1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. XL177A

XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34 nM. XL177A elicits cancer cell killing through a p53-dependent mechanism.

For research use only. We do not sell to patients.

XL177A Chemical Structure

XL177A Chemical Structure

CAS No. : 2417089-74-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 360 In-stock
Solution
10 mM * 1 mL in DMSO USD 360 In-stock
Solid
1 mg USD 123 In-stock
5 mg USD 240 In-stock
10 mg USD 380 In-stock
25 mg USD 760 In-stock
50 mg USD 1210 In-stock
100 mg USD 1940 In-stock
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34 nM. XL177A elicits cancer cell killing through a p53-dependent mechanism[1].

In Vitro

XL177A is a potent USP7 inhibitor and p53 stabilizer in cyto. XL177A suppresses cancer cell growth predominantly through a p53-dependent mechanism. XL177A labels the catalytic cysteine, C223, of USP7 with exquisite selectivity for USP7 across the DUBome and human proteome[1].
XL177A (1 μM) induces complete G1 arrest in MCF7 cells after 24 hours[1].
Treatment of MCF7 cells, which express WT TP53, with XL177A (0.001- 10 μM) induces rapid degradation of HDM2 within 2 hours, followed by increases in p53 and downstream p21 protein levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MCF7 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 18-24 hours
Result: The p53 and p21 protein levels remained high, but MDM2 protein levels matched DMSO control.
Molecular Weight

861.47

Formula

C48H57ClN8O5

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C(C=CC1=C2Cl)=CC1=NC3=C2CCCC3)NCCC[C@@H](CC4=CC=CC=C4)C(N5CCC(CN6C=NC7=C(C=CC(NC(CCN8CCN(C)CC8)=O)=C7)C6=O)(O)CC5)=O

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
In Vitro: 

DMSO : 25 mg/mL (29.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1608 mL 5.8040 mL 11.6081 mL
5 mM 0.2322 mL 1.1608 mL 2.3216 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (2.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (2.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1608 mL 5.8040 mL 11.6081 mL 29.0202 mL
5 mM 0.2322 mL 1.1608 mL 2.3216 mL 5.8040 mL
10 mM 0.1161 mL 0.5804 mL 1.1608 mL 2.9020 mL
15 mM 0.0774 mL 0.3869 mL 0.7739 mL 1.9347 mL
20 mM 0.0580 mL 0.2902 mL 0.5804 mL 1.4510 mL
25 mM 0.0464 mL 0.2322 mL 0.4643 mL 1.1608 mL
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XL177A Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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XL177A
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