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

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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Radicicol Chemical Structure

Radicicol Chemical Structure

CAS No. : 12772-57-5

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Based on 3 publication(s) in Google Scholar

Radicicol Related Antibodies

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  • Biological Activity

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Description

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

 

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]
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 of Hsp90 clients[1].
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].
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].

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

Radicicol Related Antibodies

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.
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].

MedChemExpress (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.
Molecular Weight

364.78

Formula

C18H17ClO6
CAS No.
Appearance

Solid

Color

White to off-white

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
Structure Classification
Initial Source

Penicillium meleagrinum
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.63%

SDS (420 KB)

COA (252 KB) RP-HPLC (619 KB)

Handling Instructions (2659 KB)
References

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
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Radicicol Related Classifications

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.

Keywords:

Radicicol12772-57-5MonordenHSPBacterialAntibioticParasiteHeat shock proteinsantifungal antibioticmitochondrial replicationrenoprotectionheat shock proteinscrotoxinmuscle damagenuclear factor kappa BInhibitorinhibitorinhibit

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