New potent and selective transforming growth factor-β type I receptor inhibitor

[skunkworks]

https://www.jstage.jst.go.jp/article/cpb/61/3/61_c12-00856/_pdf

7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole 11 (TASP0382088) was synthesized and evaluated as transforming growth factor-β (TGF-β) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitor. Compound 11, a potent and selective ALK5 inhibitor, exhibited good enzyme inhibitory activity (IC50=4.8 nM) as well as inhibitory activity against TGF-β-induced Smad2/3 phosphorylation at a cellular level (IC50=17 nM). The introduction of a methoxy group to the benzothiazole ring in 1 and the break up of the planarity between the imidazole ring and the thiazole ring improved the solubility in the lotion base of 11. Furthermore, the topical application of 3% 11 lotion significantly inhibited Smad2 phosphorylation in mouse skin at 8 h after application (71% inhibition, compared with vehicle-treated animals).

[james1947]

skunkworks

The PDF is to complicated for me to understand
Can you post some highlights, like % of success?

James

[skunkworks]

Not really, as the study is on alopecia. It is interesting though as it is a potent tgf-beta 1 receptor blocker, and a topical at that. It is highly possible that this could be an effective treatment against Peyronie's, similar to pentoxyfilline but topically.

[james1947]

How we can put hands on this topical treatment?
I had to stop Pentox because I was getting flue every 6 to 8 weeks.

James  

[MattFoley]

I might be reading it wrong but I think this chemical might keep you from getting Peyronie's not treat it. So, if you get the onset of Peyronie's, theoretically this chemical could put a stop to it. For those of us that have it, it's too late to use this chemical. The reason that this is good for alopecia is because alopecia keeps coming back. Thoughts?