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[CAS NO. 1247819-59-5] P22077
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-13865 |
| Brand: | MCE |
| CAS: | 1247819-59-5 |
Overview
| MDL | MFCD22580421 |
|---|---|
| Molecular Weight | 315.32 |
| Molecular Formula | C12H7F2NO3S2 |
| SMILES | CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O |
11 Publications Citing Use of MCE
- [1]Nat Chem Biol. 2017 Dec;13(12):1207-1215.
- [2]Nat Commun. 2023 Feb 9;14(1):731.
- [3]Nat Commun. 2022 Mar 31;13(1):1700.
- [4]Cell Chem Biol. 2021 Apr 27;S2451-9456(21)00213-0.
- [5]Haematologica. 2019 Nov;104(11):2178-2187.
- [6]Cell Death Dis. 2022 Aug 10;13(8):698.
- [7]J Med Chem. 2022 Oct 11.
- [8]Br J Cancer. 2020 Apr;122(8):1175-1184.
- [9]Mol Neurobiol. 2022 Jun 9.
- [10]Med Oncol. 2022 Feb 12;39(5):55.
- [11]J Oncol. 2022 Jun 23;2022:8724933.
Summary
P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC 50 of 8.01 μM. P 22077 also inhibits USP47 with an EC 50 of 8.74 μM.
IC50 & Target
EC50: 8.01 μM (USP7), 8.74 μM (USP47) [1]
In Vitro
P 22077 is an inhibitor of USP7 and DUB USP47, with EC 50 s of 8.01 μM and 8.74 μM, respectively. P 22077 (15-45 μM) inhibits a much smaller subset of DUBs. P 22077 (25 μM) causes DUBs inhibition in HEK293T cells [1] . P 22077 (0-20 μM) greatly reduces the cell viability of Neuroblastoma (NB) cells including IMR-32, NGP, CHLA-255, and SH-SY5Y cells but without NB-19 and SK-N-AS cells. P 22077 (10 μM) increases p53 activity and induces apoptosis in p53 wild-type and HDM2-expressing NB cells. P 22077 (5 μM) enhances the cytotoxic effect of Dox and VP-16 on NB cells, and enhances Dox- and VP-16-induced p53-mediated apoptosis [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
P 22077 (15 mg/kg, i.p. 21 days) shows potent antitumor activities in an xenograft mouse model bearing IMR-32-derived tumors; P 22077 also exhibits antitumor effects after treatment at 10 mg/kg for 14 days in mice bearing SH-SY5Y-derived tumors, and at 20 mg/kg for 12 days in mice bearing NGP-derived tumors [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 158.57 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1714 mL | 15.8569 mL | 31.7138 mL |
| 5 mM | 0.6343 mL | 3.1714 mL | 6.3428 mL |
| 10 mM | 0.3171 mL | 1.5857 mL | 3.1714 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution
References
- [1] Altun M, et al. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol. 2011 Nov 23;18(11):1401-12.
- [2] Fan YH, et al. USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis. Cell Death Dis. 2013 Oct 17;4:e867.
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