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Chemical Structure : NSC682769
Catalog No.: PC-20408Not For Human Use, Lab Use Only.
NSC682769 is a specific YAP-TEAD signaling inhibitor, blocks the association of the YAP and TEAD interaction interface, directly binds to YAP with Kd of 738 nM.
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NSC682769 is a specific YAP-TEAD signaling inhibitor, blocks the association of the YAP and TEAD interaction interface, directly binds to YAP with Kd of 738 nM.
NSC682769 blocks in vitro YAP-TEAD binding in a GST pull-down assay.
NSC682769 potently inhibits YAP expression in LN299 and GBM39 cells with IC50 of 11.8 and 5.1 nM, respectively.
NSC682769 inhibits the binding of all four TEAD members (TEAD1-4) to YAP, without appreciable effects on SMAD7, p73, FOS or TBX5 association.
NSC682769 (50 nM, 6 h) markedly reduced YAP-TEAD transcriptional activity in LN229 or GBM39 cells, resulted in a reduction of nuclear YAP and a concomitant accumulation of cytoplasmic YAP consistent.
NSC682769 inhibits proliferation, anchorage-independent growth, motility, invasive potential and induced apoptosis in glioblastoma multiforme (GBM).
NSC682769 (5 and 20 mg/kg/day) inhibited GBM tumor growth in SCID mice implanted with subcutaneous LN229 xenografts.
NSC682769 is blood-brain barrier (BBB) penetrant , twice-weekly 5 or 20 mg/kg NSC682769 increases survival of a glioma GEMM.
| M.Wt | 422.48 | |
| Formula | C27H22N2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jacquelyn T Saunders, et al. J Neurooncol. 2021 Apr;152(2):217-231.
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