Novobiocin Sodium (NSC 2382)

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

目錄號：S2492 Purity: 99.91%

Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin)是一種非常有效的細菌DNA旋轉酶和人體有機陰離子轉運體，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	價格	庫存
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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產品質控

批次：純度： 99.91%

99.91

Novobiocin Sodium (NSC 2382)相關產品

相關產品	Puromycin 2HCl Staurosporine (STS) Oligomycin A Geldanamycin Honokiol Geneticin (G418 Sulfate) Nigericin sodium salt STZ (Streptozotocin) Cephalomannine Sodium Monensin (NSC 343257) 10-Deacetylbaccatin-III Pirarubicin Hygromycin B Roxithromycin	點擊展開
相關化合物庫	FDA藥物庫天然產物庫凋亡分子化合物庫 DNA損傷/ DNA修復化合物庫細胞周期化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
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生物活性

產品描述

靶點

Topoisomerase II ^[1]

Topoisomerase IV ^[1]

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

體外研究(In Vitro)

體外研究活性

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

Novobiocin以濃度依賴性方式特異性地抑制血紅素調節(jié)eIF2alpha激酶（HRI）的成熟。Novobiocin誘導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相結合。^[2]

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

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

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

參考文獻
[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

[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