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GCN2iB
CAS No. 2183470-12-2
GCN2iB( —— )
Catalog No. M26229 CAS No. 2183470-12-2
GCN2iB is an ATP-competitive inhibitor of general control nonderepressible 2 (GCN2) with an IC50 of 2.4 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 186 | In Stock |
|
| 5MG | 169 | In Stock |
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| 10MG | 274 | In Stock |
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| 25MG | 547 | In Stock |
|
| 50MG | 767 | In Stock |
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| 100MG | 1051 | In Stock |
|
| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameGCN2iB
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NoteResearch use only, not for human use.
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Brief DescriptionGCN2iB is an ATP-competitive inhibitor of general control nonderepressible 2 (GCN2) with an IC50 of 2.4 nM.
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DescriptionGCN2iB is an ATP-competitive inhibitor of general control nonderepressible 2 (GCN2) with an IC50 of 2.4 nM.(In Vitro):GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity. In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity.(In Vivo):In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth. Notably, a combination of ASNase and GCN2iB elicits potent antitumor activity (P=0.0002) with synergistic effects. In MV-4-11 and SU.86.86 xenografts, the robust antitumor activity of the combination of GCN2iB and ASNase is observed with a synergistic effect, respectively. ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation.
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In VitroGCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity. In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity.
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In VivoIn the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth. Notably, a combination of ASNase and GCN2iB elicit potent antitumor activity (P=0.0002) with synergistic effects. In MV-4-11 and SU.86.86 xenografts, robust antitumor activity of the combination of GCN2iB and ASNase is observed with synergistic effect, respectively. ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation. The combination of ASNase and GCN2iB yield survival advantage compared with the vehicle treated control with synergistic effect.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorAntibacterial
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Research Area——
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Indication——
Chemical Information
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CAS Number2183470-12-2
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Formula Weight451.83
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Molecular FormulaC18H12ClF2N5O3S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 50 mg/mL (110.66 mM)
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SMILESCOc1ncc(Cl)cc1S(=O)(=O)Nc1ccc(F)c(C#Cc2cnc(N)nc2)c1F
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Losch K. [Pharmacokinetic studies of sulfamerazine-Na, sulfaperine-Na and sulfadimidine-Na in the hen]. Arch Exp Veterinarmed. 1980;34(4):587-94. German.
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