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Home - Products - MAPK/ERK Signaling - Ras - NSC 658497

NSC 658497

CAS No. 909197-38-2

NSC 658497( NSC658497 )

Catalog No. M16534 CAS No. 909197-38-2

NSC 658497 is a small molecule inhibitor of Ras GEF, SOS1, binds to SOS1 with Kd of 7 uM but no H-Ras.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    NSC 658497
  • Note
    Research use only, not for human use.
  • Brief Description
    NSC 658497 is a small molecule inhibitor of Ras GEF, SOS1, binds to SOS1 with Kd of 7 uM but no H-Ras.
  • Description
    NSC 658497 is a small molecule inhibitor of Ras GEF, SOS1, binds to SOS1 with Kd of 7 uM but no H-Ras, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity; showes dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation.
  • In Vitro
    NSC-658497 (0-20 μM; 2 hours; NIH/3T3 cells) dose-dependently inhibits EGF (50 ng/mL)-stimulated Ras, but not EGFR activation.Concomitant to Ras inhibition, NSC-658497 (0-100 μM; 2 hours; NIH/3T3 cells) dose-dependently inhibited the EGF activated, Ras downstream targets ERK1/2 and AKT.Consistent with these results, NSC-658497 dose-dependently suppressed Ras signaling mediated by the overexpression of an active SOS1 mutant (W729L), originally identified in Noonan’s Syndrome, in human embryonic kidney cells.NSC-658497 dose-dependently inhibits 50 nM SOS1-cat mediated GDP/GTP nucleotide exchange upon 2 μM H-Ras (aa. 1-166) in the BODIPYFL-GDP dissociation assay (IC50=15.4μM).NSC-658497 (0-60 μM; 3 days; PC-3 and DU-145 cells) inhibits proliferation of prostate cancer cells.NSC-658497 (0-60 μM; 2 hours; PC-3 and DU-145 cells) dose-dependently inhibits Ras-GTP activity and the downstream p-ERK1/2 and p-Akt activities. Cell Proliferation AssayCell Line:PC-3 and DU-145 cells Concentration:0-60 μMIncubation Time:3 days Result:Dose-dependently inhibited proliferation of PC-3 and DU-145 cells.Western Blot Analysis Cell Line:PC-3 and DU-145 cells Concentration:0-60 μM Incubation Time:2 hours Result:Dose-dependently inhibited Ras-GTP activity and the downstream p-ERK1/2 and p-Akt activities.
  • In Vivo
    ——
  • Synonyms
    NSC658497
  • Pathway
    MAPK/ERK Signaling
  • Target
    Ras
  • Recptor
    Ras
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    909197-38-2
  • Formula Weight
    438.428
  • Molecular Formula
    C20H10N2O6S2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C1/C(C(C2=C(O1)C=CC=C2)=O)=C\N(C/3=O)C(SC3=C/C4=CC=C([N+]([O-])=O)C=C4)=S
  • Chemical Name
    (Z)-3-(((Z)-5-(4-nitrobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)methylene)chroman-2,4-dione

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Evelyn CR, et al. Chem Biol. 2014 Dec 18;21(12):1618-28.
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