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Purity: ≥98%
Radicicol (Monorden), an antifungal antibiotic with antimalarial activity, is a potent Hsp90 N-terminal inhibitor with an IC50 value of 1 μM. It binds to the ATPase domain of Hsp90 and prevents maturation of Hsp90 clients, leading to proteasomal degradation. Radicicol impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB.
| ln Vitro |
By preventing ATP binding, radiciccol (1 μM or 100 μM) suppresses the activity of Hsp90 and Topo VI [1]. At 100 μM for 10 minutes, radicol binds to the ATP binding site PDK3's C-terminal domain, blocking Hsp90 [1]. At 0.25–18 μM for 48 hours, radicol inhibits P. falciparum growth with an IC50 value of 8.563 μM, and at 8 μM for 50 hours, radicol slows the cleavage-to-ring transition [2]. μM; 40 h) fluorescence probe DNA replication that doesn't interfere with the plastid genome's underlying nucleus [2]. Muscle cells are induced with a hazardous concentration of 0.1 μM by radiciccol (0.001-5 μM; 72 h) [5].
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| ln Vivo |
Radicicol (0.05 mg/20 g; subcutaneous injection; single dose) improves regeneration of rattlesnake-injured skeletal muscle by reducing NF-kB activation. Radicicol (20 mg/kg or 60 mg/kg; intraperitoneal injection; 2 times; left and right 1 h) has a renal protective effect, improves renal ischemia-reperfusion (I/R) injury, and increases renal injury renal injury HSP70 mRNA [5].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Plasmodium falciparum 3D7 Tested Concentrations: 0.25 μM, 0.75 μM, 2 μM, 4 μM, 6 μM, 8 μM, 10 μM, 14 μM, 17 μM Incubation Duration: 48 hrs (hours) Experimental Results: Displayed for Dose-dependent inhibition of parasite growth. Cytotoxicity assay [5] Cell Types: primary myoblasts (from mouse hindlimb muscle) Tested Concentrations: 0.001, 0.01, 0.1, 1, 5 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced myoblast differentiation but not myogenesis The highest concentration of cytotoxicity is 0.1 micron. |
| Animal Protocol |
Animal/Disease Models: Renal I/R injury models and proteins [4]. Mouse[4]
Doses: 20 mg/kg or 60 mg/kg Route of Administration: intraperitoneal (ip) injection; two doses; 1 hour before and after bilateral renal ischemia-reperfusion (I/R) Experimental Results: shown by inducing renal HSP70 expression Exudes renal protection. Animal/Disease Models: Male C57B1/6 mice (3 months old, 25±2g) [5] Doses: 0.05mg/20g Route of Administration: subcutaneous injection; single dose; CTX before injury (about 1 minute); 1st after injection Results were assessed on day 10 or day 10: Heat shock protein induction and diminished NF-kB activation in crotonin-injured muscles at day 10. Improves size recovery of regenerated muscle fibers and reduces NF-kB activation. |
| References |
[1]. Kato M, et al. Distinct structural mechanisms for inhibition of pyruvate dehydrogenase kinase isoforms by AZD7545, dichloroacetate, and radicicol. Structure. 2007 Aug;15(8):992-1004. Epub 2007 Aug 2.
[2]. Chalapareddy S, et al. Radicicol confers mid-schizont arrest by inhibiting mitochondrial replication in Plasmodium falciparum. Antimicrob Agents Chemother. 2014 Aug;58(8):4341-52. [3]. Wang R, et al. Identification of Natural Compound Radicicol as a Potent FTO Inhibitor. Mol Pharm. 2018 Sep 4;15(9):4092-4098. [4]. Sonoda H, et al. The protective effect of radicicol against renal ischemia--reperfusion injury in mice. J Pharmacol Sci. 2010;112(2):242-6. [5]. Nascimento TL, et al. Radicicol enhances the regeneration of skeletal muscle injured by crotoxin via decrease of NF-kB activation. Toxicon. 2019 Sep;167:6-9. |
| Additional Infomation |
Radicicol is an antifungal macrolactone antibiotic, obtained from Diheterospora chlamydosporia and Chaetomium chiversii that inhibits protein tyrosine kinase and heat shock protein 90 (Hsp90). It has a role as a tyrosine kinase inhibitor, an antifungal agent and a metabolite. It is a macrolide antibiotic, an epoxide, an enone, a cyclic ketone, a member of phenols and a member of monochlorobenzenes.
Radicicol has been reported in Fusarium neocosmosporiellum, Floropilus chiversii, and other organisms with data available. Radicicol is a macrocyclic antifungal antibiotic that inhibits signal-dependent transcriptional activation and induces differentiation in leukemia. (NCI) |
| Molecular Formula |
C18H17CLO6
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| Molecular Weight |
364.77698
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| Exact Mass |
364.071
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| CAS # |
12772-57-5
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| PubChem CID |
6323491
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
656.2±55.0 °C at 760 mmHg
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| Melting Point |
190-194ºC
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| Flash Point |
350.7±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.583
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| LogP |
1.53
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
25
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| Complexity |
588
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C[C@@H]1C[C@@H]2[C@@H](C=CC=CC(=O)CC3=C(C(=CC(=C3Cl)O)O)C(=O)O1)O2
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| InChi Key |
WYZWZEOGROVVHK-RFVWBQTHSA-N
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| InChi Code |
InChI=1S/C18H17ClO6/c1-9-6-15-14(25-15)5-3-2-4-10(20)7-11-16(18(23)24-9)12(21)8-13(22)17(11)19/h2-5,8-9,14-15,21-22H,6-7H2,1H3/b4-2+,5-3-/t9-,14+,15+/m0/s1
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| Chemical Name |
(1aR,2Z,4E,14S,15aR)-8-Chloro-9,11-dihydroxy-14-methyl-1a,14,15,15a-tetrahydro-6H-benzo[c]oxireno[2,3-k][1]oxacyclotetradecine-6,12(7H)-dione
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| Synonyms |
Radicicol Monorden
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~274.14 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2741 mL | 1.3707 mL | 2.7414 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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