1. Metabolic Enzyme/Protease
  2. Proteasome

RA190 

Cat. No.: HY-100739 Purity: 98.03%
Data Sheet SDS 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 (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $171 In-stock
5 mg $130 In-stock
10 mg $190 In-stock
25 mg $290 In-stock
50 mg $520 In-stock
100 mg $920 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

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].

References
Preparing Stock Solutions
Concentration Volume 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.
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]

RA190 is formulated in 20% (w/v) β-hydroxyisopropyl-cyclodextrin in water.

Mouse: 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
Molecular Weight

596.76

Formula

C₂₈H₂₃Cl₅N₂O₂

CAS No.

1617495-03-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 10 mM

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.03%

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Product Name:
RA190
Cat. No.:
HY-100739
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