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GCN2-IN-1 (A-92) Sale

(Synonyms: A-92) 目录号 : GC32771

An inhibitor of GCN2

GCN2-IN-1 (A-92) Chemical Structure

Cas No.:1448693-69-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,062.00
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5mg
¥1,874.00
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10mg
¥2,945.00
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25mg
¥5,891.00
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50mg
¥9,818.00
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100mg
¥16,958.00
现货

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产品描述

GCN2-IN-1 is an inhibitor of general control nonderepressible 2 kinase (GCN2; IC50 = ~0.2 μM for autophosphorylation), a serine/threonine protein kinase involved in the integrated stress response.1 It also inhibits integrase phosphorylation (IC50 = ~0.2 μM for the HIV-1 enzyme). GCN2-IN-1 inhibits ELAV-like protein 1, also known as human antigen R (HuR), protein dimerization (IC50 = 4.5 μM).2 GCN2-IN-1 also decreases the viability of U251, XD456, U87, and LN-229 glioma cells (IC50s = 4.7, 2.8, 3.2, and 2.7 μM, respectively).

References:
1.Torres, C., Garling, A., Taouji, S., et al.Targeting the integrated stress response kinase GCN2 to modulate retroviral integrationMolecules26(17)5423(2021)
2.Filippova, N., Yang, X., Ananthan, S., et al.Targeting the HuR oncogenic role with a new class of cytoplasmic dimerization inhibitorsCancer Res.81(8)2220-2233(2021)

Chemical Properties

Cas No. 1448693-69-3 SDF
别名 A-92
Canonical SMILES C1(NC2=CN(C3CCOCC3)N=C2)=NC=C(N=NN4C5=CC6=C(C=C5)C=NN6)C4=N1
分子式 C19H18N10O 分子量 402.41
溶解度 DMSO : 60 mg/mL (149.10 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.485 mL 12.4251 mL 24.8503 mL
5 mM 0.497 mL 2.485 mL 4.9701 mL
10 mM 0.2485 mL 1.2425 mL 2.485 mL
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Research Update

Amino acid sensor GCN2 promotes SARS-CoV-2 receptor ACE2 expression in response to amino acid deprivation

Commun Biol 2022 Jul 1;5(1):651.PMID:35778545DOI:PMC9249868

Angiotensin-converting enzyme 2 (ACE2) has been identified as a primary receptor for severe acute respiratory syndrome coronaviruses 2 (SARS-CoV-2). Here, we investigated the expression regulation of ACE2 in enterocytes under amino acid deprivation conditions. In this study, we found that ACE2 expression was upregulated upon all or single essential amino acid deprivation in human colonic epithelial CCD841 cells. Furthermore, we found that knockdown of general control nonderepressible 2 (GCN2) reduced intestinal ACE2 mRNA and protein levels in vitro and in vivo. Consistently, we revealed two GCN2 inhibitors, GCN2iB and GCN2-IN-1, downregulated ACE2 protein expression in CCD841 cells. Moreover, we found that increased ACE2 expression in response to leucine deprivation was GCN2 dependent. Through RNA-sequencing analysis, we identified two transcription factors, MAFB and MAFF, positively regulated ACE2 expression under leucine deprivation in CCD841 cells. These findings demonstrate that amino acid deficiency increases ACE2 expression and thereby likely aggravates intestinal SARS-CoV-2 infection.