SW033291
SW033291 (CAS 459147-39-8) is a small molecule inhibitor targeting the prostaglandin-degrading enzyme 15-PGDH. It inhibits 15-PGDH activity non-competitively, displaying potent inhibition with an IC50 of 1.5 nM and an apparent dissociation constant (Ki app) of approximately 0.1 nM. Cellular assays in A549 cells demonstrate that SW033291 elevates prostaglandin E2 (PGE2) levels (EC50 ~75 nM). In vivo administration of SW033291 in mice significantly elevates tissue PGE2 concentrations, stimulates hematopoietic cytokine expression, expands hematopoietic stem and progenitor cell populations, and promotes neutrophil expansion. Thus, SW033291 represents a research tool for studying PGE2-related pathways in tissue regeneration and hematopoiesis.
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 412.59 |
| Cas No. | 459147-39-8 |
| Formula | C21H20N2OS3 |
| Solubility | insoluble in H2O; ≥10.13 mg/mL in EtOH with ultrasonic; ≥20.65 mg/mL in DMSO |
| Chemical Name | 2-(butylsulfinyl)-4-phenyl-6-(thiophen-2-yl)thieno[2,3-b]pyridin-3-amine |
| SDF | Download SDF |
| Canonical SMILES | NC1=C(S(CCCC)=O)SC2=NC(C3=CC=CS3)=CC(C4=CC=CC=C4)=C21 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Kinase experiment [1]: | |
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Activity assays of recombinant 15-PGDH protein |
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 experiment [1]: | |
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Cell lines |
CD45- bone marrow cells |
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Preparation method |
The solubility of this compound in DMSO is > 20.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.5 μM; 2 hrs |
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Applications |
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. |
| Animal experiment [1]: | |
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Animal models |
Mice receiving a bone marrow transplant and mouse models of colon and liver injury |
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Dosage form |
10 mg/kg; i.p.; b.i.d. |
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Applications |
In mice receiving a bone marrow transplant, SW033291 promoted hematopoietic recovery. In mouse models of colon and liver injury, SW033291 lowered the levels of colitis-associated inflammatory cytokines, protected mice from colitis, as well as facilitated liver regeneration. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [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. |
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Quality Control & MSDS
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Chemical structure
