2. Cell Cycle/DNA Damage Epigenetics Anti-infection
  3. Deubiquitinase Histone Demethylase SARS-CoV
  4. XL177A

XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections.

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XL177A

XL177A Estructura química

No. CAS : 2417089-74-6

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtener un presupuesto  
500 mg   Obtener un presupuesto  

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Revisión del cliente

Based on 5 publication(s) in Google Scholar

Other Forms of XL177A:

XL177A Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas Deubiquitinase:

Ver todas las isoformas
USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15 USP28 USP25

Ver todos los productos específicos de isoformas Histone Demethylase:

Ver todas las isoformas
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • Actividad biológica

  • Pureza y Documentación

  • Referencias

  • Revisión del cliente

Descripciòn

XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections[1][2][3][4].

In Vitro

XL177A GMP (1-10 μM; 7 d) enhances the cytotoxicity of carboplatin and the chemosensitivity of stem cell-like organoids derived from ovarian cancer patients. XL177A GMP also inhibits the TNFα/NF-κB signaling pathway, upregulates TNF-related apoptotic pathways, and induces cells to transition to an early stem cell-like state[1].
XL177A GMP (5 μM) potently inhibits the proliferation of SW480 colorectal cancer cells carrying APC mutations, while exerting minimal effects on CCD 841 CoN normal colonic epithelial cells with wild-type APC[2].
XL177A GMP (1 μM; 14 d) significantly reduces the population doubling number of KELLY, NB-SD and NGP neuroblastoma cell lines[3].
XL177A GMP (1 μM; 10 d) induces neuronal differentiation in NB-SD neuroblastoma cells, resulting in neurite formation and upregulated expression of the differentiation markers SEMA6B, CHGA and GAP43[3].
XL177A GMP (7.5-15 μM; 2 d) reduces the expression of ACE2 and DPP4 in Huh7.5 cells, and inhibits the entry of SARS-CoV-2-S and MERS-CoV-S pseudoviruses at concentrations of 7.5 and 15 μM after 2 days of pretreatment[4].

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

XL177A Related Antibodies

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.
Peso molecular

861.47

Fòrmula

C48H57ClN8O5
No. CAS
Appearance

Solid

Color

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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 12.5 mg/mL (14.51 mM; ultrasonic and warming and heat to 60°C; 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 1.25 mg/mL (1.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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 +
% 
+
%
Tween-80 +
%
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.
Pureza y Documentación

Purity: 99.60%

SDS (251 KB)

COA (243 KB) HNMR (297 KB) RP-HPLC (296 KB) LCMS (118 KB)

Instrucciones de manejo (2659 KB)
Referencias

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
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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.

Keywords:

XL177A2417089-74-6DeubiquitinaseHistone DemethylaseSARS-CoVDUBsSARS coronavirusUSP7cancerp53MCF7Inhibitorinhibitorinhibit

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Nombre del producto:
XL177A
Cat. No.:
HY-138794
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SAFETY DATA SHEET (SDS)

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