LL-37(17-32)
Based on 1 Customer Validation
LL-37 (17-32) is an ABCG2 inhibitor. LL-37 (17-32) binds to ABCG2, inhibits its transport activity in a non-competitive manner, and downregulates ABCG2 protein expression via lysosomal degradation. LL-37 (17-32) increases the accumulation of Mitoxantrone (HY-13502) in cancer cells overexpressing ABCG2, thereby reversing mitoxantrone resistance. LL-37 (17-32) can be used in the research of multidrug-resistant cancers.
For research use only. We do not sell to patients.
- Purity: 96.71%
- CAS No.: 717919-61-4
- Formula: C95H161N29O21
- Molecular Weight:2045.48
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
LL-37 (17-32) (2-10 μM; 72 h) specifically reverses ABCG2-mediated multidrug resistance in MCF-7 FLV1000 cells and ABCG2-transfected HEK293 cells; at a concentration of 10 μM, it reduces the resistance fold of mitoxantrone to 43 and 5.4, respectively, and does not affect the cytotoxicity of non-ABCG2 substrate drugs or the viability of parental cells at effective concentrations[1].
LL-37 (17-32) (10-40 μM; 1.5 h) inhibits ABCG2-mediated pheophorbide A efflux in MCF-7 FLV1000 cells in a concentration-dependent manner and increases intracellular substrate retention[1].
LL-37 (17-32) (10-40 μM; 2 h) increases mitoxantrone accumulation in ABCG2-overexpressing MCF-7 FLV1000 cells in a concentration-dependent manner, but exerts no such effect on parental MCF-7 cells[1].
LL-37 (17-32) (10-40 μM; 55 min) enhances the binding of 5D3 antibody to ABCG2 in MCF-7 FLV1000 cells in a concentration-dependent manner, indicating a direct interaction with this transporter[1].
LL-37 (17-32) (0.4-50 μM; 45 min) inhibits vanadate-sensitive ABCG2 ATPase activity in crude membranes of ABCG2-expressing High Five insect cells in a concentration-dependent manner[1].
LL-37 (17-32) (5-20 μM; 24 h) downregulates the expression of ABCG2 protein in MCF-7 FLV1000 cells in a concentration-dependent manner via the lysosomal degradation pathway, without altering ABCG2 mRNA levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human breast cancer MCF-7 (parental), MCF-7 FLV1000 (ABCG2-overexpressing), human embryonic kidney HEK293 pcDNA3-transfected, HEK293 ABCG2-transfected
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Concentration:2 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:Reduced the IC50 of mitoxantrone from 2.116 μM to 0.821 μM in MCF-7 FLV1000 cells at 5 μM, decreasing fold-resistance from 218 to 85.
Dropped the mitoxantrone IC50 further to 0.415 μM in MCF-7 FLV1000 cells at 10 μM, with fold-resistance reduced to 43.
Reduced the mitoxantrone IC50 from 45.8 nM to 10.5 nM in HEK293 ABCG2-transfected cells at 5 μM, decreasing fold-resistance from 59 to 13.
Reduced the mitoxantrone IC50 to 4.2 nM in HEK293 ABCG2-transfected cells at 10 μM, with fold-resistance decreased to 5.4.
Did not significantly alter mitoxantrone cytotoxicity in parental MCF-7 or HEK293 pcDNA3-transfected cells.
Did not affect cisplatin cytotoxicity in any tested cell line.
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Cell Line:human breast cancer MCF-7 FLV1000 (ABCG2-overexpressing)
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:24 h
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Result:Reduced ABCG2 protein levels in a concentration-dependent manner: 5 μM caused a small reduction, 10 μM caused a significant reduction, and 20 μM caused the greatest reduction.
Had its ABCG2 protein downregulation reversed by co-treatment with leupeptin and pepstatin.
Caused no change in ABCG2 mRNA levels at any tested concentration via quantitative real-time RT-PCR.
Chemical Information
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CAS No. 717919-61-4
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Appearance Solid
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Molecular Weight 2045.48
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Formula C95H161N29O21
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Color White to off-white
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Sequence
Phe-Lys-Arg-Ile-Val-Gln-Arg-Ile-Lys-Asp-Phe-Leu-Arg-Asn-Leu-Val
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Sequence Shortening
FKRIVQRIKDFLRNLV
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (263 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)