1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. P-gp inhibitor 3

P-gp inhibitor 3 

Cat. No.: HY-144366
Handling Instructions

P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.

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

P-gp inhibitor 3 Chemical Structure

P-gp inhibitor 3 Chemical Structure

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Description

P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel[1].

IC50 & Target

P-glycoprotein

In Vitro

P-gp inhibitor 3 (compound 16) (10 μM; 72 hours) has appreciable cytotoxicity in KBV cancer cells, with relatively stronger MDR reversal ability[1].
P-gp inhibitor 3 (2.5, 5, 10 μM ; 3 hours) reverses tumor MDR by inhibiting the efflux function of P-gp[1].
P-gp inhibitor 3 (0.25, 0.5, 1 mM; 5 minutes) can significantly increase ATP consumption in a concentration-dependent manner (p<0.01)[1].
P-gp inhibitor 3 (10 μM; 24 hours) induces apoptosis in KBV cells in the G2/M phase[1].

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

Cell Cytotoxicity Assay

Cell Line: KBV cells[1]
Concentration: 10 μM
Incubation Time: 72 hours
Result: Showed appreciable cytotoxicity in KBV cancer cells, and exhibited relatively stronger MDR reversal ability.

Cell Cycle Analysis

Cell Line: KBV cells[1]
Concentration: 10 μM
Incubation Time: 24 hours
Result: Induced apoptosis in KBV cells in the G2/M phase.
In Vivo

P-gp inhibitor 3 (10 mg/kg; i.p., once a day, for 1 to 18 days) significantly enhances the anti-tumor activity of paclitaxel and the tumor suppression rate is 56.24%[1].

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

Animal Model: Nude mice xenograft tumor model (6-8 weeks old, BALB/c, male)[1]
Dosage: 10 mg/kg for P-gp inhibitor 3; 30 mg/kg for paclitaxel
Administration: i.p.; once a day (P-gp inhibitor 3), once every three days (paclitaxel); for 1 to 18 days
Result: Significantly enhanced the anti-tumor activity of paclitaxel and the tumor suppression rate was 56.24%.
Molecular Weight

782.06

Formula

C48H67N3O6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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P-gp inhibitor 3
Cat. No.:
HY-144366
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