F1386-0303
F1386-0303 is a highly selective MAP4K4 inhibitor with an IC50 of 34 nM against human targets. F1386-0303 exerts cardiomyocyte protective and function-preserving effects through mechanisms such as alleviating oxidative stress, inhibiting caspases, and maintaining mitochondrial membrane potential, while it does not interfere with the activity of Doxorubicin (HY-15142A) in cancer cells. F1386-0303 is rapidly cleared and has no bioavailability in mice, but it is well-suited as a tool compound for target validation. F1386-0303 can be applied to studies related to cardiac ischemia-reperfusion injury, Doxorubicin-induced cardiotoxicity, myocardial infarction and other related conditions.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 287177-12-2
- 分子式: C18H13N3O
- 分子量:287.32
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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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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Help & FAQs
MAP4K アイソフォーム固有の製品をすべて表示
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生物活性
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MAP4K4 34 nM (IC50) |
F1386-0303 (5 μM) protects iCell human iPSC-derived cardiomyocytes from oxidative stress-induced death at 5 μM, matching the protective effect of MAP4K4 gene silencing[1].
F1386-0303 (10 μM; 1 h pre-incubation prior to 24 h oxidative stress exposure) exhibits protection to vCor.4U human iPSC-derived ventricular cardiomyocytes against cell death induced by high concentrations of H2O2 or Menadione (HY-B0332)[1].
F1386-0303 (10 μM; 1 h pre-incubation before DOX treatment, assessed at 24 h, 48 h post-DOX exposure) protects rat H9c2 cardiomyocytes from DOX-induced cell death, with a pEC50 of 5.8, and reduces the cells' sensitivity to DOX by more than threefold when used at 10 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human iPSC-derived ventricular cardiomyocytes (vCor.4U cells)
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Concentration:10 μM
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Incubation Time:1 h pre-incubation prior to 24 h oxidative stress exposure
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Result:Provided near-complete protection against cell death induced by up to 200 μM H2O2 or 45 μM menadione.
Preserved cell viability and reduced cardiac troponin release at the tested concentration.
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Cell Line:rat H9c2 cardiomyocytes
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Concentration:10 μM
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Incubation Time:1 h pre-incubation before DOX treatment; assessed at 24 h, 48 h post-DOX exposure
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Result:Reduced the cardiomyocytes’ sensitivity to DOX by more than threefold at both 24 h and 48 h, shifting the pIC50 for DOX from 6.6 to <6 (P < 0.05).
Exhibited a pEC50 of 5.8 for protection against 333 nM DOX at 48 h.
化学情報
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CAS 番号 287177-12-2
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分子量 287.32
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分子式 C18H13N3O
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SMILES
O=C1N=CNC2=C1C(=CN2C=3C=CC=CC3)C=4C=CC=CC4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
参考文献
[1]. Fiedler LR, et al. MAP4K4 Inhibition Promotes Survival of Human Stem Cell-Derived Cardiomyocytes and Reduces Infarct Size In Vivo. Cell Stem Cell. 2019;24(4):579-591.e12. [Content Brief]
[2]. Golforoush PA, et al. Selective protection of human cardiomyocytes from anthracycline cardiotoxicity by small molecule inhibitors of MAP4K4. Sci Rep. 2020;10(1):12060. Published 2020 Jul 21. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
F1386-0303 関連分類
HY-W207224 関連分類
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