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Chemical Structure : GCN2 inhibitor 39
Catalog No.: PC-49370Not For Human Use, Lab Use Only.
GCN2 inhibitor 39 is a highly potent and selective, orally active inhibitor of general control nonderepressible 2 (GCN2) with IC50 of 5 nM.
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GCN2 inhibitor 39 is a highly potent and selective, orally active inhibitor of general control nonderepressible 2 (GCN2) with IC50 of 5 nM.
GCN2 inhibitor 39 displays excellent selectivity against its closely related Integrated Stress Response (ISR) family members heme-regulated inhibitor kinase (HRI), PKR, and (PKR)-like endoplasmic reticulum kinase (PERK).
GCN2 inhibitor 39 engages GCN2 at levels ≥80% with an oral dose of 15 mg/kg BID in mice.
GCN2 inhibitor 39 alleviates MDSC-related T cell suppression and restore T cell proliferation, similar to the effect seen in MDSCs from GCN2 knockout mice.
GCN2 inhibitor 39 (50 mg/kg, BID) demonstrates significant tumor growth inhibition (TGI) as a single agent in the LL2 syngeneic mouse model, also enhances TGI mediated by anti-VEGFR.
| M.Wt | 527.445 | |
| Formula | C22H23BrN8OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jeffrey J. Jackson, et al. Journal of Medicinal Chemistry, 2022
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