NSAH?

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NSAH 是一种人核糖核苷酸还原酶 (hRR) 的非核苷抑制剂。无细胞 IC50 为 32 μM，基于细胞的 IC50 约为 250 nM。萘基水杨酰腙 (NSAH) 是一种独特的非核苷小分子 hRR 抑制剂，使用虚拟筛选、结合亲和力、抑制和细胞毒性测定。 NSAH 与 hRRM1 结合的表观解离常数为 37 μM，稳态动力学揭示了竞争性抑制模式。

NSAH is a nonnucleoside inhibitor of human ribonucleotide reductase (hRR).with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively.A unique nonnucleoside small-molecule hRR inhibitor, naphthyl salicylic acyl hydrazone (NSAH), using virtual screening, binding affinity, inhibition, and cell toxicity assays.?NSAH binds to hRRM1 with an apparent dissociation constant of 37 μM, and steady-state kinetics reveal a competitive mode of inhibition.?A 2.66-? resolution crystal structure of NSAH in complex with hRRM1 demonstrates that NSAH functions by binding at the catalytic site (C-site) where it makes both common and unique contacts with the enzyme compared with NDP substrates.?Importantly, the IC for NSAH is within twofold of gemcitabine for growth inhibition of multiple cancer cell lines, while demonstrating little cytotoxicity against normal mobilized peripheral blood progenitor cells.?NSAH depresses dGTP and dATP levels in the dNTP pool causing S-phase arrest, providing evidence for RR inhibition in cells.NSAH (0-10 μM, 2, 6, 24, or 72 h) exhibits potent anti-tumor activity in 3 cancer cell lines.

NSAH depresses dGTP and dATP levels in the dNTP pool causing S-phase arrest, providing evidence for RR inhibition in cells.NSAH (0-10 μM, 2, 6, 24, or 72 h) exhibits potent anti-tumor activity in 3 cancer cell lines.NSAH blocks S-phase progression well to the extent and timing of the decreases in dATP and dGTP. Cell Viability Assay Cell Line:MDA-231, HCT116 and Panc1 cancer cell lines.Concentration:0-10 μM.Incubation Time:2, 6, 24, or 72 h.Result:Resulted in IC50 values ranging from 220 to 500 nM.

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2-hydroxy-N'-[(E)-(2-hydroxynaphthalen-1-yl)methylidene]benzohydrazide

Cell Cycle/DNA Damage

DNA/RNA Synthesis

RR

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1099592-35-4

306.3

C18H14N2O3

>98% (HPLC)

DMSO:62.5 mg/mL (204.03 mM; Need ultrasonic)

O=C(C1=CC=CC=C1O)N/N=C/C2=C3C=CC=CC3=CC=C2O

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(-20℃)

With Ice Pack

≥ 2 years