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

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.

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PFK-158

PFK-158 Chemical Structure

CAS No. : 1462249-75-7

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10 mM * 1 mL in DMSO
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Based on 11 publication(s) in Google Scholar

PFK-158 Related Antibodies

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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].

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

PFK-158 Related Antibodies

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].

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

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.
Appearance

Solid

Color

White to light yellow

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 : 50 mg/mL (152.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 98.88%

SDS (581 KB)

COA (245 KB) HNMR (167 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0461 mL 15.2304 mL 30.4609 mL 76.1522 mL
5 mM 0.6092 mL 3.0461 mL 6.0922 mL 15.2304 mL
10 mM 0.3046 mL 1.5230 mL 3.0461 mL 7.6152 mL
15 mM 0.2031 mL 1.0154 mL 2.0307 mL 5.0768 mL
20 mM 0.1523 mL 0.7615 mL 1.5230 mL 3.8076 mL
25 mM 0.1218 mL 0.6092 mL 1.2184 mL 3.0461 mL
30 mM 0.1015 mL 0.5077 mL 1.0154 mL 2.5384 mL
40 mM 0.0762 mL 0.3808 mL 0.7615 mL 1.9038 mL
50 mM 0.0609 mL 0.3046 mL 0.6092 mL 1.5230 mL
60 mM 0.0508 mL 0.2538 mL 0.5077 mL 1.2692 mL
80 mM 0.0381 mL 0.1904 mL 0.3808 mL 0.9519 mL
100 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7615 mL
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PFK-158 Related Classifications

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:

PFK-1581462249-75-7PFK158PFK 158AutophagyApoptosisPFKFB3apoptosisanti-tumorglycolysislactateanti-proliferativep-cPLA2LC3BIIInhibitorinhibitorinhibit

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