1. PI3K/Akt/mTOR Metabolic Enzyme/Protease Anti-infection Apoptosis
  2. PTEN Phosphatase Parasite Apoptosis
  3. bpV(phen)

bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.

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bpV(phen) Chemical Structure

bpV(phen) Chemical Structure

CAS No. : 42494-73-5

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Description

bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5].

IC50 & Target

IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B)[3]
Parasite Leishmania[2]
Apoptosis[1]

In Vitro

bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment causes a further decrease of cell viability in H/R-injured H9c2 cells[1].
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment increases the apoptosis of H/R-injured H9c2 cells[1].
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment significantly promotes the accumulation of cytoplasmic Cytochrome C in H/R-injured H9c2 cells[1].
After stimulation of bpV(phen), PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy is inhibited[1].
bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation[4].

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

Cell Viability Assay[1]

Cell Line: Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration: 5 μM
Incubation Time: 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result: Caused a further decrease of cell viability.

Apoptosis Analysis[1]

Cell Line: Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration: 5 μM
Incubation Time: 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result: Increased the apoptosis of H/R-injured H9c2 cells.

Western Blot Analysis[1]

Cell Line: Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration: 5 μM
Incubation Time: 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result: Showed an increased release of Cytochrome C.
In Vivo

bpV(phen) (5 mg/kg; intraperitoneal injection; daily; for 38 days; male BALB/c nude (nu/nu) athymic mice) treatment causes a significant reduction in average tumor volume[1].

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

Animal Model: Male BALB/c nude (nu/nu) athymic mice (6-7 weeks old) injected with PC-3 cells[2]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; daily; for 38 days
Result: Caused a significant reduction in average tumor volume.
Molecular Weight

350.24

Formula

C12H8KN2O5V

CAS No.
SMILES

O=[V+3]12([N]3=CC=C4)([O-][O-]1)([O-][O-]2)[N]5=C6C3=C4C=CC6=CC=C5.[K+]

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Please store the product under the recommended conditions in the Certificate of Analysis.

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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.

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bpV(phen)
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HY-136065
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