P22077 is an ubiquitin-specific protease USP7 (Ubiquitin-specific protease USP7) inhibitor with EC50 of 8.6 μM and also inhibits USP47.

 

Brand: BCM

 

In Vitro: P22077 is an analogue of the recently discovered USP7 inhibitor P5091. In the experimental concentration range, P22077 had little effect on DEN1 and SENP2core, but inhibited USP7, IC50 was 8μM. In vitro, P22077 inhibited a group of DUBs, cysteine proteases, and other family proteolytic enzymes, suggesting that P22077 inhibited USP7 and its closely related DUBUSP47. 15-45mMP22077 acted on cell lysates and inhibited a small portion of DUBs. P22077 induced tumor Chemicalbook cell death and EC50 was in the low micromolar range. Unlike a wide range of specific inhibitors, P22077 has changed its inhibitory effect on ubiquitination protein levels. P22077 treated G1/S phase U2OS cells to induce the production of hydroxyuurea, resulting in a dose-dependent reduction of Claspin protein, followed by a reduction of phosphoserine 317Chk1. Moreover, quantitative MS showed that E3 ubiquitin ligase components RBX1,DCAF7,DCAF11, and DNA damage binding protein 1(DDB1) were reduced after P22077 treatment.

 

Solubility: Soluble in DMSO (up to 25 mg/ml)

 

Melting Point: 146-148°C

 

Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

 

Isomeric SMILES: CC(=O)C1=CC(=C(S1)SC2=C(C=C(C=C2)F)F)[N+](=O)[O-]  

 

InChIKey: RMAMGGNACJHXHO-UHFFFAOYSA-N  

 

InChI: InChI=1S/C12H7F2NO3S2/c1-6(16)11-5-9(15(17)18)12(20-11)19-10-3-2-7(13)4-8(10)14/h2-5H,1H3

 

Attribute
[Chem Name]	1-[5-(2,4-difluorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone
[Synonym]	P 22077; P-22077; P22077
[CAS No.]	1247819-59-5
[MDL No.]	MFCD22580421
[Formula]	C12H7F2NO3S2
[Molecular]	315.32
[Form]	Off-white solid
[Storage]	Sealed in dry, 2-8°C

Goods Tag