P5091

For research use only. Not for therapeutic Use.

  • CAT Number: I005302
  • CAS Number: 882257-11-6
  • Molecular Formula: C₁₂H₇Cl₂NO₃S₂
  • Molecular Weight: 348.22
  • Purity: ≥95%
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P5091(Cat No.:I005302)is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), an enzyme that catalyzes the methylation of arginine residues on histone and non-histone proteins. PRMT5 is involved in regulating gene expression, RNA processing, and cell survival, and its overactivity is linked to various cancers, including lymphoma, lung, and breast cancers. By inhibiting PRMT5, P5091 disrupts these processes, leading to impaired tumor growth and increased apoptosis in cancer cells. P5091 is currently being investigated in preclinical and clinical studies for its potential as a targeted cancer therapy.


Catalog Number I005302
CAS Number 882257-11-6
Synonyms

P005091; 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone

Molecular Formula C₁₂H₇Cl₂NO₃S₂
Purity ≥95%
Target Deubiquitinase
Solubility DMSO: 28 mg/mL, H2O: <1 mg/mL
Storage Store at 4°C
IC50 4.2 uM (EC50)
IUPAC Name 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone
InChI InChI=1S/C12H7Cl2NO3S2/c1-6(16)10-5-8(15(17)18)12(20-10)19-9-4-2-3-7(13)11(9)14/h2-5H,1H3
InChIKey LKZLGMAAKNEGCH-UHFFFAOYSA-N
SMILES CC(=O)C1=CC(=C(S1)SC2=C(C(=CC=C2)Cl)Cl)[N+](=O)[O-]
Reference

1. Cell Biochem Biophys. 2011 Jun;60(1-2):61-8. doi: 10.1007/s12013-011-9185-5.
<br><br>
The multifaceted roles of USP7: new therapeutic opportunities.
<br><br>
Nicholson B(1), Suresh Kumar KG.
<br>
Author information: <br>
(1)Progenra Inc, 277 Great Valley Parkway, Malvern, PA 19355, USA.
[email protected]
<br><br>
The deubiquitylating enzyme USP7 (HAUSP) sits at a critical node regulating the
activities of numerous proteins broadly characterized as tumor suppressors, DNA
repair proteins, immune responders, viral proteins, and epigenetic modulators.
Aberrant USP7 activity may promote oncogenesis and viral disease making it a
compelling target for therapeutic intervention. Disclosed drug discovery programs
have identified inhibitors of USP7 such as P005091 with cellular proof of concept
and anti-proliferative activity in cancer models. Taken together, USP7 inhibitors
hold promise as a new strategy for the treatment of disease.

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