001; Figure 8H), compared with the mouse control groups. These results suggested that the inhibition of NOX2 attenuated P2X7R-mediated oxidative stress following ICH. Reference: Neural Regen Res. 2021 Aug;16(8):1582-1591. https://pubmed.ncbi.nlm.nih.gov/33433488/

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	66.58
	DMSO	66.3	147.07
	DMSO:PBS (pH 7.2) (1:4)	0.2	0.44
	Ethanol	20.0	44.39

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 450.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Hirano K, Chen WS, Chueng AL, Dunne AA, Seredenina T, Filippova A, Ramachandran S, Bridges A, Chaudry L, Pettman G, Allan C, Duncan S, Lee KC, Lim J, Ma MT, Ong AB, Ye NY, Nasir S, Mulyanidewi S, Aw CC, Oon PP, Liao S, Li D, Johns DG, Miller ND, Davies CH, Browne ER, Matsuoka Y, Chen DW, Jaquet V, Rutter AR. Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor. Antioxid Redox Signal. 2015 Aug 10;23(5):358-74. doi: 10.1089/ars.2014.6202. PMID: 26135714; PMCID: PMC4545375. 2. Deng H, Zhang Y, Li GG, Yu HH, Bai S, Guo GY, Guo WL, Ma Y, Wang JH, Liu N, Pan C, Tang ZP. P2X7 receptor activation aggravates NADPH oxidase 2-induced oxidative stress after intracerebral hemorrhage. Neural Regen Res. 2021 Aug;16(8):1582-1591. doi: 10.4103/1673-5374.303036. PMID: 33433488; PMCID: PMC8323669. 3. Hu XF, Xiang G, Wang TJ, Ma YB, Zhang Y, Yan YB, Zhao X, Wu ZX, Feng YF, Lei W. Impairment of type H vessels by NOX2-mediated endothelial oxidative stress: critical mechanisms and therapeutic targets for bone fragility in streptozotocin-induced type 1 diabetic mice. Theranostics. 2021 Jan 30;11(8):3796-3812. doi: 10.7150/thno.50907. PMID: 33664862; PMCID: PMC7914348.

In vitro protocol:

In vivo protocol:

1. Deng H, Zhang Y, Li GG, Yu HH, Bai S, Guo GY, Guo WL, Ma Y, Wang JH, Liu N, Pan C, Tang ZP. P2X7 receptor activation aggravates NADPH oxidase 2-induced oxidative stress after intracerebral hemorrhage. Neural Regen Res. 2021 Aug;16(8):1582-1591. doi: 10.4103/1673-5374.303036. PMID: 33433488; PMCID: PMC8323669. 2. Hu XF, Xiang G, Wang TJ, Ma YB, Zhang Y, Yan YB, Zhao X, Wu ZX, Feng YF, Lei W. Impairment of type H vessels by NOX2-mediated endothelial oxidative stress: critical mechanisms and therapeutic targets for bone fragility in streptozotocin-induced type 1 diabetic mice. Theranostics. 2021 Jan 30;11(8):3796-3812. doi: 10.7150/thno.50907. PMID: 33664862; PMCID: PMC7914348.

1: Pick E. Absolute and Relative Activity Values in Assessing the Effect of NADPH Oxidase Inhibitors. Antioxid Redox Signal. 2015 Nov 20;23(15):1250-1. doi: 10.1089/ars.2015.6470. PubMed PMID: 26566924. 2: Jaquet V, Rutter AR. Response to Pick. Antioxid Redox Signal. 2015 Nov 20;23(15):1251-3. doi: 10.1089/ars.2015.6565. PubMed PMID: 26566578. 3: Hirano K, Chen WS, Chueng AL, Dunne AA, Seredenina T, Filippova A, Ramachandran S, Bridges A, Chaudry L, Pettman G, Allan C, Duncan S, Lee KC, Lim J, Ma MT, Ong AB, Ye NY, Nasir S, Mulyanidewi S, Aw CC, Oon PP, Liao S, Li D, Johns DG, Miller ND, Davies CH, Browne ER, Matsuoka Y, Chen DW, Jaquet V, Rutter AR. Discovery of GSK2795039, a Novel Small Molecule NADPH Oxidase 2 Inhibitor. Antioxid Redox Signal. 2015 Aug 10;23(5):358-74. doi: 10.1089/ars.2014.6202. PubMed PMID: 26135714; PubMed Central PMCID: PMC4545375.