Description
GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.
Product information
CAS Number: 2183470-12-2
Molecular Weight: 451.83
Formula: C18H12ClF2N5O3S
Chemical Name: N-{3-[2-(2-aminopyrimidin-5-yl)ethynyl]-2,4-difluorophenyl}-5-chloro-2-methoxypyridine-3-sulfonamide
Smiles: COC1=NC=C(Cl)C=C1S(=O)(=O)NC1=CC=C(F)C(C#CC2C=NC(N)=NC=2)=C1F
InChiKey: JGHVXJKGYJYWOP-UHFFFAOYSA-N
InChi: InChI=1S/C18H12ClF2N5O3S/c1-29-17-15(6-11(19)9-23-17)30(27,28)26-14-5-4-13(20)12(16(14)21)3-2-10-7-24-18(22)25-8-10/h4-9,26H,1H3,(H2,22,24,25)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 16.67 mg/mL (36.89 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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 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.
Products are for research use only. Not for human use.
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