Art. -Nr.: HY-136528

RA-9

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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.

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Reinheit: 98.57%
CAS. Nr.: 919091-63-7
Formel: C₁₉H₁₅N₃O₅
Molecular Weight:365.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

RA-9 Chemical Structure

CAS. Nr.: 919091-63-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen :

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]
CCRF-CEM	IC₅₀	0.81 μM Compound: 410	Antiproliferative activity against human CEM cells assessed as cell growth inhibition Antiproliferative activity against human CEM cells assessed as cell growth inhibition	[PMID: 32172081]
CCRF-CEM	IC₅₀	4.47 μM Compound: 1e	Cytotoxicity against CEM T-lymphocytes. Cytotoxicity against CEM T-lymphocytes.	[PMID: 11170648]
CCRF-CEM	IC₅₀	4.47 μM Compound: 1e	Cytotoxicity against human CEM cells Cytotoxicity against human CEM cells	[PMID: 19819135]
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]
L1210	IC₅₀	0.81 μM Compound: 410	Antiproliferative activity against mouse L1210 cells assessed as cell growth inhibition Antiproliferative activity against mouse L1210 cells assessed as cell growth inhibition	[PMID: 32172081]
L1210	IC₅₀	214 μM Compound: 1e	Inhibitory effect on the biosyntheses of protein in murine L1210 cells. Inhibitory effect on the biosyntheses of protein in murine L1210 cells.	[PMID: 11170648]
L1210	IC₅₀	228 μM Compound: 1e	Inhibitory effect on the biosyntheses of DNA in murine L1210 cells. Inhibitory effect on the biosyntheses of DNA in murine L1210 cells.	[PMID: 11170648]
L1210	IC₅₀	276 μM Compound: 1e	Inhibitory effect on the biosyntheses of RNA in murine L1210 cells. Inhibitory effect on the biosyntheses of RNA in murine L1210 cells.	[PMID: 11170648]
L1210	IC₅₀	32.09 μM Compound: 1e	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 19819135]
L1210	IC₅₀	32.9 μM Compound: 1e	Cytotoxicity against murine L1210 cells. Cytotoxicity against murine L1210 cells.	[PMID: 11170648]
MOLT-4	IC₅₀	8.28 μM Compound: 1e	Cytotoxicity against human Molt4/C8 cells Cytotoxicity against human Molt4/C8 cells	[PMID: 19819135]
P388	IC₅₀	0.2 μM Compound: 1e	Cytotoxicity against murine P388 cells. Cytotoxicity against murine P388 cells.	[PMID: 11170648]
P388	IC₅₀	0.81 μM Compound: 410	Antiproliferative activity against mouse P388 cells assessed as cell growth inhibition Antiproliferative activity against mouse P388 cells assessed as cell growth inhibition	[PMID: 32172081]
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.

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.

Chemical Information

CAS. Nr. 919091-63-7
Appearance Solid
Molecular Weight 365.34
Formel C₁₉H₁₅N₃O₅
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Coughlin K, et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ubiquitination Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RA-9

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ubiquitination Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RA-9 Related Classifications

HY-136528 Related Classifications