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製品番号: HY-182274

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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 番号: 3106606-60-1
分子式: C₂₅H₂₁NO₅
分子量:415.44

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

DM245 構造式

CAS 番号: 3106606-60-1

容量

価格（税別）

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数量

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

IC₅₀ & Target

p-STAT3

Acyltransferase アイソフォーム固有の製品をすべて表示 :

STAT アイソフォーム固有の製品をすべて表示 :

体外実験

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.

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.

化学情報

CAS 番号 3106606-60-1
分子量 415.44
分子式 C₂₅H₂₁NO₅
SMILES

O=C(O)C(NCC1=CC=C(OC(C(C2=CC=C3C=CC=CC3=C2)=O)=C4C(C)C)C4=C1)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Morgan D, et al. Development and Evaluation of Benzofuran Oxoacetic Acid Compounds as EPAC1 Activators. J Med Chem. 2026;69(6):6706-6735. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
化学情報
純度とドキュメンテーション
参考文献

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DM245

Acyltransferase アイソフォーム固有の製品をすべて表示

STAT アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

DM245 関連分類

HY-182274 関連分類