1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Anti-infection
  2. HSP Bacterial Antibiotic Parasite
  3. Radicicol

Radicicol  (Synonyms: 根赤壳菌素; Monorden)

目录号: HY-N6769 纯度: 99.63%
COA 产品使用指南

Radicicol 是一种 Hsp90 抑制剂,导致蛋白酶体降解,IC50 <1 μM。Radicicol 抑制 PDKIC50 为 230 μM (PDK1) 和 400 μM (PDK3)。Radicicol 也是一种抗真菌和抗疟疾的抗生素,通过靶向恶性疟原虫的拓扑异构酶 VIB 破坏线粒体复制。Radicicol 还抑制脂肪团和肥胖相关蛋白 (FTO),IC50 为 16.04 μM。

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Radicicol Chemical Structure

Radicicol Chemical Structure

CAS No. : 12772-57-5

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1 mg ¥1950
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5 mg ¥4800
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation[1]. Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB[2]. Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM[3].

IC50 & Target

HSP90

1 μM (IC50)

Plasmodium

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
3Y1 cell line IC50
0.7 μM
Compound: 1 (radicicol)
Concentration to inhibit growth of normal rat fibroblast cells (3Y1-B cells) after 72 h exposure
Concentration to inhibit growth of normal rat fibroblast cells (3Y1-B cells) after 72 h exposure
[PMID: 12773056]
A549 IC50
0.1 μM
Compound: 14
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 28749671]
A549 GI50
1.43 μM
Compound: Radicicol
Growth inhibition of human A549 cells after 48 hrs by SRB assay
Growth inhibition of human A549 cells after 48 hrs by SRB assay
[PMID: 24797798]
HeLa IC50
0.1 μM
Compound: 14
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
[PMID: 28749671]
J774.A1 IC50
2.35 μM
Compound: Radicicol
Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay
Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay
[PMID: 28835791]
MCF7 IC50
0.03 μM
Compound: 1
Antiproliferative activity against human MCF7 cells by MTT assay
Antiproliferative activity against human MCF7 cells by MTT assay
[PMID: 16499313]
MCF7 IC50
0.0892 μM
Compound: 2, RDC
Cytotoxicity against human MCF7 cells after 24 hrs
Cytotoxicity against human MCF7 cells after 24 hrs
[PMID: 18487051]
MCF7 IC50
0.4 μM
Compound: 14
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 28749671]
NRK IC50
0.29 μM
Compound: 1 (radicicol)
Concentration to inhibit growth of normal rat kidney epithelial cells (NRK cells) after 72 hr exposure
Concentration to inhibit growth of normal rat kidney epithelial cells (NRK cells) after 72 hr exposure
[PMID: 12773056]
SK-BR-3 IC50
0.00364 μM
Compound: 2, RDC
Cytotoxicity against human SKBR3 cells after 24 hrs
Cytotoxicity against human SKBR3 cells after 24 hrs
[PMID: 18487051]
T-cell EC50
9.1 μM
Compound: 1, monorden
Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis
Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis
[PMID: 24495105]
Vero IC50
0.2 μM
Compound: 1
Antiviral activity against HSV1 F infected in african green monkey Vero cells assessed as reduction of virus-induced cytopathic effect by cellular replication assay
Antiviral activity against HSV1 F infected in african green monkey Vero cells assessed as reduction of virus-induced cytopathic effect by cellular replication assay
[PMID: 12828470]
体外研究
(In Vitro)

Radicicol (1 μM 或 100 μM) 通过阻断 ATP 结合来抑制 Hsp90 和 Topo VI 的活性[1]
Radicicol (100 μM;10 分钟) 结合 ATP 结合位点PDK3 的 C 端结构域并阻止Hsp90 课题[1]的成熟。
Radicicol (0.25-18 μM;48 h) 抑制 P. falciparum 生长,IC50 值为 8.563 μM,并且 (8 μM;50 h) 延迟了裂殖体到环的转变[2]
Radicicol (1.5 μM;40 h) 抑制线粒体 DNA 复制而不影响细胞核和顶端质体基因组[2]
Radicicol (0.001-5 μM;72 h) 诱导成肌细胞分化成肌细胞,毒性浓度为0.1 μM[5]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: P. falciparum 3D7
Concentration: 0.25 μM, 0.75 μM, 2 μM, 4 μM, 6 μM, 8 μM, 10 μM, 14 μM, 17 μM
Incubation Time: 48 hours
Result: Showed a dose-dependent inhibitory effect on parasite growth.

Cell Cytotoxicity Assay[5]

Cell Line: Primary myoblasts (from mice hindlimb muscles)
Concentration: 0.001, 0.01, 0.1, 1, 5 μM
Incubation Time: 72 hours
Result: Induced myoblast differentiation with a highest concentration of not inducing myoblast toxicity of 0.1 μM.
体内研究
(In Vivo)

Radicicol (20 mg/kg or 60 mg/kg;腹腔注射;2次给药;前后1 h) 具有肾脏保护作用,改善肾缺血再灌注 (I/R) 损伤,增加肾损伤小鼠肾脏 HSP70 mRNA 和蛋白[4]
Radicicol (0.05 mg/20 g;皮下注射;单剂量) 通过降低 NF-kB 激活增强受到响尾蛇毒素损伤的骨骼肌的再生[5]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Renal I/R injury model in mice[4]
Dosage: 20 mg/kg or 60 mg/kg
Administration: Intraperitoneal injection; twice dosages; 1 h before and just after bilateral renal ischemia reperfusion (I/R)
Result: Showed renoprotection effect by inducing renal HSP70 expressing.
Animal Model: Male C57B1/6 mice (3-month-old, 25±2 g)[5]
Dosage: 0.05 mg/20 g
Administration: Subcutaneous injection; single dose; immediately before CTX injury (~1 min); evaluated on day one or 10 after injection
Result: Resulted heat shock protein induction and decreased NF-kB activation in muscle injured by crotoxin at days 10.
Improved the size recovery of regenerating myofibers and decreased NF-kB activation.
分子量

364.78

Formula

C18H17ClO6

CAS 号
性状

固体

颜色

White to off-white

中文名称

根赤壳菌素

结构分类
初始来源

Penicillium meleagrinum

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (274.14 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7414 mL 13.7069 mL 27.4138 mL
5 mM 0.5483 mL 2.7414 mL 5.4828 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.63%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7414 mL 13.7069 mL 27.4138 mL 68.5345 mL
5 mM 0.5483 mL 2.7414 mL 5.4828 mL 13.7069 mL
10 mM 0.2741 mL 1.3707 mL 2.7414 mL 6.8534 mL
15 mM 0.1828 mL 0.9138 mL 1.8276 mL 4.5690 mL
20 mM 0.1371 mL 0.6853 mL 1.3707 mL 3.4267 mL
25 mM 0.1097 mL 0.5483 mL 1.0966 mL 2.7414 mL
30 mM 0.0914 mL 0.4569 mL 0.9138 mL 2.2845 mL
40 mM 0.0685 mL 0.3427 mL 0.6853 mL 1.7134 mL
50 mM 0.0548 mL 0.2741 mL 0.5483 mL 1.3707 mL
60 mM 0.0457 mL 0.2284 mL 0.4569 mL 1.1422 mL
80 mM 0.0343 mL 0.1713 mL 0.3427 mL 0.8567 mL
100 mM 0.0274 mL 0.1371 mL 0.2741 mL 0.6853 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Radicicol
目录号:
HY-N6769
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