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Radicicol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Radicicol图片
CAS NO:12772-57-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品名称
根赤壳菌素
Monorden
产品介绍
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。
生物活性

Radicicol is an inhibitor ofHsp90with anIC50value< 1 μM, and leads to proteasomal degradation[1]. Radicicol exhibits inhibition onPDKwithIC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarialantibiotic, impairs mitochondrial replication by targetingP. falciparumtopoisomeraseVIB[2]. Radicicol is also an inhibitor offat mass and obesity-associated protein(FTO), with anIC50value of 16.04 μM[3].

IC50& Target

HSP90

1 μM (IC50)

Plasmodium

 

体外研究
(In Vitro)

Radicicol (1 μM or 100 μM) inhibits the activities of Hsp90 and Topo VI by blocking ATP binding[1].
Radicicol (100 μM; 10 min) binds to ATP-binding site in the C-terminal domain of PDK3 and prevents maturation ofHsp90clients[1].
Radicicol (0.25-18 μM; 48 h) inhibitsP. falciparum 3D7 growth with an IC50value of 8.563 μM, and (8 μM; 50 h) delays the schizont-to-ring transition[2].
Radicicol (1.5 μM; 40 h) suppresses mitochondrial DNA replication without affecting nuclear and apicoplast genomes[2].
Radicicol (0.001-5 μM; 72 h) induces myoblast differentiation with the myoblast toxicity concentration of 0.1 μM[5].

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; i.p.; twice dosages; 1 h before and after) has renoprotection effect, and ameliorates renal ischemia reperfusion (I/R) injury and increases renal HSP70 mRNA and protein in renal injury mice[4].
Radicicol (0.05 mg/20 g; s.c.; single dose) enhances the regeneration of skeletal muscle injured by crotoxin via decrease of NF-kB activation[5].

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

性状

Solid

Formula

C18H17ClO6

CAS 号

12772-57-5

中文名称

根赤壳菌素

结构分类
  • Phenols
  • Polyphenols
  • Antibiotics
  • Macrolide Antibiotics
来源

Penicillium meleagrinum

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(274.14 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7414 mL13.7069 mL27.4138 mL
5 mM0.5483 mL2.7414 mL5.4828 mL
10 mM0.2741 mL1.3707 mL2.7414 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。