Ro 90-7501

CAS# 293762-45-5

Ro 90-7501

2D Structure

Catalog No. BCC7351----Order now to get a substantial discount!

Product Name & Size Price Stock
Ro 90-7501: 5mg $92 In Stock
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3D structure

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Ro 90-7501

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Chemical Properties of Ro 90-7501

Cas No. 293762-45-5 SDF Download SDF
PubChem ID 824226 Appearance Powder
Formula C20H16N6 M.Wt 340.39
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in 1eq. HCl and to 100 mM in DMSO
Chemical Name 2-[2-(4-aminophenyl)-3H-benzimidazol-5-yl]-3H-benzimidazol-5-amine
SMILES C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C4=NC5=C(N4)C=C(C=C5)N)N
Standard InChIKey PAGZCEHLFCJSPV-UHFFFAOYSA-N
Standard InChI InChI=1S/C20H16N6/c21-13-4-1-11(2-5-13)19-23-15-7-3-12(9-17(15)25-19)20-24-16-8-6-14(22)10-18(16)26-20/h1-10H,21-22H2,(H,23,25)(H,24,26)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Ro 90-7501

DescriptionInhibitor of amyloid β42 (Aβ42) fibril assembly; reduces Aβ42-induced toxicity (EC50 = 2 μM).

Ro 90-7501 Dilution Calculator

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Ro 90-7501 Molarity Calculator

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Preparing Stock Solutions of Ro 90-7501

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9378 mL 14.689 mL 29.3781 mL 58.7561 mL 73.4452 mL
5 mM 0.5876 mL 2.9378 mL 5.8756 mL 11.7512 mL 14.689 mL
10 mM 0.2938 mL 1.4689 mL 2.9378 mL 5.8756 mL 7.3445 mL
50 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.1751 mL 1.4689 mL
100 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.5876 mL 0.7345 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Ro 90-7501

RO 90-7501 enhances TLR3 and RLR agonist induced antiviral response.[Pubmed:23056170]

PLoS One. 2012;7(10):e42583.

Recognition of virus infection by innate pattern recognition receptors (PRRs), including membrane-associated toll-like receptors (TLR) and cytoplasmic RIG-I-like receptors (RLR), activates cascades of signal transduction pathways leading to production of type I interferons (IFN) and proinflammatory cytokines that orchestrate the elimination of the viruses. Although it has been demonstrated that PRR-mediated innate immunity plays an essential role in defending virus from infection, it also occasionally results in overwhelming production of proinflammatory cytokines that cause severe inflammation, blood vessel leakage and tissue damage. In our efforts to identify small molecules that selectively enhance PRR-mediated antiviral, but not the detrimental inflammatory response, we discovered a compound, Ro 90-7501 ('2'-(4-Aminophenyl)-[2,5'-bi-1H-benzimidazol]-5-amine), that significantly promoted both TLR3 and RLR ligand-induced IFN-beta gene expression and antiviral response, most likely via selective activation of p38 mitogen-activated protein kinase (MAPK) pathway. Our results thus imply that pharmacological modulation of PRR signal transduction pathways in favor of the induction of a beneficial antiviral response can be a novel therapeutic strategy.

Ro 90-7501 inhibits PP5 through a novel, TPR-dependent mechanism.[Pubmed:27840051]

Biochem Biophys Res Commun. 2017 Jan 8;482(2):215-220.

Protein phosphatase 5 (PP5) is a serine/threonine phosphatase that belongs to the PPP family phosphatases. PP5 and the other phosphatases of the PPP family share significantly similar catalytic domain structure. Due to this structural similarity, natural competitive inhibitors such as okadaic acid and cantharidin exhibit broad specificity over the PPP family phosphatases. In this study, we report the identification of three PP5 inhibitors, Ro 90-7501, aurothioglucose, and N-oleoyldopamine, along with a novel inhibitory mechanism of Ro 90-7501. Unlike other inhibitors binding to the phosphatase domain, Ro 90-7501 inhibited PP5 in a TPR-dependent manner. This TPR-dependent PP5 inhibition shown by Ro 90-7501 is a unique and novel inhibitory mechanism, which might be a useful tool for studies of PP5 on both regulatory mechanism and drug discovery.

Self-assembly of beta-amyloid 42 is retarded by small molecular ligands at the stage of structural intermediates.[Pubmed:10940228]

J Struct Biol. 2000 Jun;130(2-3):232-46.

Assemblyof the amyloid-beta peptide (Abeta) into fibrils and its deposition in distinct brain areas is considered responsible for the pathogenesis of Alzheimer's disease (AD). Thus, inhibition of fibril assembly is a potential strategy for therapeutic intervention. Electron cryomicroscopy was used to monitor the initial, native assembly structure of Abeta42. In addition to the known fibrillar intermediates, a nonfibrillar, polymeric sheet-like structure was identified. A temporary sequence of supramolecular structures was revealed with (i) polymeric Abeta42 sheets during the onset of assembly, inversely related to the appearance of (ii) fibril intermediates, which again are time-dependently replaced by (iii) mature fibrils. A cell-based primary screening assay was used to identify compounds that decrease Abeta42-induced toxicity. Hit compounds were further assayed for binding to Abeta42, radical scavenger activity, and their influence on the assembly structure of Abeta42. One compound, Ro 90-7501, was found to efficiently retard mature fibril formation, while extended polymeric Abeta42 sheets and fibrillar intermediates are accumulated. Ro 90-7501 may serve as a prototypic inhibitor for Abeta42 fibril formation and as a tool for studying the molecular mechanism of fibril assembly.

Description

Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.

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