2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. P-gb-IN-1

P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells.

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P-gb-IN-1

P-gb-IN-1 Chemical Structure

CAS No. : 2632874-49-6

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Based on 1 publication(s) in Google Scholar

P-gb-IN-1 Related Antibodies

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Description

P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells[1].

Cellular Effect
Cell Line Type Value Description References
NCI/ADR-RES IC50
0.09 μM
Compound: Cpd III-8
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
[PMID: 37229830]
NCI/ADR-RES IC50
0.09 μM
Compound: Cpd III-8
Sensitization of doxorubicin-induced antitumor activity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Sensitization of doxorubicin-induced antitumor activity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
[PMID: 37229830]
NCI/ADR-RES IC50
0.36 μM
Compound: Cpd III-8
Sensitization of daunorubicin-induced antitumor activity against human MCF7ADR cells assessed as daunorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Sensitization of daunorubicin-induced antitumor activity against human MCF7ADR cells assessed as daunorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
[PMID: 37229830]
NCI/ADR-RES IC50
0.37 μM
Compound: Cpd III-8
Sensitization of paclitaxel-induced antitumor activity against human MCF7ADR cells assessed as paclitaxel IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Sensitization of paclitaxel-induced antitumor activity against human MCF7ADR cells assessed as paclitaxel IC50 at 5 uM incubated for 48 hrs by CCK8 assay
[PMID: 37229830]
NCI/ADR-RES IC50
0.53 μM
Compound: Cpd III-8
Sensitization of vincristine-induced antitumor activity against human MCF7ADR cells assessed as vincristine IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Sensitization of vincristine-induced antitumor activity against human MCF7ADR cells assessed as vincristine IC50 at 5 uM incubated for 48 hrs by CCK8 assay
[PMID: 37229830]
NCI/ADR-RES IC50
15.5 μM
Compound: Cpd III-8
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 0.1 uM incubated for 48 hrs by CCK8 assay
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 0.1 uM incubated for 48 hrs by CCK8 assay
[PMID: 37229830]
NCI/ADR-RES IC50
5.78 μM
Compound: Cpd III-8
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 0.5 uM incubated for 48 hrs by CCK8 assay
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 0.5 uM incubated for 48 hrs by CCK8 assay
[PMID: 37229830]
Molecular Weight

512.55

Formula

C30H28N2O6
CAS No.
SMILES

O=C(NC1=CC=C(C2=CC=C(C(N3CCC(C=C(OC)C(OC)=C4)=C4C3)=O)O2)C=C1)C5=CC=C(OC)C=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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P-gb-IN-1 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:

P-gb-IN-12632874-49-6P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD2432,5-disubstituted furanH-bondAsn 721Met 986MCF-7ADRInhibitorinhibitorinhibit

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P-gb-IN-1
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HY-149360
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