2. Metabolic Enzyme/Protease
  3. Proteasome
  4. RA190

RA190 

Cat. No.: HY-100739 Purity: 99.09%
COA Handling Instructions

RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

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

RA190 Chemical Structure

RA190 Chemical Structure

CAS No. : 1617495-03-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 205 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 205 In-stock
Solid
5 mg USD 156 In-stock
10 mg USD 228 In-stock
25 mg USD 348 In-stock
50 mg USD 624 In-stock
100 mg USD 1104 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

IC50 & Target

IC50: 0.15 μM (HeLa cell)
In Vitro

RA190 covalently binds to cysteine 88 of ubiquitin receptor RPN13 in the 19S regulatory particle and inhibits proteasome function, triggering rapid accumulation of polyubiquitinated proteins. Multiple myeloma (MM) lines, even those resistant to bortezomib, are sensitive to RA190 via endoplasmic reticulum stress-related apoptosis. RA190 stabilizes targets of human papillomavirus (HPV) E6 oncoprotein, and preferentially kills HPV-transformed cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

RA190 distributes to plasma and major organs excepting brain, and inhibits proteasome function in skin and muscle. RA190 administration profoundly reduces growth of multiple myeloma and ovarian cancer xenografts, and oral RA190 treatment retards HPV16+ syngeneic mouse tumor growth, without impacting spontaneous HPV-specific CD8+ T cell responses[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

596.76

Appearance

Solid

Formula

C28H23Cl5N2O2
CAS No.
SMILES

O=C1/C(CN(C([[email protected]@H](N)CC2=CC=CC=C2)=O)C/C1=C/C3=CC=C(Cl)C(Cl)=C3)=C\C4=CC=C(Cl)C(Cl)=C4.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (167.57 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6757 mL 8.3786 mL 16.7572 mL
5 mM 0.3351 mL 1.6757 mL 3.3514 mL
10 mM 0.1676 mL 0.8379 mL 1.6757 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.38 mg/mL (3.99 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.09%

COA (251 KB) LCMS (259 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

RA190 is dissolved in DMSO and diluted with cell culture medium. HeLa cells are treated with RA190 (0.2, 0.4, 0.6, 0.8, 1, 2, 3, 4, 5 μM) for 48 hr. Cell viability is assayed using commerical kit[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Mice are divided into two groups and treated daily i.p. with RA190 (10 mg/kg) or vehicle, and imaged again on day 7 and day 14. NOG mice (5 per group) are inoculated with 1X106 NCI-H929-GFP-Luc cells i.v., and after 4 weeks, mice are imaged for their luciferase activity and divided into two groups. Mice are treated i.p. with RA190 (20 mg/kg) or vehicle, and imaged again at the end of the treatment for their luciferase activity[1].

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

RA1901617495-03-0RA 190RA-190ProteasomeInhibitorinhibitorinhibit

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