YCH2823
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.87%
- 分子式: C29H32N4O4
- 分子量:500.59
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Ubiquitination Compound Library
HY-L050
-
Metabolic Enzyme Compound Library
HY-L146
-
Protease Inhibitor Library
HY-L147
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
生物活性
|
USP7 49.6 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | IC50 |
102.4 nM
Compound: Z8
|
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 3 days by SRB assay
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 3 days by SRB assay
|
[PMID: 39133975] |
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.
-
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.
-
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.
化学情報
-
性状 Solid
-
分子量 500.59
-
分子式 C29H32N4O4
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
-
データシート (274 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
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 |
YCH2823 関連分類
HY-158039 関連分類
Powered by Bioz