LAF-153
LAF-153 is a Methionine Aminopeptidase-2 (MetAP-2) inhibitor with human IC50 values of 0.074 μM and 0.16 μM.LAF-153 has a t-butyl group extending into the innermost portion of the MetAP-2 cleft, a lactam ring coordinated in the enzyme’s shallow surface pocket, and three hydroxyl groups coordinating to the two cobalt ions in the enzyme’s active site.
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- CAS. Nr.: 661482-39-9
- Formel: C18H32N2O7
- Molecular Weight:388.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
150 μM
Compound: 9c
|
Cytotoxicity in human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
Cytotoxicity in human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
|
[PMID: 30108762] |
| HepG2 | IC50 |
150 μM
Compound: 9c
|
Cytotoxicity in human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
Cytotoxicity in human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
|
[PMID: 30108762] |
| HL-60 | IC50 |
150 μM
Compound: 9c
|
Cytotoxicity in human HL60 cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
Cytotoxicity in human HL60 cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
|
[PMID: 30108762] |
| KB | IC50 |
62.6 μM
Compound: 9c
|
Cytotoxicity in human KB cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
Cytotoxicity in human KB cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
|
[PMID: 30108762] |
| Lu1 | IC50 |
23.4 μM
Compound: 9c
|
Cytotoxicity in human Lu1 cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
Cytotoxicity in human Lu1 cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
|
[PMID: 30108762] |
| MCF7 | IC50 |
23.4 μM
Compound: 9c
|
Cytotoxicity in human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
Cytotoxicity in human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by neutral red staining based colorimetry
|
[PMID: 30108762] |
In Vitro
LAF-153 reversibly binds to human MetAP-2 via coordination of its hydroxyl groups to the enzyme's cobalt ions, with its t-butyl group and lactam ring occupying distinct pockets in the enzyme cleft[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS. Nr. 661482-39-9
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Molecular Weight 388.46
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Formel C18H32N2O7
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SMILES
CC(C)(C)/C=C/[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC)C(N[C@@H]1C(NC[C@@H](CC1)O)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)