1. Cell Cycle/DNA Damage Apoptosis
  2. Deubiquitinase Apoptosis
  3. YCH2823

YCH2823 is an inhibitor of USP7 (IC50 = 49.6 nM; Kd = 0.117 μM). YCH2823 shows significant efficacy in inhibiting TP53 wild-type and mutant tumors, with approximately 5-fold higher potency than FT671. YCH2823 induce apoptosis. YCH2823 synergistic effects with mTOR inhibitors.

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YCH2823 Chemical Structure

YCH2823 Chemical Structure

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5 mg USD 330 In-stock
10 mg USD 548 In-stock
25 mg USD 1152 In-stock
50 mg USD 1844 In-stock
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200 mg   Get quote  

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Description

YCH2823 is an inhibitor of USP7 (IC50 = 49.6 nM; Kd = 0.117 μM). YCH2823 shows significant efficacy in inhibiting TP53 wild-type and mutant tumors, with approximately 5-fold higher potency than FT671. YCH2823 induce apoptosis. YCH2823 synergistic effects with mTOR inhibitors[1].

IC50 & Target

USP7

49.6 nM (IC50)

In Vitro

YCH2823 interacts directly with USP7 with high affinity and effectively inhibits its enzymatic activity. Potentially low toxicity to IMR-90 cells[1].
YCH2823 (0-10 μM; 72 h or 5 days) demonstrates significant dose-dependent inhibition of cell proliferation across different cancer cell lines. High sensitivity to TP53 wild-type, mutant. [1].
YCH2823 (0-1 μM; 1-48 h ) affects protein stability and cell cycle regulation. It leads to decrease in MDM2 protein levels within 1 h and elevation of p53 and p21 levels in LNCaP cells. In MM.1S cells, although p53 protein levels do not change significantly, p21 levels are independently higher, indicating a possible p53-independent pathway for p21 induction.n the TP53 mutant Capan-1 resulted in a significant decrease in Rad18 and DNMT1 proteins, along with an increase in p21 levels[1].
YCH2823 (0-1 μM; 6-48 h ) causes up-regulation of BCL6 protein and mRNA. It induces apoptosis by increasing the proportion of cells in G1 phase in CHP212 cells and IMR-32 cells. The manipulations of DNMT1, p53, and p21 has no impact on the YCH2823-induced upregulation of BCL6[1].
YCH2823 with Rapamycin (HY-10219) or Ridaforolimus (HY-50908) results in a synergistic effect, where is more effective than either agent alone[1].

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

Apoptosis Analysis[1]

Cell Line: CHP-212 cells
Concentration: 0, 0.03, 0.1, 0.3, 1 μM
Incubation Time: 48 h
Result: Induced significant apoptosis, demonstrating YCH2823’s capacity to induce programmed cell death.

Western Blot Analysis[1]

Cell Line: CHP212 cells
Concentration: 0, 0.1, 0.3, 1 μM
Incubation Time: 6-48 h
Result: YCH2823 led to a significant upregulation of BCL6 protein and mRNA, observable as early as 6 hours post-treatment and sustained over time. This suggests that YCH2823 may impact transcriptional regulation related to BCL6. Also led the decreases in Rad18 and DNMT1 suggesting effects on DNA repair mechanisms.
Molecular Weight

500.59

Formula

C29H32N4O4

Appearance

Solid

Color

Off-white to light yellow

SMILES

COC1=CC=C(C=C1)N2C=CC3=C2N=CN(C3=O)CC4(CCN(CC4)C(C[C@H](C5=CC=CC=C5)C)=O)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 : 100 mg/mL (199.76 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 1.9976 mL 9.9882 mL 19.9764 mL
5 mM 0.3995 mL 1.9976 mL 3.9953 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: ≥ 5 mg/mL (9.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (9.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 1.9976 mL 9.9882 mL 19.9764 mL 49.9411 mL
5 mM 0.3995 mL 1.9976 mL 3.9953 mL 9.9882 mL
10 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9941 mL
15 mM 0.1332 mL 0.6659 mL 1.3318 mL 3.3294 mL
20 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4971 mL
25 mM 0.0799 mL 0.3995 mL 0.7991 mL 1.9976 mL
30 mM 0.0666 mL 0.3329 mL 0.6659 mL 1.6647 mL
40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
50 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9988 mL
60 mM 0.0333 mL 0.1665 mL 0.3329 mL 0.8324 mL
80 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
100 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4994 mL
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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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Product Name:
YCH2823
Cat. No.:
HY-158039
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