tHGA
tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM.
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- CAS No.: 43230-43-9
- Formule: C18H24O4
- Masse moléculaire:304.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2 x 10-5 M
Compound: 39
|
Cytotoxicity against human A549 cells after 72 hrs by XTT assay
Cytotoxicity against human A549 cells after 72 hrs by XTT assay
|
[PMID: 20619940] |
| A549 | IC50 |
3.5 μM
Compound: 10
|
Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis
Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis
|
[PMID: 28240894] |
| HeLa | IC50 |
2.1 x 10-5 M
Compound: 39
|
Cytotoxicity against human HeLa cells after 72 hrs by XTT assay
Cytotoxicity against human HeLa cells after 72 hrs by XTT assay
|
[PMID: 20619940] |
| HL-60 | IC50 |
1.9 x 10-5 M
Compound: 39
|
Cytotoxicity against human HL60 cells after 72 hrs by XTT assay
Cytotoxicity against human HL60 cells after 72 hrs by XTT assay
|
[PMID: 20619940] |
| HMEC-1 | IC50 |
22.5 μM
Compound: 4a
|
Antiproliferative activity against human HMEC1 cells after 72 hrs
Antiproliferative activity against human HMEC1 cells after 72 hrs
|
[PMID: 25128665] |
| HT-29 | IC50 |
1.9 x 10-5 M
Compound: 39
|
Cytotoxicity against human HT-29 cells after 72 hrs by XTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by XTT assay
|
[PMID: 20619940] |
| Sf21 | IC50 |
0.4 μM
Compound: 1, tHGA
|
Inhibition of human recombinant COX2 expressed in insect Sf21 cells assessed as inhibition of conversion of arachidonic acid to PGE2 preincubated for 15 mins before substrate addition measured after 5 mins by enzyme immunoassay
Inhibition of human recombinant COX2 expressed in insect Sf21 cells assessed as inhibition of conversion of arachidonic acid to PGE2 preincubated for 15 mins before substrate addition measured after 5 mins by enzyme immunoassay
|
[PMID: 21958738] |
Chemical Information
-
CAS No. 43230-43-9
-
Masse moléculaire 304.38
-
Formule C18H24O4
-
SMILES
OC1=CC(O)=C(C(O)=C1C(C)=O)C/C=C(CC/C=C(C)\C)\C
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)