RA-9 UPS inhibitor

Alias: RA-9; RA 9; RA9; RA-9 UPS inhibitor
Cat No.:V2165 Purity: ≥98%
RA-9 is a cell permeable and potent inhibitor of the ubiquitin-proteasome system (UPS).
RA-9 UPS inhibitor Chemical Structure CAS No.: 919091-63-7
Product category: DUB
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

RA-9 is a cell permeable and potent inhibitor of the ubiquitin-proteasome system (UPS). RA-9 Inhibits Proteasome-Associated DUBs and Ovarian Cancer in Vitro and in Vivo via Exacerbating Unfolded Protein Responses. 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 treatment with RA-9 retards tumor growth, increases overall survival, and was well tolerated by the host.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
The growth of primary cultures and cell lines of ovarian cancer is inhibited by RA-9 (10-30 μM; 48 hours) [1]. In ovarian cancer cells, RA-9 (1.25-5 μM; 18 hours) induces cell cycle arrest and caspase-mediated apoptosis [1]. Inducing ER-stress responses in ovarian cancer cells, RA-9 (5 μM; 0-24 hours) [1]. RA-9 (5 μM; more than a day) treatment outcomes, with as early as eight hours of time-dependent accumulation of the cleaved form of PARP [1].
ln Vivo
In a mouse model of ovarian cancer, RA-9 (5 mg/kg; i.p.; one day on, two days off) prolongs survival by inhibiting the growth of human ovarian cancer cells in vivo [1].
Animal Protocol
Six-week-old female immunodeficient (NCr nu/nu) mice [1].
5 mg/kg
References

[1]. Small-molecule RA-9 inhibits proteasome-associated DUBs and ovarian cancer in vitro and in vivo via exacerbating unfolded protein responses. Clin Cancer Res. 2014;20(12):3174-3186.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H15N3O5
Molecular Weight
365.345
Exact Mass
365.1012
Elemental Analysis
C, 62.46; H, 4.14; N, 11.50; O, 21.90
CAS #
919091-63-7
Appearance
Solid powder
SMILES
O=C1/C(CNC/C1=C\C2=CC=C([N+]([O-])=O)C=C2)=C/C3=CC=C([N+]([O-])=O)C=C3
InChi Key
YUYPWAMLWZVHAE-KAVGSWPWSA-N
InChi Code
InChI=1S/C19H15N3O5/c23-19-15(9-13-1-5-17(6-2-13)21(24)25)11-20-12-16(19)10-14-3-7-18(8-4-14)22(26)27/h1-10,20H,11-12H2/b15-9+,16-10+
Chemical Name
(3E,5E)-3,5-Bis[(4-nitrophenyl)methylene]-4-piperidinone
Synonyms
RA-9; RA 9; RA9; RA-9 UPS inhibitor
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO :4.17~8 mg/mL ( 11.41~21.89 mM )
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7371 mL 13.6855 mL 27.3710 mL
5 mM 0.5474 mL 2.7371 mL 5.4742 mL
10 mM 0.2737 mL 1.3686 mL 2.7371 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
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