Home Ubiquitin DUB inhibitor XL177A For research use only.

XL177A

XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.

XL177A Chemical Structure

XL177A Chemical Structure

CAS: 2417089-74-6

Purity & Quality Control

Batch: S896701 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 98.77%
98.77

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Signaling Pathway

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Biological Activity

Description XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.
Targets
USP7 [1]
(Cell-free assay)
0.34 nM
In vitro
In vitro

Evaluation of the cellular effects of XL177A reveals that selective USP7 inhibition suppresses cancer cell growth predominantly through a p53-dependent mechanism: XL177A specifically upregulates p53 transcriptional targets transcriptome-wide, hotspot mutations in TP53 but not any other genes predict response to XL177A across a panel of ~500 cancer cell lines, and TP53 knockout rescues XL177A-mediated growth suppression of TP53 wild-type (WT) cells.[1]
Cell Research Cell lines MCF7 cells
Concentrations 0.1 μM, 1 μM
Incubation Time 24 h
Method

MCF7 cells are seeded in a 384 well plate at 2500 cells per well, allowed to adhere for 24 hours, then treated with two doses in triplicate of XL177A, XL177B, Nutlin-3, or DMSO. After 24 hours of treatment, an EL405x plate washer is used to aspirate the media and wash once with PBS.

Chemical Information & Solubility

Molecular Weight 849.46 Formula

C47H57ClN8O5
CAS No. 2417089-74-6 SDF --
Smiles CN1CCN(CC1)CCC(=O)NC2=CC3=C(C=C2)C(=O)N(CC4(O)CCN(CC4)C(=O)C(CCCNC(=O)C5=CC6=C(C=C5)[Cl]=C7CCCCC7=N6)CC8=CC=CC=C8)C=N3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (117.72 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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