• Search chemicals, activators, Inhibitors, APIs, intermediates and raw materials.

1247819-59-5 (P 22077)

1

Identification

P 22077 P 22077
Name P 22077
Formula C12H7F2NO3S2
MW 315.32
CAS No. 1247819-59-5
EINECS
Smiles CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O
Synonyms P22077;P-22077; 1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone
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
2

Introduction

P22077 is a potent inhibitor of ubiquitin-specific protease (USP) 7 (EC50=8.6 uM), P22077 also inhibits the closely related deubiquitinase (DUB) USP47. IC50 Value: 8.6 uM (EC50) [1] Target: USP7; USP47 in vitro: P22077 potently induces apoptosis in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression.

Background Information

P22077 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor. P22077 stabilized p53 by inducing HDM2 protein degradation in NB cells. P22077 also significantly augmented the cytotoxic effects of doxorubicin (Dox) and etoposide (VP-16) in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression. In an in vivo orthotopic NB mouse model, P22077 significantly inhibited the xenograft growth of three NB cell lines. P22077 treatment of U2OS cells during release from G1/S arrest induces with hydroxyurea resulted in a dose-dependent loss of claspin protein and a concomitant decrease in phospho Serine 317 Chk1. ......by AbMole BioScience
P 22077 is a cell-permeable inhibitor of the ubiquitin-specific protease (IC?? = 8.6 μM) and the closely related deubiquitinase (DUB) USP47. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
P22077 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor. P22077 potently induces apoptosis in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression. P2207 ......by BOC Sciences
A cell-permeable inhibitor of the ubiquitin-specific protease (IC₅₀ = 8.6 µM) and the closely related deubiquitinase (DUB) USP47. P22077 displays weak or no inhibition (EC₅₀>50 µM) towards a panel of 14 isopeptidases and other proteases. Inhibits USP7-mediated p53 deubiquitination. ......by BioVision, Inc.,
P 22077 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 8.01 μM, and also inhibits USP47, with an EC50 of 8.74 μM. ......by MedChemexpress Co., Ltd.
P22077 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor. P22077 potently induces apoptosis in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression. P22077 also significantly augmented the cytotoxic effects of doxorubicin (Dox) and etoposide (VP-16) in NB cells with an intact USP7-HDM2-p53 axis. Moreover, P22077 was found to be able to sensitize chemoresistant LA-N-6 NB cells to chemotherapy. In an in vivo orthotopic NB mouse model, P22077 significantly inhibited the xenograft growth of three NB cell lines. USP7-specific inhibitors like P22077 may serve not only as a stand-alone therapy but also as an effective adjunct to current chemotherapeutic regimens for treating NB with an intact USP7-HDM2-p53 axis. ......by MedKoo Biosciences, Inc.
P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47. ......by Selleck Chemicals LLC
P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47. ......by Target Molecule Corp.
Inhibitor of ubiquitin-specific protease (USP) 7 (EC50 = 8.6 μM); also inhibits the closely related deubiquitinase (DUB) USP47. Demonstrates downstream inhibition of HDM2 and claspin in vitro. Inhibits USP7-mediated p53 deubiquitination. Blocks deubiquitination of Tip60 (KAT5) histone lysine acetyltransferase. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000014768

Storage condition

Store at +4°C by Tocris Bioscience Inc.

Solubility

DMSO 63 mg/ml; Water <1 mg/ml by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 63 mg/mL (199.79 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
Soluble to 100 mM in DMSO by Tocris Bioscience Inc.
5

Mechanism and Indication

Signaling Pathways Cell Cycle/DNA Damage
Target Deubiquitinase
Research Area Cancer
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
P 22077 - Discovery
P 22077 - No Development Reported
7

Safety Data of P 22077

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences 100mg/USD298(In stock)
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD94();50mg/USD354() USA
MedChemexpress Co., Ltd. 10mg/USD94();50mg/USD354() USA
MedKoo Biosciences, Inc. USA
Selleck Chemicals LLC 10mg/USD147(In stock);50mg/USD370(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD94();50mg/USD354() China
Target Molecule Corp. 10mg/USD125();25mg/USD244();50mg/USD328() USA
Tocris Bioscience Inc. USA
10

Related Products

Other Forms of 1247819-59-5

Name CAS No Formula MW

Recommended Compounds in Deubiquitinase

Name CAS No Formula MW
DUBs-IN-2 924296-19-5 C15H9N5O 275.26
ML-323 1572414-83-5 C23H24N6 384.48
HBX 19818 1426944-49-1 C25H28ClN3O 421.96
b-AP15 1009817-63-3 C22H17N3O6 419.39
SJB2-043 63388-44-3 C17H9NO3 275.26
P005091 882257-11-6 C12H7Cl2NO3S2 348.22
IU1 314245-33-5 C18H21FN2O 300.37
PR-619 2645-32-1 C7H5N5S2 223.28
USP7/USP47 inhibitor 1247825-37-1 C18H11Cl2N3O3S3 484.4
BAY 11-7082 19542-67-7 C10H9NO2S 207.249
DUBs-IN-3 924296-17-3 C16H9N5O 287.28
DUBs-IN-1 924296-18-4 C20H11N5O 337.33
WP1130 856243-80-6 C19H18BrN3O 384.27
VLX1570 1431280-51-1 C23H17F2N3O6 469.39
LDN-57444 668467-91-2 C17H11Cl3N2O3 397.64
USP7-IN-1 1381291-36-6 C23H24ClN3O3 425.91
NSC632839 157654-67-6 C21H22ClNO 339.8585
ML364 1991986-30-1 C24H18F3N3O3S2 0.0
Cadmium pyrithione C10H8CdN2O2S2 364.72
IU1-47 670270-31-2 C19H23ClN2O 330.85

Recommended Compounds in Same Indication

Name CAS No Formula MW
11

Route of Synthesis

12

References

13

More Information

P 22077

Tags: buy 1247819-59-5 IC50 | 1247819-59-5 price | 1247819-59-5 cost | 1247819-59-5 solubility | 1247819-59-5 purchase | 1247819-59-5 manufacturer | 1247819-59-5 research buy | 1247819-59-5 order | 1247819-59-5 MSDS | 1247819-59-5 chemical structure | 1247819-59-5 Storage condition | 1247819-59-5 molecular weight | 1247819-59-5 mw | 1247819-59-5 datasheet | 1247819-59-5 supplier | 1247819-59-5 cell line | 1247819-59-5 NMR | 1247819-59-5 MS | 1247819-59-5 IR | 1247819-59-5 solubility | 1247819-59-5 Safe information | 1247819-59-5 Qc and Spectral Information | 1247819-59-5 Clinical Information | 1247819-59-5 Clinical Trial | 1247819-59-5 Route of Synthesis | 1247819-59-5 storage condition | 1247819-59-5 diseases and conditions | 1247819-59-5 flash point | 1247819-59-5 boiling point | 1247819-59-5 melting point | 1247819-59-5 storage condition | 1247819-59-5 brand