A GCN2 inhibitor
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GCN2iB

Item No. 35897

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[2-(2-amino-5-pyrimidinyl)ethynyl]-2,4-difluorophenyl]-5-chloro-2-methoxy-3-pyridinesulfonamide
CAS Number
2183470-12-2
Molecular Formula
C18H12ClF2N5O3S
Formula Weight
451.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
O=S(NC1=CC=C(C(C#CC2=CN=C(N)N=C2)=C1F)F)(C3=CC(Cl)=CN=C3OC)=O
InChi Code
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)
InChi Key
JGHVXJKGYJYWOP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $54

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    1 mg

    $103

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    5 mg

    $351

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    10 mg

    $647

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    Product Description

    GCN2iB is an inhibitor of general control nonderepressible 2 kinase (GCN2; IC50 = 2.4 nM).1 It is selective for GCN2 over a panel of 465 kinases but does inhibit MAP2K5, eukaryotic translation initiation factor 2α kinase 2 (EIF2AK2), and MAP3K20 at 1 µM. GCN2iB (1 µM), in combination with L-aspariginase, reduces the viability of mouse embryonic fibroblasts (MEFs). It decreases the levels of activating transcription factor 4 (ATF4) and phosphorylated GCN2 in combination with L-aspariginase in CCRF CEM leukemia cells when used at a concentration of 0.4 µM. In vivo, GCN2iB (10 mg/kg twice per day), in combination with L-aspariginase, reduces tumor volume in CCRF CEM and MV4-11 leukemia mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nakamura, A., Nambu, T., Ebara, S., et al. Inhibition of GCN2 sensitizes ASNS-low cancer cells to asparaginase by disrupting the amino acid response. Proc. Natl. Acad. Sci. USA 115(33), E7776-E7785 (2018).