Home > Products > Featured products

RA-9

  Cat. No.:  DC39255   Featured
Chemical Structure
919091-63-7
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
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[1].
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 919091-63-7
Chemical Name: RA-9
Synonyms: 4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-, (3E,3E)-;(3E,5E)-3,5-Bis[(4-Nitrophenyl)methylene]-4-piperidinone;4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-, (3E,5E)-;RA-9 UPS inhibitor;RA-9;(3E,5E)-3,5-Bis[(4-nitrophenyl)methylene]-4-piperidinone (ACI)
SMILES: C(/C1C=CC([N+](=O)[O-])=CC=1)=C1/CNC/C(=C\C2C=CC([N+](=O)[O-])=CC=2)/C/1=O
Formula: C19H15N3O5
M.Wt: 365.339504480362
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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.
Description: 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[1].
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]. 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.
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]. 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.
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC33635 DODAP DODAP, also known as 1,2-Dioleoyl-3-dimethylammonium-propane, is a cationic lipid. It has been used as a component in liposomes that can be used to encapsulate siRNA, immunostimulatory oligodeoxynucleotides, antisense oligonucleotides, or chemotherapeutic agents for in vitro and in vivo delivery.
DC58047 DSPE-PEG 2000 PEG2000-DSPE is used for creating micelles that are able to carry drugs with low solubility.
DC31000 LP-01 LP-01 is an ionizable cationic amino lipid (pKa = ~6.1). It has been used in the generation of lipid nanoparticles (LNPs). LNPs containing LP-01 and encapsulating both Cas9 mRNA and modified single-guide RNA (sgRNA) for the transport protein transthyretin (Ttr) induce gene editing in liver cells in mice in a dose-dependent manner resulting in reduced serum Ttr levels for at least 12 months.
DC66546 R-Sirpiglenastat R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
DC60597 AZD0780 AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.
DC66114 FAPI-46 FAPI46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI 46 can be used for tumor imaging of a multitude of different cancers.
DC60580 Endosidin5(ES5) Endosidine 5 (ES5), is one of the most potent small molecules interferes with recycling endosomes through Annexin A6, thereby promoting the release and expression of mRNA into the cytoplasm. The delivered mRNAs is greatly enhanced via inhibition of endocytic recycling in cells and in live mice. NAV2729 (NAV) and endosidin 5 (ES5), resulted in significant enhancement (1.5–2 folds) of LNP-mediated delivery of Fluc mRNAs. Incubation of NAV and ES5 together caused modest further increases in Fluc expression in comparison to the sole application of either compound.
DC90056 PLX-5622 HCl form (water solubility form) PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.
DC60559 PT-179 PT-179 is a new orthogonal immunomodulatory drug (IMiD) derivative that binds CRBN but does not induce degradation of off-target proteins. PT-179 potently degrades proteins fused to SD40 at either the N or C terminus.
DC65841 MC1 MC1 is a selective and potent inhibitor for COX-2, and [11C]MC1 detected COX-2 in nonhuman primates after intracerebral injection of an inflammogen.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia