DM245
DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor with a target pIC50 of 4.801. DM245 activates EPAC1 to increase Rap1-GTP levels, with no activation of EPAC2 or PKA. DM245 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM245 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing αSMA and Collagen I levels. DM245 exhibits minimal cytotoxicity in normal human lung fibroblasts, with negligible loss of intact nuclei after 72 h exposure.
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- CAS No.: 3106606-60-1
- 화학식: C25H21NO5
- 분자량:415.44
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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p-STAT3 |
DM245 binds to the EPAC1 CNBD with a pIC50 of 4.80, indicating micromolar affinity for the EPAC1 cyclic nucleotide-binding domain[1].
DM245 (100 μM) significantly activates the EPAC1-Rap1 signaling pathway in EPAC1-transfected U2OS cells[1].
DM245 (1 μM) significantly attenuates IL-6/IL-6Rα-induced STAT3 phosphorylation in HUVECs[1].
DM245 (logarithmic concentration range; 1 h pretreatment, 72 h TGF-β1 stimulation) inhibits TGF-β1-induced fibroblast-to-myofibroblast transition in normal human lung fibroblasts, with midmicromolar potency for both αSMA (pIC50 = 4.58) and Collagen I (pIC50 = 4.34) suppression[1].
DM245 (logarithmic concentration range; 72 h) exhibits minimal cytotoxicity in normal human lung fibroblasts at concentrations effective for suppressing TGF-β1-induced fibroblast-to-myofibroblast transition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:normal human lung fibroblasts (Lonza, CC-512)
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Concentration:logarithmic concentration range (same as fibroblast-to-myofibroblast transition assay)
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Incubation Time:72 h
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Result:Showed minimal change in nuclear counts under matched conditions, with shallow or nonmeasurable cytotoxic concentration-response curves within the tested range.
Chemical Information
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CAS No. 3106606-60-1
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분자량 415.44
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화학식 C25H21NO5
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SMILES
O=C(O)C(NCC1=CC=C(OC(C(C2=CC=C3C=CC=CC3=C2)=O)=C4C(C)C)C4=C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DM245 Related Classifications
HY-182274 Related Classifications
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