GSK235
GSK235 is an orally active, selective and allosteric endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with pIC50 values of 8.45 and 7.59 for human and mouse ERAP1, respectively. GSK235 exhibits over 1000-fold selectivity for the two most homologous enzymes, ERAP2 and IRAP. GSK235 can regulate the immunopeptidome of cancer cells and enhance cancer cell antigenicity. GSK235 can be used for the study of colorectal cancer and arthritis.
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- 화학식: C21H30N4O3
- 분자량:386.49
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
GSK235 (compound 21) (1 μM, 0.61 μM; 1 hour, 24 h) demonstrates potent inhibition of ERAP1 and ERAAP with high selectivity in human and mouse enzymes[1].
GSK235 shows a pIC50 value of 7.25 in HeLa antigen presentation assay[1].
GSK235 (1 µM; 30 days) affects a wider variety of immunopeptides in CT26 tumor cells. Substantial evidence of peptide lengthening was observed; for example, significant increases in 10-mer and 11-mer peptides were accompanied by decreases in 9-mer and 8-mer peptides[1].
GSK235 shows no activity against the hERG channel[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Note | Cmax | AUC0-t |
|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 文献审核 | 8516 ng/mL | 15440 ng·h/mL |
GSK235 (30, 90, 270 mg/kg, oral, twice daily; from day 18 to day 36) reduces arthritis scores and immune activation in the collagen-induced arthritis (CIA) model in a dose-dependent mannerwithout evidence of autoimmune exacerbation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c (6-8 weeks old) were inoculated subcutaneously in the right hind flank with 5x104 CT26 cells[1]
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Dosage:30 mg/kg, 90 mg/kg, 270 mg/kg
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Administration:Oral; twice daily (BID); for 17 days
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Result:Observed with significant reduction in tumor volume by termination of the study, day 17, at the highest dose (270 mg/kg) and no significant dose-dependent body-weightchanges were observed.
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Animal Model:Male DBA/1OlaHsd (6-7 weeks old) (Collagen-induced arthritis (CIA) model)[1]
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Dosage:30 mg/kg, 90 mg/kg, 270 mg/kg
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Administration:Oral; twice daily (BID); from day 18 to day 36
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Result:Showed a dose-dependent reduction in arthritis scores, with the highest dose (270 mg/kg) achieving a reduction comparable to the TNF inhibitor Enbrel.
Also reduced anti-collagen type II IgG levels, IL-12p40, and IL-6 levels, and decreased MHC-I expression on B cells and cDCs.
No exacerbation of autoimmune responses was observed.
Chemical Information
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분자량 386.49
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화학식 C21H30N4O3
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SMILES
CC1=C(C#N)C(N2C[C@H](C(C)C)[C@@H](C(O)=O)C2)=NC(NC3(C)CCOCC3)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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