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

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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XL177A

XL177A Chemical Structure

CAS No. : 2417089-74-6

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XL177A Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

View All Isoforms
USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15

View All Histone Demethylase Isoform Specific Products:

View All Isoforms
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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Description

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[1][2][3][4].

IC50 & Target

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.

XL177A Related Antibodies

Cell Viability Assay[3]

Cell Line: KELLY, NB-SD, NGP neuroblastoma cell lines
Concentration: 1 μM
Incubation Time: 14 days
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.

Cell Differentiation Assay[3]

Cell Line: NB-SD neuroblastoma cell lines
Concentration: 1 μM
Incubation Time: 10 days
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.

Real Time qPCR[4]

Cell Line: Huh7.5 cells
Concentration: 7.5 µM, 15 µM
Incubation Time: 2 days
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.
Molecular Weight

861.47

Formula

C48H57ClN8O5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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XL177A Related Classifications

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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.

Keywords:

XL177A (GMP)2417089-74-6DeubiquitinaseSARS-CoVHistone DemethylaseDUBsSARS coronavirusCCD 841 CoN normal colonic epithelial cellsNGP neuroblastoma cell lineKELLY neuroblastoma cell linecoronavirusesSW480 colorectal carcinoma cellsAPC-mutated colorectal carcinoma cellsSARS-CoV-2 variantsneuroblastomaNB-SD neuroblastoma cell lineUSP7Inhibitorinhibitorinhibit

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