2. JAK/STAT Signaling Stem Cell/Wnt Metabolic Enzyme/Protease
  3. STAT Acyltransferase
  4. DM243

DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769 for EPAC1. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts.

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DM243

DM243 Chemical Structure

CAS No. : 3106606-59-8

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DM243 Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

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Description

DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769 for EPAC1. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts[1].

IC50 & Target

p-STAT3

 

In Vitro

DM243 (log concentration range; 4 h) binds to the cyclic nucleotide-binding domains of both EPAC1 and EPAC2, with a modest preference for EPAC1, as indicated by pIC50 values of 4.769 and 4.436, respectively[1].
DM243 (100 μM) potently activates the EPAC1-Rap1 signaling pathway in EPAC1-transfected U2OS cells, significantly increasing Rap1-GTP levels at a concentration of 100 μM[1].
DM243 (1 μM) significantly attenuates IL-6/IL-6Rα-induced STAT3 phosphorylation in human umbilical vascular endothelial cells, reducing the normalized phospho-STAT3 signal to a greater extent than other tested analogues[1].
DM243 (logarithmic concentration range; 1 h pretreatment, 72 h) suppresses TGF-β1-induced fibroblast-to-myofibroblast transition in normal human lung fibroblasts, with midmicromolar potencies (pIC50 = 4.34 for αSMA, pIC50 = 4.40 for Collagen I)[1].
DM243 (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, with only a shallow reduction in nuclear counts observed across the tested range[1].
DM243 (1 μM) does not activate PKA in EPAC1-transfected U2OS cells, as shown by the absence of detectable phospho-VASP (Ser157) signal[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DM243 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: normal human lung fibroblasts
Concentration: logarithmic concentration range
Incubation Time: 72 h
Result: Showed minimal change in nuclear counts under the tested conditions.
Exhibited a shallow or nonmeasurable cytotoxic concentration-response curve.
Indicated low cytotoxicity at efficacious concentrations.
Molecular Weight

395.41

Formula

C22H21NO6
CAS No.
SMILES

O=C(O)C(NCC1=CC=C(OC(C(C2=CC=CC=C2OC)=O)=C3C(C)C)C3=C1)=O
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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DM243 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:

DM2433106606-59-8DM 243DM-243STATAcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferasefibroblast-to-myofibroblast transitionα-smooth muscle actinEPAC2endothelial cellsCollagen IRap1EPAC1TGF-β1PKASTAT3Inhibitorinhibitorinhibit

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