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RA-9

Catalog No. T8464 CAS 919091-63-7

RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.

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RA-9, CAS 919091-63-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 45.00
10 mg	In stock	$ 76.00
25 mg	In stock	$ 133.00
50 mg	In stock	$ 197.00
100 mg	In stock	$ 308.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.31%

Biological Description

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Description	RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.
In vitro	The characterization of RA-9 as a small-molecule inhibitor of proteasome-associated DUBs.?Treatment with RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors.?Loss of cell viability following RA-9 exposure is associated with an unfolded protein response as mechanism to compensate for unsustainable levels of proteotoxic stress.
In vivo	In vivo treatment with RA-9 retards tumor growth, increases overall survival, and was well tolerated by the host.
Animal Research	Mice were inoculated i.p. with 100,000 ES-2 cells (in 100 μl DMEM) stably expressing GFP.?When tumor was detectable (approx.?6 days post inoculation), mice were randomly assigned into two groups receiving RA-9 or 0.9% saline.?Treatment with RA-9 was given i.p. on a one-day on, two-days off schedule.?The control group received the vehicle alone at the same schedule.?Working concentrations of RA-9 (10 mg/ml) were reached by dissolution in Cremophor EL and polyethylene glycol 400 (Sigma).?Prior to each injection RA-9 was further diluted in 0.9% saline (working concentration 1mg/ml).?To monitor for tumor growth, RA-9 treated and control mice were imaged with an IVIS SpectrumCT Pre-clinical in vivo imaging system (PerkinElmer) every other day.?Animals were sacrificed when abdomens became distended to twice normal size.

Molecular Weight	365.34
Formula	C19H15N3O5
CAS No.	919091-63-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4 mg/mL (10.95 mM), Sonification and heating to 80℃ are recommended.

References and Literature

1. Coughlin K , Anchoori R , Iizuka Y , et al. Small-molecule RA-9 inhibits proteasome-associated DUBs and ovarian cancer in vitro and in vivo via exacerbating unfolded protein responses.[J]. Clinical Cancer Research An Official Journal of the American Association for Cancer Research, 2014, 20(12):3174-86.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library DNA Damage & Repair Compound Library Ubiquitination Compound Library Bioactive Compound Library Covalent Inhibitor Library Anti-Cancer Compound Library Apoptosis Compound Library Cell Cycle Compound Library

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Keywords

RA-9 919091-63-7 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB Unfolded cancer RA 9 DUBs Inhibitor Response Deubiquitinase cells inhibit Protein RA9 ovarian survival inhibitor

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