2417089-73-5
Chemical Structure
(Rac)-XL177A
- CAS No.: 2417089-73-5
- Formula:C48H57ClN8O5
- Molecular Weight:861.47
InChIKey: UYJWYMWIVMCGQZ-UHFFFAOYSA-N
SMILES: O=C(C(C=CC1=C2Cl)=CC1=NC3=C2CCCC3)NCCCC(CC4=CC=CC=C4)C(N5CCC(CN6C=NC7=C(C=CC(NC(CCN8CCN(C)CC8)=O)=C7)C6=O)(O)CC5)=O
Biological Activity: (Rac)-XL177A is the racemic isomer of XL177A (HY-138794). 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].
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(Rac)-XL177A | (Rac)-XL177A is the racemic isomer of XL177A (HY-138794). 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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References
- [1]. Pirttikoski A, Gall-Mas L, Senkowski W, et al. Conserved cell state dynamics reveal targetable resistance patterns in ovarian high-grade serous carcinoma[J]. bioRxiv, 2025: 2025.06. 13.659489.
- [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]
- [4]. Huang M Z, et al. Antagonistic ubiquitin switching by USP7 and RNF40 orchestrates KDM6A homeostasis to license coronavirus susceptibility[J]. Advanced Science, 2026, 13(23): e18058.
