2. MAPK/ERK Pathway
  3. MAP4K
  4. 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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F1386-0303

F1386-0303 Chemical Structure

CAS No. : 287177-12-2

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F1386-0303 Related Antibodies

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

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Description

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].

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.

F1386-0303 Related Antibodies

Cell Viability Assay[1]

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 Viability Assay[2]

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
Species Dose Route CL T1/2 Cmax Vd AUCinf Tmax
Mice[1] 1 mg/kg i.v. 5.33 L/h/kg 0.1 h 3262 nM 1.05 L/kg / /
Mice[1] 50 mg/kg p.o. / 3.7 h 295 nM / 2162 nM·h 1.00 h
Molecular Weight

287.32

Formula

C18H13N3O
CAS No.
SMILES

O=C1N=CNC2=C1C(=CN2C=3C=CC=CC3)C=4C=CC=CC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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F1386-0303 Related Classifications

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  • 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:

F1386-0303287177-12-2MAP4KMAPK Kinase Kinase KinaseMAP4K4human THP1 acute monocytic leukemia cellsmyocardial infarctioniCell human iPSC-derived cardiomyocytesMINK1/MAP4K6HEK293TvCor.4U human iPSC-derived ventricular cardiomyocytesTNIK/MAP4K7cardiac ischemia-reperfusion injuryrat H9c2 cardiomyocytesInhibitorinhibitorinhibit

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