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SW03329115-PGDH enzyme inhibitor

SW033291

Catalog No. A8709
Size Price Stock Qty
5mg $90.00 In stock
25mg $365.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

SW033291

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Chemical Properties

Cas No. 459147-39-8 SDF Download SDF
Chemical Name 2-(butylsulfinyl)-4-phenyl-6-(thiophen-2-yl)thieno[2,3-b]pyridin-3-amine
Canonical SMILES NC1=C(S(CCCC)=O)SC2=NC(C3=CC=CS3)=CC(C4=CC=CC=C4)=C21
Formula C21H20N2OS3 M.Wt 412.59
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

SW033291 is a potent inhibitor of 15-PGDH enzyme with IC50 value of 1.5 nM and dissociation constant Ki app value of 0.1 nM. SW033291 inhibits 15-PGDH with noncompetitive pattern. SW033291 shifted the 15-PGDH melting temperature by 13.5°C. [1]
Treatment of A549 cells with SW033291 increased PGE2 levels by 3.5-fold at 500 nM, with EC50 value of ~75 nM. In CD45 cells, SW033291 treatment induced a greater than four-fold increase in expression of CXCL12 and SCF. In SKL cells, SW033291 had no significant effects on expression of CXCL12, SCF, CXCR4, survivin, or JAG1. SW033291 also increased cyclic AMP levels in CD45 cells. SW033291 treatment increases the expression of cytokines from the hematopoietic niche. [1]
The phenotype of mice injected with SW033291 closely matched with 15-PGDH knockout mice (10mg/kg). SW033291 induced a two-fold increase in PGE2 levels in bone marrow, colon, lung, and liver. Importantly, no toxicity was induced by injecting SW033291 for inhibition of 15-PGDH in adult mice. Mice injected with SW033291 exhibited many good benefits, such as doubling peripheral neutrophils, a 65% increase in marrow SKL cells, a 71% increase in marrow SLAM cells, and 55% increases in the numbers of hematopoietic colonies. [1]
Reference:
1.    Zhang Y, Desai A, Yang SY et al. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration. Science. 2015 Jun 12;348(6240). pii: aaa2340.