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SW-033291
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SW-033291图片
CAS NO:459147-39-8
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
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5mg电议
10mg电议
25mg电议
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产品介绍
理化性质和储存条件
Molecular Weight (MW)412.59
FormulaC21H20N2OS3
CAS No.459147-39-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 83 mg/mL (201.2 mM)
Water: <1 mg/mL
Ethanol: 32 mg/mL warmed (77.6 mM)
Other infoChemical Name: 2-(Butylsulfinyl)-4-phenyl-6-(2-thienyl)-thieno[2,3-b]pyridin-3-amine
InChi Key: LCYAYKSMOVLVRL-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H20N2OS3/c1-2-3-12-27(24)21-19(22)18-15(14-8-5-4-6-9-14)13-16(23-20(18)26-21)17-10-7-11-25-17/h4-11,13H,2-3,12,22H2,1H3
SMILES Code: NC1=C(S(CCCC)=O)SC2=NC(C3=CC=CS3)=CC(C4=CC=CC=C4)=C21
SynonymsSW-033291; SW033291; SW 033291
实验参考方法
In Vitro

In vitro activity: In Vaco-503 cells, SW033291 (2.5 μM) decreases cellular 15-PGDH enzyme activity by 85%. 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


Kinase Assay: For initial characterization of inhibition of 15-PGDH enzyme activity by SW033291, reactions were assembled with experiment specific concentrations of 15-PGDH enzyme, and experiment specific concentrations of SW033291, plus 150 μM NAD(+) and 25 μM PGE2 in reaction buffer (50 mM Tris-HCl, pH7.5, 0.01% Tween 20). The reaction mix was incubated for 15 mins at 25°C in an Envision Reader. Enzyme activity was determined by following generation of NADH as assayed by recording fluorescence at Ex/Em = 340 nM/485 nM every 30s for 3 mins, commencing immediately after addition of PGE2. IC50 values were calculated with GraphPad Prism 5 software using the sigmoidal dose-response function and plotted against SW033291 concentration.


Cell Assay: In CD45- bone marrow cells, SW033291 inhibited 15-PGDH, increased tissue levels of PGE2, and induced CXCL12 and SCF expression, which in turn accelerated homing of transplanted hematopoietic stem cells, generation of mature blood elements, as well as posttransplant recovery of normal blood counts. In addition, inhibiting 15-PGDH also stimulated cell proliferation after injury to colon or liver, and accelerated repair of these tissues.

In VivoIn mice receiving a bone marrow transplant, SW033291 (10 mg/kg, i.p.) promotes hematopoietic recovery. In mouse models of colon and liver injury, SW033291 (10 mg/kg, i.p.) reduces the levels of colitis-associated inflammatory cytokines, protects mice from colitis, and promotes liver regeneration.
Animal modelMice receiving a bone marrow transplant, and Mouse models of colon and liver injury
Formulation & DosageDissolved in 10% ethanol, 5% Cremaphor EL, 85% D5W; 10mg/kg; i.p. injection
References

Science. 2015 Jun 12;348(6240):aaa2340.