2. Membrane Transporter/Ion Channel Apoptosis
  3. P-glycoprotein Apoptosis
  4. ABCB1-IN-3

ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrug resistance (MDR) to Paclitaxel in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with Paclitaxel exhibits potent tumor suppression in vivo without generating toxicity.

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ABCB1-IN-3 Chemical Structure

ABCB1-IN-3 Chemical Structure

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ABCB1-IN-3 Related Antibodies

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Description

ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrug resistance (MDR) to Paclitaxel in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with Paclitaxel exhibits potent tumor suppression in vivo without generating toxicity[1].

In Vitro

ABCB1-IN-3 (72 h) significantly increases the sensitivity of ABCB1-mediated MDR SW620/AD300 cells to Paclitaxel (IC50 = 15.33 nM) and hardly shows toxicity even at a high concentration of 20 μM when used alone[1].
ABCB1-IN-3 (5-20 μM; 24 h) distinctly enhances the arresting effect of Paclitaxel on the SW620/AD300 cell cycle, thereby inhibiting their proliferation[1].
ABCB1-IN-3 (5-20 μM; 7 d) combined with Paclitaxel inhibits the cell colony formation, exhibits great reversal activity against Paclitaxel resistance cells[1].
ABCB1-IN-3 (5-20 μM; 24 h) is confirmed to directly bind to ABCB1 to inhibit efflux function, reducing cellular efflux and ensuring stable intracellular concentration of Paclitaxel without affecting ABCB1 normal expression[1].

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

ABCB1-IN-3 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: SW620/AD300 cells
Concentration: 5, 10, 20 μM
Incubation Time: 24 h
Result: Induced more cells to stay in the G2/M phase combined with Paclitaxel.

Cell Proliferation Assay[1]

Cell Line: SW620/AD300 cells
Concentration: 5, 10, 20 μM
Incubation Time: 7 days
Result: Significantly inhibited the cell colony formation of SW620/AD300 cells combined with Paclitaxel.
In Vivo

ABCB1-IN-3 (50 mg/kg; i.g.; once every 3 days for 14 days) combined with Paclitaxel exhibits potent tumor suppression in male BALB/c nude mice injected with SW620/AD300 cells without generating toxicity, but shows week tumor suppression when used alone[1].

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

Animal Model: Male BALB/c nude mice (18-22 g, aged 6-7 weeks, 1×107 SW620/AD300 cells were inoculated subcutaneously into the forelimb of each mouse.)[1]
Dosage: 50 mg/kg
Administration: Intragastric gavage (i.g.); once every 3 days for 14 days
Result: The tumor volume and weight had little difference when used alone, and remarkable reduced when combined with Paclitaxel, showing better antitumor activity.
The cell apoptosis in tumor tissues was more remarkable when used with Paclitaxel, resulted in more massive degeneration and necrosis than in vehicle or mono-therapy groups.
Showed no significant loss of body weight.
Molecular Weight

288.34

Formula

C19H16N2O
SMILES

CN1C2=CC=CC=C2C3=C1C(C4=CC=C(OC)C=C4)=NC=C3
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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ABCB1-IN-3 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:

ABCB1-IN-3P-glycoproteinApoptosisP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243apoptosisABCB1 inhibitoranti-tumormultidrug resistanceMDRInhibitorinhibitorinhibit

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