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JNJ0966

Catalog No. T4783   CAS 315705-75-0

JNJ0966 is a highly selective MMP-9 zymogen inhibitor (IC50: 440 nM).

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JNJ0966 Chemical Structure
JNJ0966, CAS 315705-75-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 55.00
2 mg In stock $ 75.00
5 mg In stock $ 97.00
10 mg In stock $ 147.00
25 mg In stock $ 322.00
50 mg In stock $ 578.00
100 mg In stock $ 833.00
500 mg In stock $ 1,690.00
1 mL * 10 mM (in DMSO) In stock $ 76.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JNJ0966 is a highly selective MMP-9 zymogen inhibitor (IC50: 440 nM).
Targets&IC50 MMP9 zymogen:440 nM
In vitro The activations of proMMP-1, proMMP-2, and proMMP-3 are not significantly different in the presence or absence of 10 μM JNJ0966, whereas proMMP-9 activation by trypsin is significantly attenuated by JNJ0966. The addition of JNJ0966 to the reaction results in a significant reduction in fully processed MMP-9 and an apparent accumulation of the intermediate species[1].
In vivo JNJ0966 demonstrated effectiveness in alleviating the severity of disease in a mouse model of experimental autoimmune encephalomyelitis. Its effectiveness is dose-dependent, showing plasma and brain concentrations of 77.5±31.1 ng/mL (215 nM) and 481.6±162.5 ng/g (~1336 nM) at a 10-mg/kg dose, and 293.6±118.4 ng/mL (815 nM) in plasma and 1394.0±649.1 ng/g (~3867 nM) in the brain at a 30-mg/kg dose, respectively. Moreover, JNJ0966 exhibits a preference for accumulation in the brain, evidenced by brain/plasma ratios of 6.2 at the 10 mg/kg dose and 4.7 at the 30 mg/kg dose.
Molecular Weight 360.45
Formula C16H16N4O2S2
CAS No. 315705-75-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL(416.15 mM)

TargetMolReferences and Literature

1. Scannevin RH, et al. Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) thatallosterically inhibits zymogen activation. J Biol Chem. 2017 Oct 27;292(43):17963-17974.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Inhibitor Library Anti-Aging Compound Library Anti-Fibrosis Compound Library Bioactive Compound Library Target-Focused Phenotypic Screening Library Anti-Pancreatic Cancer Compound Library NO PAINS Compound Library Angiogenesis related Compound Library Anti-Cancer Compound Library

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Keywords

JNJ0966 315705-75-0 Proteases/Proteasome MMP Inhibitor Matrix metalloproteinases JNJ 0966 JNJ-0966 inhibit inhibitor

 

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