XL177A GMP is XL177A (HY-138794) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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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- No. CAS: 2417089-74-6
- Fòrmula: C48H57ClN8O5
- Peso molecular:861.47
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
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KDM6 |
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.
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Cell Line:KELLY, NB-SD, NGP neuroblastoma cell lines
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Concentration:1 μM
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Incubation Time:14 days
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Result:Significantly reduced population doublings compared to vehicle control in all three cell lines: KELLY showed a lower number of doublings at day 10 and day 14.
Reduced doublings in NB-SD at day 5, day 10, and day 14.
Reduced doublings in NGP at day 5, day 10, and day 14.
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Cell Line:NB-SD neuroblastoma cell lines
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Concentration:1 μM
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Incubation Time:10 days
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Result:Induced neurite extensions in NB-SD cells, which was enhanced by NGF supplementation.
Increased expression of neuronal differentiation markers SEMA6B, CHGA, and GAP43 compared to vehicle control.
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Cell Line:Huh7.5 cells
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Concentration:7.5 µM, 15 µM
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Incubation Time:2 days
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Result:Significantly reduced ACE2 and DPP4 mRNA levels in Huh7.5 cells.
Dose-dependently inhibited entry of SARS-CoV-2-S and MERS-CoV-S pseudoviruses, reducing luciferase activity relative to control.
Chemical Information
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No. CAS 2417089-74-6
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Peso molecular 861.47
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Fòrmula C48H57ClN8O5
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XL177A (GMP) Related Classifications
HY-138794G Related Classifications
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Keywords
- XL177A (GMP)
- 2417089-74-6
- Deubiquitinase
- SARS-CoV
- Histone Demethylase
- CCD 841 CoN normal colonic epithelial cells
- NGP neuroblastoma cell line
- KELLY neuroblastoma cell line
- coronaviruses
- SW480 colorectal carcinoma cells
- APC-mutated colorectal carcinoma cells
- SARS-CoV-2 variants
- neuroblastoma
- NB-SD neuroblastoma cell line
- USP7
- Inhibitor
- inhibitor
- inhibit