A3023-50mg | P005091 [882257-11-6] Clinisciences

Background

P005091 is a selective, potent inhibitor of USP7 deubiquitylating activity, which is demonstrated to downregulate claspin and phosphorylation of the DNA checkpoint kinase Chk1, and to synergize with genotoxic agents. USP7, known as herpes-associated-ubiquitin-specificprotease (HAUSP), is a deubiquitylating enzyme that regulates the levels of the oncoprotein HDM2 and its substrate, the tumor suppressor p53. P005091 accelerated the degradation of HDM2, while analogs of the compound induced dose- and time-dependent increases in the protein levels of p53 and p21.What’s more,P005091 induced apoptosis in numerous cancer cell lines, including both p53+/+ and p53-mutant cancer cell lines.

Reference

Jeffrey G Marblestone. Ubiquitin Drug Discovery & Diagnostics 2009 – First Annual Conference. IDrugs. 2009; 12(12):750 – 753.

Product Citation

1. Letizia Granieri, Federica Marocchi, et al. "Targeting the USP7/RRM2 axis drives senescence and sensitizes melanoma cells to HDAC/LSD1 inhibitors." Cell Rep. 2022 Sep 20;40(12):111396. PMID: 36130505
2. Lee MJ, Miller Z, et al. "H727 cells are inherently resistant to the proteasome inhibitor carfilzomib, yet require proteasome activity for cell survival and growth." Sci Rep. 2019 Mar 11;9(1):4089. PMID: 30858500

Chemical Properties

Physical Appearance	A solid
Storage	Store at 4°C
M.Wt	348.22
Cas No.	882257-11-6
Formula	C₁₂H₇Cl₂NO₃S₂
Synonyms	P005091,P5091
Solubility	insoluble in H2O; insoluble in EtOH; ≥17.4 mg/mL in DMSO
Chemical Name	1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone
SDF	Download SDF
Canonical SMILES	CC(=O)C1=CC(=C(S1)SC2=C(C(=CC=C2)Cl)Cl)[N+](=O)[O-]
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:
Cell lines	NCI-60 human tumor cell line.
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reaction Conditions	Growth inhibition: 48 h. Cytotoxic activity: 72 h.Solubilized in 100% (v/v) DMSO at 400-fold the desired final maximum test concentration and stored frozen prior to use.
Applications	P005091 exhibits growth inhibition with GI50 value of 1.82 μM in HL-60(TB) cell line and exhibits broad growth inhibition. In HCT-116 cells, P005091 shows cytotoxic activity with EC50 value of 9.21 μM.
Animal experiment [1]:
Animal models	Severe combined immunodeficient (SCID) mice inoculated subcutaneously with human multiple myeloma tumor cells.
Dosage form	10 mg/kg; intravenously twice a week for three weeks.
Applications	In SCID mice, P5091 significantly inhibits human plasmacytoma growth and enhances survival.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Cao P, Weinstock J, Kingsbury WD, et al. Anti-neoplastic compounds, compositions and methods. Patent: US 8680139 B2, 2009.

Biological Activity

Description	P5091(P005091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM and the closely related USP47.
Targets
IC50	4.2 μM (EC50)

Quality Control

Purity = 99.67%

Chemical structure

Related Biological Data

HEK293T cells were treated with DMSO or P5091; crude cell extracts were labeled with indicated UbVME probe, followed by immunoblotting (IB) with indicated antibodies.

P005091 [882257-11-6]

Referentie A3023-50mg

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Background

Product Citation

Chemical Properties

Protocol

Biological Activity

Quality Control

Chemical structure

Related Biological Data

Related Biological Data

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