XL177A
Based on 6 publication(s) in Google Scholar
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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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: 99.60%
- CAS 番号: 2417089-74-6
- 分子式: C48H57ClN8O5
- 分子量:861.47
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 XL177A
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生物活性
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.
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Cell Line:MCF7 cells
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:18-24 hours
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Result:The p53 and p21 protein levels remained high, but MDM2 protein levels matched DMSO control.
化学情報
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CAS 番号 2417089-74-6
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性状 Solid
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分子量 861.47
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分子式 C48H57ClN8O5
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Color White to light yellow
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Commun
Targeted degradation of USP7 in solid cancer cells reveals distinct effects of deubiquitinase degraders and inhibitors. [Abstract]2026 May 13;17(1):4331. PMID: 42129197 -
Redox Biol
USP20 governs tyrosine kinase inhibitors resistance through ferroptosis evasion by targeting GPX4 in cancers. [Abstract]2026 May:92:104086. PMID: 41844497 -
Adv Sci (Weinh)
Antagonistic Ubiquitin Switching by USP7 and RNF40 Orchestrates KDM6A Homeostasis to License Coronavirus Susceptibility. [Abstract]2026 Apr;13(23):e18058. PMID: 41691482 -
Cell Rep
2024 Oct 15;43(11):114872. PMID: 39412987 -
J Med Virol
2025 Jan;97(1):e70168. PMID: 39821265 -
Anim Cells Syst
Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]2024 May 11;28(1):237-250. PMID: 38741950
溶剤 & 溶解度
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)
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: ≥ 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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データシート (273 KB)
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SDS (251 KB)
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- Korean - KR (251 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Abdrabou AM, et al. nuPRISM: Microfluidic Genome-Wide Phenotypic Screening Platform for Cellular Nuclei. ACS Cent Sci. 2022;8(12):1618-1626. [Content Brief]
[3]. Cmarik EA, et al. Inhibition of USP7 destabilizes the noncanonical PRC1.1 complex and induces neuroblastoma differentiation. Mol Cancer Res. Published online March 19, 2026. [Content Brief]
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 |
XL177A 関連分類
HY-138794 関連分類
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