Proteasome-IN-3

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 563039

CAS#: 1262295-74-8

Description: Proteasome-IN-3 is an inhibitor of proteasome-associated DUBs.

Chemical Structure

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Proteasome-IN-3
CAS# 1262295-74-8
Instruction

Theoretical Analysis

MedKoo Cat#: 563039
Name: Proteasome-IN-3
CAS#: 1262295-74-8
Chemical Formula: C32H37Cl4N7O5
Exact Mass: 739.16
Molecular Weight: 741.490
Elemental Analysis: C, 51.83; H, 5.03; Cl, 19.12; N, 13.22; O, 10.79

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: RA-9; RA 9; RA9; Proteasome-IN-3

IUPAC/Chemical Name: N2-[[(3E,5E)-3,5-bis[(3,4-dichlorophenyl)methylene]-4-oxo-1-piperidinyl]carbonyl]-L-arginyl-L-lysine

InChi Key: BNQKHLJMLJIRBI-PMWHKEQESA-N

InChi Code: InChI=1S/C32H37Cl4N7O5/c33-22-8-6-18(14-24(22)35)12-20-16-43(17-21(28(20)44)13-19-7-9-23(34)25(36)15-19)32(48)42-26(5-3-11-40-31(38)39)29(45)41-27(30(46)47)4-1-2-10-37/h6-9,12-15,26-27H,1-5,10-11,16-17,37H2,(H,41,45)(H,42,48)(H,46,47)(H4,38,39,40)/b20-12+,21-13+/t26-,27-/m0/s1

SMILES Code: NCCCC[C@@H](C(O)=O)NC([C@H](CCCNC(N)=N)NC(N1C/C(C(/C(C1)=C/C2=CC=C(Cl)C(Cl)=C2)=O)=C\C3=CC=C(Cl)C(Cl)=C3)=O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 741.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: De Winter LM, Hansen WL, van Steenbergen HW, Geusens P, Lenaerts J, Somers K, Stinissen P, van der Helm-van Mil AH, Somers V. Autoantibodies to two novel peptides in seronegative and early rheumatoid arthritis. Rheumatology (Oxford). 2016 Aug;55(8):1431-6. doi: 10.1093/rheumatology/kew198. Epub 2016 Apr 19. PubMed PMID: 27094600.

2: Vogel RI, Coughlin K, Scotti A, Iizuka Y, Anchoori R, Roden RB, Marastoni M, Bazzaro M. Simultaneous inhibition of deubiquitinating enzymes (DUBs) and autophagy synergistically kills breast cancer cells. Oncotarget. 2015 Feb 28;6(6):4159-70. PubMed PMID: 25784654; PubMed Central PMCID: PMC4414179.

3: Coughlin K, Anchoori R, Iizuka Y, Meints J, MacNeill L, Vogel RI, Orlowski RZ, Lee MK, Roden RB, Bazzaro M. 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 Jun 15;20(12):3174-86. doi: 10.1158/1078-0432.CCR-13-2658. Epub 2014 Apr 11. PubMed PMID: 24727327; PubMed Central PMCID: PMC4269153.

4: Issaenko OA, Amerik AY. Chalcone-based small-molecule inhibitors attenuate malignant phenotype via targeting deubiquitinating enzymes. Cell Cycle. 2012 May 1;11(9):1804-17. doi: 10.4161/cc.20174. Epub 2012 May 1. Erratum in: Cell Cycle. 2012 Sep 15;11(18):3518. PubMed PMID: 22510564; PubMed Central PMCID: PMC3372381.

5: van der Poel EP, Stevens RJ, Lohse D. Connecting flow structures and heat flux in turbulent Rayleigh-Bénard convection. Phys Rev E Stat Nonlin Soft Matter Phys. 2011 Oct;84(4 Pt 2):045303. Epub 2011 Oct 19. PubMed PMID: 22181218.

6: Zhu GY, Li YW, Hau DK, Jiang ZH, Yu ZL, Fong WF. Acylated protopanaxadiol-type ginsenosides from the root of Panax ginseng. Chem Biodivers. 2011 Oct;8(10):1853-63. doi: 10.1002/cbdv.201000196. PubMed PMID: 22006713.