8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate is an irreversible CYP2A6 inhibitor with IC50s of 8.64 μM and 22.3 μM with pre-incubation and co-incubaition, respectively. 8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate also inhibits MAO-A and MAO-B with IC50s of 60.2 and 38.6 μM, respectively.
For research use only. We do not sell to patients.
- CAS No.: 67667-71-4
- Formula: C21H26O8
- Molecular Weight:406.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
IC50: 8.64 μM (CYP2A6, pre-incubation), 22.3 μM (CYP2A6, co-incubation), 38.6 μM (MAO-B), 60.2 μM(MAO-A)[1]
Ki: 15.1 μM (CYP2A6), 27.2 μM (MAO-B), 60.2 μM (MAO-A)[1]
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
5.2 μM
Compound: 5
|
Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay
Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay
|
[PMID: 22850207] |
| MCF7 | IC50 |
7.7 μM
Compound: 7
|
Antiproliferative activity against human MCF7 cells for 72 hrs by cyquant assay
Antiproliferative activity against human MCF7 cells for 72 hrs by cyquant assay
|
[PMID: 26331426] |
| MDA-MB-231 | IC50 |
5.2 μM
Compound: 7
|
Antiproliferative activity against human MDA-MB-231 cells for 72 hrs by cyquant assay
Antiproliferative activity against human MDA-MB-231 cells for 72 hrs by cyquant assay
|
[PMID: 26331426] |
| NIH3T3 | IC50 |
7.1 μM
Compound: 7
|
Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by cyquant cells
Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by cyquant cells
|
[PMID: 26331426] |
| RAW264.7 | IC50 |
6.6 μM
Compound: 5
|
Antiinflammatory activity against LPS-induced NO production in mouse RAW264.7 cells assessed as reduction in nitrite level preincubated for 15 mins prior to LPS treatment by Griess method
Antiinflammatory activity against LPS-induced NO production in mouse RAW264.7 cells assessed as reduction in nitrite level preincubated for 15 mins prior to LPS treatment by Griess method
|
[PMID: 22850207] |
| SF-295 | IC50 |
9.1 μM
Compound: 7
|
Antiproliferative activity against human SF295 cells for 72 hrs by cyquant assay
Antiproliferative activity against human SF295 cells for 72 hrs by cyquant assay
|
[PMID: 26331426] |
| U-251 | IC50 |
2.6 μM
Compound: 7
|
Antiproliferative activity against human U251MG cells for 72 hrs by cyquant assay
Antiproliferative activity against human U251MG cells for 72 hrs by cyquant assay
|
[PMID: 26331426] |
| U-373MG ATCC | IC50 |
8.3 μM
Compound: 7
|
Antiproliferative activity against human U373MG cells for 72 hrs by cyquant assay
Antiproliferative activity against human U373MG cells for 72 hrs by cyquant assay
|
[PMID: 26331426] |
Chemical Information
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CAS No. 67667-71-4
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Molecular Weight 406.43
-
Formula C21H26O8
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SMILES
CC(OCC1=C([C@H](C[C@H]2C)OC(C(C)=C)=O)/C(OC1=O)=C\[C@](O[C@]23O)(CC3)C)=O
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Structure Classification
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)