Radicicol (Synonyms: Monorden)

Name: Radicicol
Brand: MedChemExpress
SKU: HY-N6769
Rating: 5.0 (4 reviews)

Cat. No.: HY-N6769 Purity: 99.72%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 12772-57-5

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE Radicicol

Cell Proliferation/Viability Assay

: 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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Biological Activity
Purity & Documentation
References
Customer Review

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	GI₅₀	0.11 μM Compound: 8	Growth inhibition of human A549 cells Growth inhibition of human A549 cells	[PMID: 18243703]
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]
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]
DLD-1	GI₅₀	0.076 μM Compound: 8	Growth inhibition of human DLD1 cells Growth inhibition of human DLD1 cells	[PMID: 18243703]
HCT-116	GI₅₀	0.058 μM Compound: 8	Growth inhibition of human HCT116 cells Growth inhibition of human HCT116 cells	[PMID: 18243703]
HCT-116	GI₅₀	0.13 μM Compound: Radicicol	Inhibitory concentration against cell proliferation of human HCT116 cell Inhibitory concentration against cell proliferation of human HCT116 cell	[PMID: 15974572]
HCT-116	GI₅₀	0.13 μM Compound: Radicicol	Inhibition of cell proliferation in HCT116 human colon cancer cell line Inhibition of cell proliferation in HCT116 human colon cancer cell line	[PMID: 16202589]
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]
Macrophage	IC₅₀	27 nM Compound: K00087	Inhibition of COX2 expression in LPS-stimulated human macrophages Inhibition of COX2 expression in LPS-stimulated human macrophages	[PMID: 18077363]
MCF7	EC₅₀	25 nM Compound: 3, radicicol	Binding affinity to Hsp90 in MCF7 cell lysate Binding affinity to Hsp90 in MCF7 cell lysate	[PMID: 16913725]
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]
MCF7	IC₅₀	23 nM Compound: 8, RD	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 19017562]
MCF7	IC₅₀	30 nM Compound: 6; RDC	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 31663736]
MCF7	IC₅₀	47.7 nM Compound: RDC	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 19896848]
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]
SK-BR-3	IC₅₀	37.5 nM Compound: RDC	Antiproliferative activity against human SK-BR-3 cells Antiproliferative activity against human SK-BR-3 cells	[PMID: 19896848]
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.

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.

12772-57-5

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

Microorganisms

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
10 mM	0.2741 mL	1.3707 mL	2.7414 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.96%

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Data Sheet (282 KB) SDS (480 KB)

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

Handling Instructions (2659 KB)

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. [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

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

Radicicol Related Classifications

Infection

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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Radicicol (Synonyms: Monorden)

Customer Review

Radicicol Related Antibodies

4 Publications Citing Use of MCE Radicicol

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Complete Stock Solution Preparation Table

Radicicol Related Classifications

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