Novobiocin Sodium (NSC 2382)

別名: Albamycin,Cathomycin,NSC 2382 中文名稱：新生霉素鈉

目錄號(hào)：S2492 Purity: 99.91%

Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin)是一種非常有效的細(xì)菌DNA旋轉(zhuǎn)酶和人體有機(jī)陰離子轉(zhuǎn)運(yùn)體，作用于hOAT1，hOAT3和hOAT4，K_i分別為14.87±0.40μM, 4.77±1.12μM 和 90.50±7.50μM。

Novobiocin Sodium (NSC 2382) Chemical Structure

CAS: 1476-53-5

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1071.68	現(xiàn)貨
50mg	787.79	現(xiàn)貨
1g	5487.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.91%

99.91

Novobiocin Sodium (NSC 2382)相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	Puromycin 2HCl Staurosporine (STS) Oligomycin A Geldanamycin Honokiol Geneticin (G418 Sulfate) STZ (Streptozotocin) Cephalomannine Sodium Monensin (NSC 343257) 10-Deacetylbaccatin-III Pirarubicin Hygromycin B Roxithromycin	點(diǎn)擊展開
相關(guān)化合物庫(kù)	FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 凋亡分子化合物庫(kù) DNA損傷/ DNA修復(fù)化合物庫(kù) 細(xì)胞周期化合物庫(kù)	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
MELN	Function assay	200 uM	18 hrs	Inhibition of estradiol-induced ER-mediated transcription in MELN cells by measuring luciferase activity at 200 uM after 18 hrs	17979263
yeast PP30	Function assay	100 uM	3 hrs	Inhibition of human HSP90alpha expressed in yeast PP30 cells co-expressing HSF-lacZ reporter assessed as inhibition of heat stress-induced response at 100 uM after 3 hrs	21129982
SKBR3	Function assay	1000 uM	18 hrs	Inhibition of HSP90 in human SKBR3 cells assessed as aggregation of intracellular HER2 at 1000 uM after 18 hrs by DAPI staining-based immunofluorescence microscopic analysis	23859777
SH-SY5Y	Neuroprotection assay	10 nM		Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release at 10 nM	19138859
BL21 (DE3) pLysS	Function assay		100 mins	Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay, IC50=0.18μM	25129171
BL21 (DE3) pLysS	Function assay		100 mins	Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay, IC50=0.18μM	25801151
BL21 (DE3) pLysS	Function assay		100 mins	Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay, IC50=0.18μM	26318054
BL21 (DE3) pLysS	Function assay		120 mins	Inhibition of Mycobacterium smegmatis 155 6His-tagged DNA gyrase B catalytic domain ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inorganic phosphate release after 120 mins in presence of ATP by malachite green dye based, IC50=0.046μM	27371925
MCF7-MX	Function assay			TP_TRANSPORTER: inhibition of mitoxantrone efflux in BCRP-expressing MCF7-MX cells, IC50=25μM	16460798
SH-SY5Y	Neuroprotection assay			Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.04839μM	19138859
SH-SY5Y	Neuroprotection assay			Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release	19138859
LNCaP-LN3	Antiproliferative assay			Antiproliferative activity against human LNCaP-LN3 cells, IC50=1.05μM	21129982
Sf9	Function assay			Inhibition of Escherichia coli His6-tagged ParC/ParE expressed in baculovirus-infected Sf9 cells by gel electrophoresis, IC50=0.21μM	21235241
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

Topoisomerase II ^[1]

Topoisomerase IV ^[1]

體外研究(In Vitro)
體外研究活性	Novobiocin和Hsp90結(jié)合，改變分子伴侶對(duì)geldanamycin和radicicol的親和力，造成關(guān)鍵調(diào)節(jié)Hsp90依賴性激酶，包括V形的Src，RAF-1，和P185（ErbB2）在體內(nèi)外的損耗。Novobiocin干擾共伴侶Hsc70和p23對(duì)Hsp90的結(jié)合。^[1] Novobiocin以濃度依賴性方式特異性地抑制血紅素調(diào)節(jié)eIF2alpha激酶（HRI）的成熟。Novobiocin誘導(dǎo)Hsp90和CDC37從未成熟HRI解離，而Hsp90的共分子伴侶P23，F(xiàn)KBP52，和蛋白磷酸酶5仍然與未成熟HRI相結(jié)合。^[2] Novobiocin引起特征形態(tài)和生化變化，導(dǎo)致細(xì)胞死亡，顯示出后生動(dòng)物細(xì)胞凋亡。^[3] Novobiocin，一個(gè)HSP90抑制劑，可降低SMYD3的表達(dá)并劑量依賴性抑制MDA-MB-231人乳腺癌細(xì)胞的增殖和遷移Novobiocin能抑制乳腺癌細(xì)胞的遷移，這可能涉及SMYD3的下調(diào)。^[4] Novobiocin，一個(gè)aminocoumarin抗生素，干擾了熱休克蛋白90和缺氧誘導(dǎo)因子依賴的基因表達(dá)，從而損害了細(xì)胞的存活。Novobiocin（500 μM）導(dǎo)致[Ca（2 +）] i的顯著增加，減少前向散射，增加膜聯(lián)蛋白-V結(jié)合并增強(qiáng)ceramide的形成。Novobiocin刺激紅細(xì)胞死亡，至少部分是因?yàn)榧?xì)胞外Ca（2+）的進(jìn)入和ceramide的形成。^[5]

體外研究(In Vitro)

體外研究活性

Novobiocin和Hsp90結(jié)合，改變分子伴侶對(duì)geldanamycin和radicicol的親和力，造成關(guān)鍵調(diào)節(jié)Hsp90依賴性激酶，包括V形的Src，RAF-1，和P185（ErbB2）在體內(nèi)外的損耗。Novobiocin干擾共伴侶Hsc70和p23對(duì)Hsp90的結(jié)合。^[1]

Novobiocin以濃度依賴性方式特異性地抑制血紅素調(diào)節(jié)eIF2alpha激酶（HRI）的成熟。Novobiocin誘導(dǎo)Hsp90和CDC37從未成熟HRI解離，而Hsp90的共分子伴侶P23，F(xiàn)KBP52，和蛋白磷酸酶5仍然與未成熟HRI相結(jié)合。^[2]

Novobiocin引起特征形態(tài)和生化變化，導(dǎo)致細(xì)胞死亡，顯示出后生動(dòng)物細(xì)胞凋亡。^[3]

Novobiocin，一個(gè)HSP90抑制劑，可降低SMYD3的表達(dá)并劑量依賴性抑制MDA-MB-231人乳腺癌細(xì)胞的增殖和遷移Novobiocin能抑制乳腺癌細(xì)胞的遷移，這可能涉及SMYD3的下調(diào)。^[4]

Novobiocin，一個(gè)aminocoumarin抗生素，干擾了熱休克蛋白90和缺氧誘導(dǎo)因子依賴的基因表達(dá)，從而損害了細(xì)胞的存活。Novobiocin（500 μM）導(dǎo)致[Ca（2 +）] i的顯著增加，減少前向散射，增加膜聯(lián)蛋白-V結(jié)合并增強(qiáng)ceramide的形成。Novobiocin刺激紅細(xì)胞死亡，至少部分是因?yàn)榧?xì)胞外Ca（2+）的進(jìn)入和ceramide的形成。^[5]

參考文獻(xiàn)
[1] Marcu MG, et al. J Biol Chem,?000, 275(47), 37181-37186. [2] Yun BG, et al. Biochemistry,?004, 43(25), 8217-8229. [3] Singh G, et al. Mol Biochem Parasitol,?005, 141(1), 57-69. [4] Luo XG, et al. IUBMB Life,?010, 62(3), 194-199. [5] Lupescu A, et al. Cell Physiol Biochem,?014, 33(3), 670-680. [6] Rodriguez-Cerrato V, et al. Int J Antimicrob Agents. 2010 Jun;35(6):544-9. + 展開

參考文獻(xiàn)

[1] Marcu MG, et al. J Biol Chem,?000, 275(47), 37181-37186.
[2] Yun BG, et al. Biochemistry,?004, 43(25), 8217-8229.
[3] Singh G, et al. Mol Biochem Parasitol,?005, 141(1), 57-69.

[4] Luo XG, et al. IUBMB Life,?010, 62(3), 194-199.
[5] Lupescu A, et al. Cell Physiol Biochem,?014, 33(3), 670-680.
[6] Rodriguez-Cerrato V, et al. Int J Antimicrob Agents. 2010 Jun;35(6):544-9.

+ 展開