1. Autophagy
    Apoptosis
  2. Autophagy
    Apoptosis
  3. PFK-158

PFK-158 

Cat. No.: HY-12203 Purity: 98.85%
Handling Instructions

PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.

For research use only. We do not sell to patients.

PFK-158 Chemical Structure

PFK-158 Chemical Structure

CAS No. : 1462249-75-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
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50 mg USD 290 In-stock
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100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria[1][2][3].

IC50 & Target

IC50 : 137 nM (PFKFB3)[1][3]

In Vitro

PFK-158 (10 µM ; 24 hours; OV2008 and C13 cells) combined with Carboplatin (CBPt; 77-453 μM) results in significant increase in apoptosis in C13 (45%) and OV2008 cells (24.6%)[1].
PFK-158 (0-10 µM ; 24 hours; C13 and HeyA8MDR cells) treatment results in a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels[1].
PFK-158 (10 μM; 24 hours) has synergistic anti-proliferative effects in vitro when combined with Cisplatin in C13 and HeyA8MDR cells compared to OV2008 and HeyA8, respectively[1].
PFK-158 (0‐10 μM; 24 h) treatment shows a dose-dependent downregulation of p62/SQSTM1 and upregulation of LC3BII, two markers of autophagy induction, in both C13 and HeyA8MDR cells. PFK-158 treatment also reduces the numbers of LDs[1].

Apoptosis Analysis[1]

Cell Line: OV2008 and C13 cells
Concentration: 10 µM
Incubation Time: 24 hours
Result: Combined with Carboplatin (CBPt) treatment resulted in significant increase in apoptosis.

Western Blot Analysis[1]

Cell Line: C13 and HeyA8MDR cells
Concentration: 0 µM, 5 µM, 10 µM
Incubation Time: 24 hours
Result: Demonstrated a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels.
In Vivo

PFK-158 (15 mg/kg; intraperitoneal injection; once a week; for 4 weeks; female athymic nude mice) plus CBPt (51 mg/kg) treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model[1].

Animal Model: Female athymic nude mice (nu/nu) (5-6 weeks old) injected with HeyA8MDR cells[1]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection; once a week; for 4 weeks
Result: A marked reduction of tumor growth was observed in the combination treatment.
Clinical Trial
Molecular Weight

328.29

Formula

C₁₈H₁₁F₃N₂O

CAS No.

1462249-75-7

SMILES

O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC(C(F)(F)F)=CC=C3C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (91.38 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0461 mL 15.2304 mL 30.4609 mL
5 mM 0.6092 mL 3.0461 mL 6.0922 mL
10 mM 0.3046 mL 1.5230 mL 3.0461 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2 mg/mL (6.09 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (6.09 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (6.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PFK-158PFK158PFK 158AutophagyApoptosisPFKFB3apoptosisanti-tumorglycolysislactateanti-proliferativep-cPLA2LC3BIIInhibitorinhibitorinhibit

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