(R)-N4-Hydroxy-N1-[(S)-2-(1H-indol-3-yl)-1-methylcarbamoyl-ethyl]-2-isobutyl-succinamide has been used:
To study its effect on the profiling of active aggrecanases and their specific aggrecan degradation fragments.[1]
To study the involvement of autocrine EGF (epidermal growth factor) receptor activation in the regulation of the morphogenetic process, using human umbilical vein endothelial cells.[2]
To study the effect of GM6001 blockade on the expression of angiotensin II, the interstitial collagenases and soluble elastin fragments in explant culture supernatants.[3]
Biochem/physiol Actions
GM6001 promotes cardiovascular and hepatocellular function.[4]
Inhibits a wide variety of matrix metalloproteases with Kis in the nanomolar range. Active in a number of animal models of diseases where matrix metalloproteases are thought to be involved.
The hydroxamic acid HONHCOCH2CH(i-Bu)CO-L-Trp-NHMe, isomer 6A (GM 6001), inhibits human skin fibroblast collagenase with Ki of 0.4 nM using the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. The other isomer, 6B, which has the opposite configuration at the CH2CH(i-Bu)CO
Autocrine EGF receptor activation mediates endothelial cell migration and vascular morphogenesis induced by VEGF under interstitial flow
Regeneration following spinal root avulsion is broadly unsuccessful despite the regenerative capacity of other PNS-located nerves. By combining focal laser lesioning to model root avulsion in zebrafish, time-lapse imaging, and transgenesis, we identify that regenerating DRG neurons fail to recapitulate
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