2. Anti-infection
  3. Antibiotic Fungal
  4. Frenolicin B

Frenolicin B is a covalent enzyme inhibitor and an orally active antiparasitic agent, with an IC50 of 0.2 μM against human Prx1. Frenolicin B selectively inhibits Glutaredoxin 3 via covalent modification of the active-site cysteines Cys159/Cys261. Frenolicin B selectively inhibits Peroxiredoxin 1 via covalent modification of the active-site cysteines Cys83/Cys173. Frenolicin B can be used in research related to colon cancer, breast cancer, lung cancer and malaria.

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Frenolicin B

Frenolicin B Chemical Structure

CAS No. : 68930-68-7

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Frenolicin B Related Antibodies

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Description

Frenolicin B is a covalent enzyme inhibitor and an orally active antiparasitic agent, with an IC50 of 0.2 μM against human Prx1. Frenolicin B selectively inhibits Glutaredoxin 3 via covalent modification of the active-site cysteines Cys159/Cys261. Frenolicin B selectively inhibits Peroxiredoxin 1 via covalent modification of the active-site cysteines Cys83/Cys173. Frenolicin B can be used in research related to colon cancer, breast cancer, lung cancer and malaria[1][2].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.28 μM
Compound: 7
Cytotoxicity against human A549 cells after 2 days by MTT assay
Cytotoxicity against human A549 cells after 2 days by MTT assay
[PMID: 23944931]
MDA-MB-468 IC50
0.06 μM
Compound: 3, frenolicin
Cytotoxicity against human MDA468 cells expressing AKT
Cytotoxicity against human MDA468 cells expressing AKT
[PMID: 19309081]
In Vitro

Frenolicin B (0.032-30 μM; 15 min room temperature incubation) is a potent, selective inhibitor of purified recombinant human Prx1, with an apparent IC50 of 0.2 μM, inhibition kinetics parameters kᵢ = 0.65 μM and kᵢₙₐcₜ = 0.02 min-1, and ~20-fold higher potency against Prx1 than Prx2[1].
Frenolicin B (1-10 μM; 1 h pre-incubation) directly engages Prx1 and Grx3 in HCT116 colon cancer cell lysates and with purified recombinant proteins, as demonstrated by competitive binding with an active biotinylated probe[1].
Frenolicin B (200 μM; 2 h 37 °C incubation) covalently modifies the active site cysteines Cys83/Cys173 of purified recombinant human Prx1 and Cys159/Cys261 of purified recombinant human Grx3, which are essential for ligand binding[1].
Frenolicin B (2 μM; 12 h post-transfection incubation) inhibits cap-dependent translation in a 4E-BP1-dependent manner in HCT116 human colon cancer cells[1].
Frenolicin B (72 h incubation) exhibits preferential cytotoxicity against human cancer cell lines (colon, breast, lung) with IC50 values ranging from 50 nM to 130 nM after 72 h incubation, compared to non-malignant cells with higher IC50 values[1].
Frenolicin B (2 μM; 3 h incubation) increases extracellular H2O2 levels and at 2 μM for 1 h increases intracellular ROS levels in HCT116 human colon cancer cells, with ROS induction reversible by NAC pre-treatment[1].
Frenolicin B (0.2-2 μM; 12 h incubation) dose-dependently inhibits mTORC1-mediated 4E-BP1 phosphorylation at T37/46, S65, and T70, and induces apoptosis (cleaved PARP) in HCT116 human colon cancer cells, with these effects reversed by NAC pre-treatment[1].
Frenolicin B (0.002-80 μM; 72 h) inhibits in vitro growth of Plasmodium falciparum HB3, Dd2, and 7G8 strains with IC50 values of 600 ± 100 nM, 800 ± 200 nM, and 800 ± 150 nM, respectively, and incubation with selected human cytochrome P450 enzymes either maintains or improves its antiparasitic potency[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Frenolicin B Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116 human colon cancer cell; purified recombinant human Prx1/Grx3 proteins
Concentration: 1-10 μM (Frenolicin B, HCT116 lysate pre-incubation); 1-2 μM (probe 1)
Incubation Time: 1 h (Frenolicin B pre-incubation with HCT116 lysates); 1 h (probe 1 incubation)
Result: Competed with active probe 1 for binding to Prx1 and Grx3 in HCT116 lysates.
Confirmed direct binding to pure recombinant Prx1 and Grx3 via probe 1 labeling.

Western Blot Analysis[1]

Cell Line: HCT116 human colon cancer cells
Concentration: 0.2-2 μM; 400 μM (NAC pre-treatment)
Incubation Time: 12 h (phosphorylation analysis); 6 h (NAC reversal analysis); 1 h (NAC pre-treatment)
Result: Dose-dependently inhibited phosphorylation of 4E-BP1 at T37/46, S65, and T70.
Induced cleaved PARP (apoptotic marker).
Had inhibition of 4E-BP1 phosphorylation and induction of cleaved PARP reversed by pre-treatment with NAC.
In Vivo

Frenolicin B (10-63 mg/kg; p.o.; daily; 4 days) exhibits dose-dependent oral activity against Plasmodium berghei in CD1 mice, with the highest tested dose of 63 mg/kg daily for 4 days reducing mean parasitemia to 15 ± 16% and curing 2/5 mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD1 mice (8-week-old)[2]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg; 63 mg/kg
Administration: p.o.; daily; 4 days
Result: Reduced mean parasitemia to 39 % and cured 0/5 mice at 10 mg/kg.
Reduced mean parasitemia to 37 % and cured 0/5 mice at 20 mg/kg.
Reduced mean parasitemia to 33 % and cured 1/5 mice at 40 mg/kg.
Reduced mean parasitemia to 15% (a >50% reduction relative to vehicle control) and cured 2/5 mice at 63 mg/kg.
Molecular Weight

328.32

Formula

C18H16O6
CAS No.
SMILES

O=C1C2=C(C(C3=C(O)C=CC=C31)=O)[C@H](O[C@@]4([H])[C@]2([H])OC(C4)=O)CCC
Structure Classification
Initial Source

S. roseofulvus.
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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Frenolicin B Related Classifications

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Help & FAQs
  • 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:

Frenolicin B68930-68-7AntibioticFungalPlasmodium bergheiGlutaredoxin 3HCT116 human colon cancer cellsPrx1Eimeria tenellaPlasmodium falciparumPeroxiredoxin 1mTORC1/4E-BP1 signalingCD1 micecytochrome P450 enzymesInhibitorinhibitorinhibit

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