287177-12-2
Chemical Structure
F1386-0303
- CAS No.: 287177-12-2
- Formula:C18H13N3O
- Molecular Weight:287.32
IUPAC Name: 5,7-diphenyl-1,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
InChIKey: YTLWLZPZXNOVGS-UHFFFAOYSA-N
SMILES: O=C1N=CNC2=C1C(=CN2C=3C=CC=CC3)C=4C=CC=CC4
Biological Activity: 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[1][2][3].
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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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References
- [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]
- [3]. Eeda V, et al. Catalyst-Free and Scalable Process for Synthesis of Novel MAP4K4 Inhibitor DMX-5804 and Its Glyco-Conjugates[J]. Organic Process Research & Development, 2021, 25(7): 1658-1663.
