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SW033291 Dehydrogenase inhibitor

Cat.No.S7900

SW033291 is a selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with IC50 and Ki of 1.5 nM and 0.1 nM, respectively.
SW033291 Dehydrogenase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 412.59

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 412.59 Formula

C21H20N2OS3

Storage (From the date of receipt)
CAS No. 459147-39-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCCCS(=O)C1=C(C2=C(S1)N=C(C=C2C3=CC=CC=C3)C4=CC=CS4)N

Solubility

In vitro
Batch:

DMSO : 83 mg/mL ( (201.16 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
15-PGDH [1]
(Cell-free assay)
0.1 nM(Ki)
15-PGDH [1]
(Cell-free assay)
1.5 nM
In vitro

In Vaco-503 cells, SW033291 (2.5 μM) decreases cellular 15-PGDH enzyme activity by 85%.[1]

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

In mice receiving a bone marrow transplant, SW033291 (10 mg/kg, i.p.) promotes hematopoietic recovery. In mouse models of colon and liver injury, this compound reduces the levels of colitis-associated inflammatory cytokines, protects mice from colitis, and promotes liver regeneration. [1]

References

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