2. Cytoskeleton Metabolic Enzyme/Protease PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway NF-κB
  3. Cadherin MMP Akt FAK ERK NF-κB
  4. (Rac)-AAA

(Rac)-AAA is a regulator and inhibitor targeting GPR75. By blocking the 20-HETE-induced downregulation of GPR75 expression, (Rac)-AAA effectively inhibits the activation of key downstream signaling pathways including EGFR, AKT, NF-κB and FAK. (Rac)-AAA reverses 20-HETE-mediated epithelial-mesenchymal transition, which is specifically characterized by downregulating vimentin (vimentin), upregulating E-Cadherin, as well as reducing MMP-2 activity and cancer cell migration ability. (Rac)-AAA also abolishes the 20-HETE-induced upregulation of HIC-5 expression and anchorage-independent growth, and modulates the subcellular localization of PKC-α and phosphorylated AKT. (Rac)-AAA is investigated in androgen-independent prostate cancer (castration-resistant prostate cancer).

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(Rac)-AAA

(Rac)-AAA Chemical Structure

CAS No. : 3055022-23-3

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Other Forms of (Rac)-AAA:

(Rac)-AAA Related Antibodies

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

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Akt Akt1 Akt2 Akt3

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ERK ERK1 ERK2 ERK5 ERK8

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Description

(Rac)-AAA is a regulator and inhibitor targeting GPR75. By blocking the 20-HETE-induced downregulation of GPR75 expression, (Rac)-AAA effectively inhibits the activation of key downstream signaling pathways including EGFR, AKT, NF-κB and FAK. (Rac)-AAA reverses 20-HETE-mediated epithelial-mesenchymal transition, which is specifically characterized by downregulating vimentin (vimentin), upregulating E-Cadherin, as well as reducing MMP-2 activity and cancer cell migration ability. (Rac)-AAA also abolishes the 20-HETE-induced upregulation of HIC-5 expression and anchorage-independent growth, and modulates the subcellular localization of PKC-α and phosphorylated AKT. (Rac)-AAA is investigated in androgen-independent prostate cancer (castration-resistant prostate cancer)[1].

IC50 & Target

MMP-2

 

In Vitro

(Rac)-AAA (5-10 μM; 12 h) reverses the 20-HETE-induced reduction in GPR75 expression, and increases baseline GPR75 expression in PC-3 human prostate cancer cells[1].
(Rac)-AAA (5-10 μM; 2 h) reduces 20-HETE-induced phosphorylation of EGFR, AKT, and NF-κB, and increases baseline p38 phosphorylation in PC-3 human prostate cancer cells[1].
(Rac)-AAA (5-10 μM; 24 h) reverses 20-HETE-induced epithelial-mesenchymal transition by restoring E-cadherin expression and reducing or abrogating vimentin expression in PC-3 human prostate cancer cells[1].
(Rac)-AAA (5-10 μM; 24 h) reduces or abrogates 20-HETE-induced MMP-2 activity in conditioned medium from PC-3 human prostate cancer cells[1].
(Rac)-AAA (5 μM; 21 days) abrogates the increase in anchorage-independent colony formation induced by 5,14-HEDGE in PC-3 human prostate cancer cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(Rac)-AAA Related Antibodies

Western Blot Analysis[1]

Cell Line: PC-3 human prostate cancer cells
Concentration: 5 μM (co-incubated with 20-HETE); 10 μM (co-incubated with 20-HETE); 10 μM (incubated alone)
Incubation Time: 2 h (all conditions)
Result: Decreased 20-HETE-induced EGFR phosphorylation by 44% (5 μM) and 68% (10 μM) relative to 20-HETE alone.
Decreased 20-HETE-induced AKT phosphorylation by 40% (5 μM) and 58% (10 μM) relative to 20-HETE alone.
Decreased 20-HETE-induced NF-κB phosphorylation by 66% (both 5 μM and 10 μM) relative to 20-HETE alone.
Increased baseline p38 phosphorylation by 248% relative to control.

Western Blot Analysis[1]

Cell Line: PC-3 human prostate cancer cells
Concentration: 5 μM (co-incubated with 20-HETE); 10 μM (co-incubated with 20-HETE)
Incubation Time: 24 h (all conditions)
Result: Reversed the 20-HETE-induced 40% downregulation of E-cadherin.
Reduced the 20-HETE-induced 150% upregulation of vimentin by 75% (5 μM) relative to 20-HETE alone, and completely abrogated this upregulation at 10 μM.

Cell Migration Assay[1]

Cell Line: PC-3 human prostate cancer cells
Concentration: 5 μM (co-incubated with 20-HETE)
Incubation Time: 16 h
Result: Reduced 20-HETE-induced wound closure from 48.9% to 36.0% relative to 20-HETE alone.
Molecular Weight

483.55

Formula

C24H39NNa2O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(NC(CCCC/C=C\CCCCCCC/C=C\CCCCO)=O)CC(O[Na])=O)O[Na]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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(Rac)-AAA Related Classifications

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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.

Keywords:

(Rac)-AAA3055022-23-3CadherinMMPAktFAKERKNF-κBMatrix metalloproteinasesPKBProtein kinase BPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseExtracellular signal regulated kinasesNuclear factor-κBNuclear factor-kappaBAKTPC-3 human prostate cancer cellsepithelial-mesenchymal transitionEGFRE-cadherin20-HETEandrogen-insensitive prostate cancerGPR75vimentinInhibitorinhibitorinhibit

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