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

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

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

RA-9 Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

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USP1 USP2 USP7 USP8 USP30 UCHL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.4 μM
Compound: 4c
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 19046794]
Caov-3 cell line IC50
1.03 μM
Compound: 4c
Cytotoxicity against human Caov3 cells after 72 hrs by MTT assay
Cytotoxicity against human Caov3 cells after 72 hrs by MTT assay
[PMID: 19046794]
HepG2 IC50
> 2000 ng/mL
Compound: 5b
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 24139941]
HepG2 IC50
356 ng/mL
Compound: 5b
Antimalarial activity against liver stage Plasmodium berghei ANKA sporozoites infected in human HepG2 cells after 48 hrs by luciferase reporter gene assay
Antimalarial activity against liver stage Plasmodium berghei ANKA sporozoites infected in human HepG2 cells after 48 hrs by luciferase reporter gene assay
[PMID: 24139941]
HL-60 CC50
3.6 μM
Compound: 1c
Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test
Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test
[PMID: 17499885]
HSC-2 CC50
0.9 μM
Compound: 1c
Cytotoxicity against human HSC2 by MTT method
Cytotoxicity against human HSC2 by MTT method
[PMID: 17499885]
HSC-4 CC50
6.1 μM
Compound: 1c
Cytotoxicity against human HSC4 cells by MTT method
Cytotoxicity against human HSC4 cells by MTT method
[PMID: 17499885]
PC-3 IC50
1.54 μM
Compound: 4c
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
[PMID: 19046794]
SK-OV-3 IC50
2.5 μM
Compound: 4c
Cytotoxicity against human Scov3 cells after 72 hrs by MTT assay
Cytotoxicity against human Scov3 cells after 72 hrs by MTT assay
[PMID: 19046794]
U-87MG ATCC IC50
7.15 μM
Compound: 2e
Cytotoxicity against human U87MG cells after 48 hrs by resazurin assay
Cytotoxicity against human U87MG cells after 48 hrs by resazurin assay
[PMID: 25639862]
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].

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

RA-9 Related Antibodies

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].

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

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.
Appearance

Solid

Color

Light yellow to yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 4.17 mg/mL (11.41 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7372 mL 13.6859 mL 27.3718 mL 68.4294 mL
5 mM 0.5474 mL 2.7372 mL 5.4744 mL 13.6859 mL
10 mM 0.2737 mL 1.3686 mL 2.7372 mL 6.8429 mL
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RA-9 Related Classifications

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:

RA-9919091-63-7RA9RA 9DeubiquitinaseApoptosisDUBsovariancancercellsUnfoldedProteinResponsesurvivalERInhibitorinhibitorinhibit

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