2. Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling
  3. Acyltransferase STAT
  4. 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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DM245

DM245 Chemical Structure

CAS No. : 3106606-60-1

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DM245 Related Antibodies

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ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

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STAT3 STAT5 STAT6 STAT1

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Description

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[1].

IC50 & Target

p-STAT3

 

In Vitro

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.

DM245 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: normal human lung fibroblasts (Lonza, CC-512)
Concentration: logarithmic concentration range (same as fibroblast-to-myofibroblast transition assay)
Incubation Time: 72 h
Result: Showed minimal change in nuclear counts under matched conditions, with shallow or nonmeasurable cytotoxic concentration-response curves within the tested range.
Molecular Weight

415.44

Formula

C25H21NO5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DM245 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DM2453106606-60-1DM 245DM-245AcyltransferaseSTATDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseTGF-β1Rap1-GTPPKAfibroblast-to-myofibroblast transitionendothelial cellsnormal human lung fibroblastsEPAC1STAT3 phosphorylationEPAC2IL-6/IL-6RαInhibitorinhibitorinhibit

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