Novobiocin Sodium (Albamycin; Cathomycin) 是一种口服抗生素 (antibiotic) 化合物,源于链霉菌,也是一个强效的 DNA gyrase 抑制剂通过结合 ATP 结合位点在 ATP 酶亚基。Novobiocin Sodium 对革兰氏阳性菌有较强的抗菌活性,但由于外膜中含有脂多糖,对革兰氏阴性菌的抗菌活性有限。Novobiocin Sodium 与 Hsp90 的 c 端结合,轻微诱导 Hsp90 依赖的 client 蛋白的降解 (IC50=700 μM)。
Novobiocin Sodium Chemical Structure
CAS No. : 1476-53-5
规格
价格
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数量
10 mM * 1 mL in DMSO
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5 g
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生物活性
Novobiocin Sodium (Albamycin; Cathomycin) is an orally active antibiotic compound derived from Streptomyces niveus and a potent DNA gyrase inhibitor by binding the ATP-binding site in the ATPase subunit[1]. Novobiocin Sodium manifests strong anti-bacterial activities effectively against gram-positive pathogens and shows limited activity against gram-negative organisms due to LPS-containing outer membrane.Novobiocin Sodium binds to the C-terminus of Hsp90 and slightly induces degradation of Hsp90-dependent client proteins (IC50=700 µM)[1][2].
IC50 & Target
IC50: 700 μM (HSP90)[2]
体外研究 (In Vitro)
Novobiocin Sodium (0.3 mM; 48 hours) induces a caspase-3/7 enzyme–dependent apoptosis assays with an induction of approximately three- to fivefold of apoptotic cells in K562, HL60, Mutz-2[1]. Novobiocin (0-500 μM; 15-hours) is against wild type, lptB1, lptB1(R144H), and efflux pump-deficient ∆tolC strains with IC50 values of 62.5-125 μM; 0.5 μM; 62.5-125 μM; and 2 μM, respectively[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[2]
Cell Line:
K562, HL60, Mutz-2 cells
Concentration:
0.3 mM
Incubation Time:
48 hours
Result:
Decreased caspase-3/7 activity in K562, HL60, Mutz-2 cells.
分子量
634.61
Formula
C31H35N2NaO11
CAS 号
1476-53-5
中文名称
新生霉素钠
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Bhatia S, et al. Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response.Blood. 2018 Jul 19;132(3):307-320.
[2]. Burlison JA, et al. Novobiocin: redesigning a DNA gyrase inhibitor for selective inhibition of hsp90.J Am Chem Soc. 2006 Dec 6;128(48):15529-36.