1. Cell Cycle/DNA Damage
    Apoptosis
  2. Deubiquitinase
    Apoptosis
  3. RA-9

RA-9 

Cat. No.: HY-136528
Handling Instructions

RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.

For research use only. We do not sell to patients.

RA-9 Chemical Structure

RA-9 Chemical Structure

CAS No. : 919091-63-7

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 95 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
100 mg USD 420 In-stock
Estimated Time of Arrival: December 31
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Description

RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells[1].

In Vitro

RA-9 (10-30 μM; 48 hours) inhibits growth of ovarian cancer cell lines and primary cultures[1].
RA-9 (1.25-5 μM; 18 hours) causes cell cycle arrest and caspase-mediated apoptosis in ovarian cancer cells[1].
RA-9 (5 μM; 0-24 hours) induces ER-stress responses in ovarian cancer cells[1].
RA-9 (5 μM; over 24 hours) treatment results with time-dependent accumulation of the cleaved formed of PARP noticeable as early as 8 hours[1].

Cell Viability Assay[1]

Cell Line: Cisplatin-sensitive ovarian cancer cell lines TOV-21G and ES-2, Cisplatin-resistant ovarian cancer cell lines HEY and OVCAR-3, primary ovarian cancer cells
Concentration: 10, 20, 30 μM
Incubation Time: 48 hours
Result: Compromised the viability of ovarian cancer cells in a dose-dependent fashion.

Cell Cycle Analysis[1]

Cell Line: ES-2 cells
Concentration: 1.25, 5 μM
Incubation Time: 18 hours
Result: Resulted in a dose-dependent increase in the fraction of ES-2 cells in the G2-M cell cycle phase.

Western Blot Analysis[1]

Cell Line: ES-2, SKOV-3 and TOV-21G ovarian cancer cells
Concentration: 5 μM
Incubation Time: 0-24 h
Result: Caused a time-dependent increase in the steady levels of the early ER-stress marker GRP-78, as well as the late ER-stress markers IRE1-α and Ero1L-α.
In Vivo

RA-9 (5 mg/kg; i.p; one-day on, two-days off) inhibits human ovarian cancer cell growth in vivo and prolongs survival in a mouse model for ovarian cancer[1].

Animal Model: Six-week-old female immunodeficient (NCr nu/nu) mice[1]
Dosage: 5 mg/kg
Administration: I.p; one-day on, two-days off
Result: Significant reduction in tumor burden at day 12.
Molecular Weight

365.34

Formula

C₁₉H₁₅N₃O₅

CAS No.

919091-63-7

SMILES

O=C1/C(CNC/C1=C\C2=CC=C([N+]([O-])=O)C=C2)=C/C3=CC=C([N+]([O-])=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 4.17 mg/mL (11.41 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7372 mL 13.6859 mL 27.3718 mL
5 mM 0.5474 mL 2.7372 mL 5.4744 mL
10 mM 0.2737 mL 1.3686 mL 2.7372 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

RA-9RA9RA 9DeubiquitinaseApoptosisDUBsovariancancercellsUnfoldedProteinResponsesurvivalERInhibitorinhibitorinhibit

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RA-9
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HY-136528
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