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

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

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10 mM * 1 mL in DMSO
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5 mg USD 156 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

RA190 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

RA190 Related Antibodies
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].

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

596.76

Formula

C28H23Cl5N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1/C(CN(C([C@@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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.38 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (23.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6757 mL 8.3786 mL 16.7572 mL 41.8929 mL
5 mM 0.3351 mL 1.6757 mL 3.3514 mL 8.3786 mL
10 mM 0.1676 mL 0.8379 mL 1.6757 mL 4.1893 mL
15 mM 0.1117 mL 0.5586 mL 1.1171 mL 2.7929 mL
20 mM 0.0838 mL 0.4189 mL 0.8379 mL 2.0946 mL
25 mM 0.0670 mL 0.3351 mL 0.6703 mL 1.6757 mL
30 mM 0.0559 mL 0.2793 mL 0.5586 mL 1.3964 mL
40 mM 0.0419 mL 0.2095 mL 0.4189 mL 1.0473 mL
50 mM 0.0335 mL 0.1676 mL 0.3351 mL 0.8379 mL
60 mM 0.0279 mL 0.1396 mL 0.2793 mL 0.6982 mL
80 mM 0.0209 mL 0.1047 mL 0.2095 mL 0.5237 mL
100 mM 0.0168 mL 0.0838 mL 0.1676 mL 0.4189 mL
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RA190 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:

RA1901617495-03-0RA 190RA-190ProteasomeInhibitorinhibitorinhibit

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