1. Immunology/Inflammation
  2. AP-1
  3. (+)-Glaucarubinone

(+)-Glaucarubinone is a potent AP-1 (activator protein-1) inhibitor with an EC50 value of 0.13 µM. (+)-Glaucarubinone shows noncytotoxic.

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(+)-Glaucarubinone Chemical Structure

(+)-Glaucarubinone Chemical Structure

CAS No. : 1259-86-5

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Description

(+)-Glaucarubinone is a potent AP-1 (activator protein-1) inhibitor with an EC50 value of 0.13 µM. (+)-Glaucarubinone shows noncytotoxic[1].

IC50 & Target

EC50: 0.13 µM (AP-1)[1]

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.04 μM
Compound: 4
Inhibition of TPA-induced AP1 transfected in HEK293 cells assessed as inhibition of beta-lactamase reporter activity treated 1 hr before TPA stimulation measured after 18 hrs by luciferase reporter gene assay
Inhibition of TPA-induced AP1 transfected in HEK293 cells assessed as inhibition of beta-lactamase reporter activity treated 1 hr before TPA stimulation measured after 18 hrs by luciferase reporter gene assay
[PMID: 19199792]
HEK-293T EC50
0.13 μM
Compound: 2
Inhibition of TPA-induced AP-1 activity expressed in human HEK293T cells treated 1 hr before TPA challenge measured after 18 hrs by FRET based beta-lactamase reporter assay
Inhibition of TPA-induced AP-1 activity expressed in human HEK293T cells treated 1 hr before TPA challenge measured after 18 hrs by FRET based beta-lactamase reporter assay
[PMID: 21733691]
HeLa IC50
0.27 μM
Compound: 4
Inhibition of protein synthesis in human HeLa cells assessed as [35S]methionine incorporation into protein treated for 45 mins before [35S]methionine addition by Whatman paper analysis
Inhibition of protein synthesis in human HeLa cells assessed as [35S]methionine incorporation into protein treated for 45 mins before [35S]methionine addition by Whatman paper analysis
[PMID: 19199792]
HL-60 IC50
0.5 μM
Compound: 25
Antiproliferative activity against human HL60 cells assessed as inhibition of [3H]thymidine incorporation after 4 days by liquid scintillation counter
Antiproliferative activity against human HL60 cells assessed as inhibition of [3H]thymidine incorporation after 4 days by liquid scintillation counter
[PMID: 11754601]
HL-60 IC50
1 μM
Compound: 25
Cytotoxicity against human HL60 cells assessed as loss of membrane integrity after 4 days by trypan blue exclusion assay
Cytotoxicity against human HL60 cells assessed as loss of membrane integrity after 4 days by trypan blue exclusion assay
[PMID: 11754601]
HL-60 EC50
1.8 μM
Compound: 25
Induction of cell differentiation in human HL60 cells assessed as superoxide anion production after 4 days by NBT reduction assay
Induction of cell differentiation in human HL60 cells assessed as superoxide anion production after 4 days by NBT reduction assay
[PMID: 11754601]
Molecular Weight

494.53

Formula

C25H34O10

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@]3([H])[C@]45[C@@]([C@H]([C@H]([C@@]3(OC5)O)O)C)([H])[C@H](C(O[C@]4([H])C[C@@]1([H])C(C)=CC([C@H]2O)=O)=O)OC([C@@](C)(O)CC)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Purity & Documentation

Purity: 96.46%

References
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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.

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(+)-Glaucarubinone
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