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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 287177-12-2
- Fòrmula: C18H13N3O
- Peso molecular:287.32
-
Almacenamiento:
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]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas MAP4K
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
MAP4K4 34 nM (IC50) |
In Vitro
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.
-
Cell Line:Human iPSC-derived ventricular cardiomyocytes (vCor.4U cells)
-
Concentration:10 μM
-
Incubation Time:1 h pre-incubation prior to 24 h oxidative stress exposure
-
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.
-
Cell Line:rat H9c2 cardiomyocytes
-
Concentration:10 μM
-
Incubation Time:1 h pre-incubation before DOX treatment; assessed at 24 h, 48 h post-DOX exposure
-
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.
Parmacokinetics
Chemical Information
-
No. CAS 287177-12-2
-
Peso molecular 287.32
-
Fòrmula C18H13N3O
-
SMILES
O=C1N=CNC2=C1C(=CN2C=3C=CC=CC3)C=4C=CC=CC4
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
F1386-0303 Related Classifications
HY-W207224 Related Classifications
Powered by Bioz
Keywords