Radicicol 是一种Hsp90抑制剂，导致蛋白酶体降解，IC50<1 μm。radicicol 抑制PDK，IC50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 |
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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. |
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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. |
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| 结构分类 | - Antibiotics
- Macrolide Antibiotics
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| 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 | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(274.14 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7414 mL | 13.7069 mL | 27.4138 mL | | 5 mM | 0.5483 mL | 2.7414 mL | 5.4828 mL | | 10 mM | 0.2741 mL | 1.3707 mL | 2.7414 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。 |
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