Radicicol
Based on 4 publication(s) in Google Scholar
Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation. 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. Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM.
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- Pureté: 99.72%
- CAS No.: 12772-57-5
- Formule: C18H17ClO6
- Masse moléculaire:364.78
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Radicicol
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Cell Proliferation/Viability Assay
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IF
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WB
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IP
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Activité biologique
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HSP90 1 μM (IC50) |
Plasmodium |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 3Y1 cell line | IC50 |
0.7 μM
Compound: 1 (radicicol)
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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
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[PMID: 12773056] |
| A549 | GI50 |
0.11 μM
Compound: 8
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Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
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[PMID: 18243703] |
| A549 | GI50 |
1.43 μM
Compound: Radicicol
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Growth inhibition of human A549 cells after 48 hrs by SRB assay
Growth inhibition of human A549 cells after 48 hrs by SRB assay
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[PMID: 24797798] |
| A549 | IC50 |
0.1 μM
Compound: 14
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Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
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[PMID: 28749671] |
| DLD-1 | GI50 |
0.076 μM
Compound: 8
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Growth inhibition of human DLD1 cells
Growth inhibition of human DLD1 cells
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[PMID: 18243703] |
| HCT-116 | GI50 |
0.058 μM
Compound: 8
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Growth inhibition of human HCT116 cells
Growth inhibition of human HCT116 cells
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[PMID: 18243703] |
| HCT-116 | GI50 |
0.13 μM
Compound: Radicicol
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Inhibitory concentration against cell proliferation of human HCT116 cell
Inhibitory concentration against cell proliferation of human HCT116 cell
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[PMID: 15974572] |
| HCT-116 | GI50 |
0.13 μM
Compound: Radicicol
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Inhibition of cell proliferation in HCT116 human colon cancer cell line
Inhibition of cell proliferation in HCT116 human colon cancer cell line
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[PMID: 16202589] |
| HeLa | IC50 |
0.1 μM
Compound: 14
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Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 28749671] |
| J774.A1 | IC50 |
2.35 μM
Compound: Radicicol
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Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay
Cytotoxicity against mouse J774.A1 cells after 72 hrs by MTS assay
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[PMID: 28835791] |
| Macrophage | IC50 |
27 nM
Compound: K00087
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Inhibition of COX2 expression in LPS-stimulated human macrophages
Inhibition of COX2 expression in LPS-stimulated human macrophages
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[PMID: 18077363] |
| MCF7 | EC50 |
25 nM
Compound: 3, radicicol
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Binding affinity to Hsp90 in MCF7 cell lysate
Binding affinity to Hsp90 in MCF7 cell lysate
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[PMID: 16913725] |
| MCF7 | IC50 |
0.03 μM
Compound: 1
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Antiproliferative activity against human MCF7 cells by MTT assay
Antiproliferative activity against human MCF7 cells by MTT assay
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[PMID: 16499313] |
| MCF7 | IC50 |
0.0892 μM
Compound: 2, RDC
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Cytotoxicity against human MCF7 cells after 24 hrs
Cytotoxicity against human MCF7 cells after 24 hrs
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[PMID: 18487051] |
| MCF7 | IC50 |
0.4 μM
Compound: 14
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Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
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[PMID: 28749671] |
| MCF7 | IC50 |
23 nM
Compound: 8, RD
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Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
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[PMID: 19017562] |
| MCF7 | IC50 |
30 nM
Compound: 6; RDC
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Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
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[PMID: 31663736] |
| MCF7 | IC50 |
47.7 nM
Compound: RDC
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Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
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[PMID: 19896848] |
| NRK | IC50 |
0.29 μM
Compound: 1 (radicicol)
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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
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[PMID: 12773056] |
| SK-BR-3 | IC50 |
0.00364 μM
Compound: 2, RDC
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Cytotoxicity against human SKBR3 cells after 24 hrs
Cytotoxicity against human SKBR3 cells after 24 hrs
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[PMID: 18487051] |
| SK-BR-3 | IC50 |
37.5 nM
Compound: RDC
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Antiproliferative activity against human SK-BR-3 cells
Antiproliferative activity against human SK-BR-3 cells
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[PMID: 19896848] |
| T-cell | EC50 |
9.1 μM
Compound: 1, monorden
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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
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[PMID: 24495105] |
| Vero | IC50 |
0.2 μM
Compound: 1
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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
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[PMID: 12828470] |
Radicicol (1 μM or 100 μM) inhibits the activities of Hsp90 and Topo VI by blocking ATP binding[1].
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Radicicol (100 μM; 10 min) binds to ATP-binding site in the C-terminal domain of PDK3 and prevents maturation of Hsp90 clients[1].
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Radicicol (0.25-18 μM; 48 h) inhibits P. falciparum?3D7 growth with an IC50 value of 8.563 μM, and (8 μM; 50 h) delays the schizont-to-ring transition[2].
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Radicicol (1.5 μM; 40 h) suppresses mitochondrial DNA replication without affecting nuclear and apicoplast genomes[2].
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Radicicol (0.001-5 μM; 72 h) induces myoblast differentiation with the myoblast toxicity concentration of 0.1 μM[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:P. falciparum 3D7
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Concentration:0.25 μM, 0.75 μM, 2 μM, 4 μM, 6 μM, 8 μM, 10 μM, 14 μM, 17 μM
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Incubation Time:48 hours
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Result:Showed a dose-dependent inhibitory effect on parasite growth.
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Cell Line:Primary myoblasts (from mice hindlimb muscles)
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Concentration:0.001, 0.01, 0.1, 1, 5 μM
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Incubation Time:72 hours
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Result:Induced myoblast differentiation with a highest concentration of not inducing myoblast toxicity of 0.1 μM.
? 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Renal I/R injury model in mice[4]
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Dosage:20 mg/kg or 60 mg/kg
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Administration:Intraperitoneal injection; twice dosages; 1 h before and just after bilateral renal ischemia reperfusion (I/R)
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Result:Showed renoprotection effect by inducing renal HSP70 expressing.
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Animal Model:Male C57B1/6 mice (3-month-old, 25±2 g)[5]
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Dosage:0.05 mg/20 g
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Administration:Subcutaneous injection; single dose; immediately before CTX injury (~1 min); evaluated on day one or 10 after injection
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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.
Chemical Information
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CAS No. 12772-57-5
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Appearance Solid
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Masse moléculaire 364.78
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Formule C18H17ClO6
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Color White to off-white
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SMILES
OC1=C2C(CC(/C=C/C=C\[C@@H](O3)[C@H]3C[C@@H](C)OC2=O)=O)=C(Cl)C(O)=C1
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Synonyms
Monorden
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Phytomedicine
The liver kinase B1 mediates the therapeutic efficacy of nuciferine against hepatic lipid accumulation in diabetic KKAy mice. [Abstract]2026 Mar:152:157807. PMID: 41650502 -
New Phytol
HSP90s are required for hypocotyl elongation during skotomorphogenesis and thermomorphogenesis via the COP1-ELF3-PIF4 pathway in Arabidopsis. [Abstract]2023 Aug;239(4):1253-1265. PMID: 36707919 -
Int J Mol Sci
6-Gingerol Ameliorates Hepatic Steatosis, Inflammation and Oxidative Stress in High-Fat Diet-Fed Mice through Activating LKB1/AMPK Signaling. [Abstract]2023 Mar 27;24(7):6285. PMID: 37047258
Radicicol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Mar 27;24(7):6285. [Abstract]
CCK-8 results showed that Radicicol (5 μM) did not significantly affect cell viability.
Radicicol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Mar 27;24(7):6285. [Abstract]
Representative images of immunofluorescence for intracellular ROS treated with Radicicol (Rad) (5 μM).
Radicicol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Mar 27;24(7):6285. [Abstract]
Protein expressions of p-ACC, t-ACC, SREBP1, FAS and CPT1α in HepG2 cells by Western blotting treated with Radicicol (Rad) (5 μM).
Radicicol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Mar 27;24(7):6285. [Abstract]
Immunoblotting for LKB1, MO25 and STRAD proteins before and after immunoprecipitation of LKB1 from HepG2 cells treated with Radicicol (Rad) (5 μM).
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Solvant et solubilité
DMSO : 100 mg/mL (274.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (282 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
[3]. Wang R, et al. Identification of Natural Compound Radicicol as a Potent FTO Inhibitor. Mol Pharm. 2018 Sep 4;15(9):4092-4098. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 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 |