Minocycline HCl

Catalog No.S4226

Minocycline HCl Chemical Structure

Molecular Weight(MW): 493.94

Minocycline HCl is the most lipid soluble and most active tetracycline antibiotic, binds to the 30S ribosomal subunit, preventing the binding of tRNA to the mRNA-ribosome complex and interfering with protein synthesis.

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Biological Activity

Description Minocycline HCl is the most lipid soluble and most active tetracycline antibiotic, binds to the 30S ribosomal subunit, preventing the binding of tRNA to the mRNA-ribosome complex and interfering with protein synthesis.
In vitro

Minocycline is a second-generation tetracycline used in humans, which effectively crosses the blood−brain barrier. It inhibits the activity of caspase-1, caspase-3, inducible form of nitric oxide synthetase (iNOS) and p38 mitogen-activated protein kinase (MAPK). After experimental ischemia, minocycline inhibits caspase-1 and inducible nitric oxide synthetase (iNOS) upregulation, and decreases infarct size. Minocycline inhibits mitochondrial permeability-transition-mediated cytochrome c release. Minocycline-mediated inhibition of cytochrome c release is demonstrated in vivo, in cells, and in isolated mitochondria. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat cells MWfD[YxtKH[rYXLpcIl1gSCjc4PhfS=> Mn2wNVAuOjByINM1US=> NWjGcYhjOjRiaB?= NWXp[FZ5emWmdXPld{Bk\WyuII\pZYJqdGm2eTDhcoQhcW6mdXPld{BFVkFiZoLh[41mdnSjdHnvckBidmRiZHnzd4lx[XSrb36gc4YhfGinIH3peI9kcG:wZILpZYwhdWWvYoLhcoUheG:2ZX70bYFtKGmwIFr1dotifCClZXzsd{BjfXRiaYOgbIFzdWync4OgeI8hcHWvYX6gdIVzcXCqZYLhcEBjdG:xZDDsfY1xcG:leYTlJINmdGy|IDjoVGJNS3Nr NHu5VpAzQTZ{NUG2OS=>
hPBLCs NGDTemdE\WyuII\pZYJqdGm2eTDhd5NigQ>? M4L1RVExNTJyMDFCuW0> Moe4NlQhcA>? NHyzd3Bz\WS3Y3XzJINmdGxidnnhZoltcXS7IHHu[EBqdmS3Y3XzJGRPSSCocnHncYVvfGG2aX;uJIFv\CCmaYPzbZBifGmxbjDv[kB1cGVibXn0c4Npd26mcnnhcEBu\W2kcnHu[UBxd3SnboTpZYwhcW5iSoXyb4F1KGOnbHzzJIJ2fCCrczDoZZJudGW|czD0c{BpfW2jbjDw[ZJqeGincnHsJIJtd2:mIHz5cZBpd2O7dHWgZ4VtdHNiKHjQRmxEeyl? NI\SOXYzQTZ{NUG2OS=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
IL-6Rα / gp130; 

PubMed: 23593315     


To detect expression levels of (A) IL-6Rα or (B) gp130, SKOV-3 cells were either stimulated with IL-1β (10 ng/ml) or non-stimulated, with or without pre-treatment with minocycline (100 µM) for different time points. Cell lysates were analyzed by immunoblotting for IL-6Rα, gp130 and β-actin antibodies. β-actin was the loading control. IL-6Rα and gp130 protein levels were normalized to β-actin and their relative differences with the corresponding controls are shown (*p<0.05 and **p<0.01 vs. control cells, # p<0.05 and## p<0.01 vs. IL-1β treated cells).

p-STAT3 / STAT3 / Mcl-1 / p-ERK / ERK ; 

PubMed: 23593315     


SKOV-3 cells were treated with minocycline (100 µM) with or without IL-1β (10 ng/ml) stimulation for different time points. The expression levels of (A) p-STAT3, STAT3; (B) Mcl-1 or (C) p-ERK1/2, ERK1/2 were estimated by western blot analysis. Densitometric analysis is expressed as mean ± SD intensity of optical density obtained by three independent experiments (*p<0.05, **p<0.01 and ***p<0.001 vs. control cells, #p<0.05, ## p<0.01 vs. IL-1β treated cells).

23593315
Immunofluorescence
p-STAT3; 

PubMed: 23593315     


Confocal immunocytochemistry of p-STAT3 in SKOV-3 cells treated with 100 µM minocycline in comparison with control cells. The nuclei are counterstained with propidium iodide (red). Images were obtained at 60× magnification. The scale bars represent 10 µm.

STAT3; 

PubMed: 23593315     


Confocal immunocytochemistry of STAT3 (green) in SKOV-3 cells treated with 100 µM minocycline in comparison with control cells. The nuclei are counterstained with propidium iodide (red). Images were obtained at 60× magnification. The scale bars represent 10 µm.

23593315
Growth inhibition assay
Cell viability ; 

PubMed: 27555377     


Cell viability was assessed by MTT assay after treatment with minocycline alone. 

27555377
In vivo Minocycline is a semi-synthetic tetracycline derivative which is well absorbed and distributed in body tissues and is suitable for twice daily administration. Minocycline's effects are related to the inhibition of protein synthesis. Although minocycline's broader spectrum of activity, compared to other members of the group, includes activity against Neisseria meningitidis, its use as a prophylaxis is no longer recomended because of side effects (dizziness and vertigo). [1] Minocycline is remarkable neuroprotective qualities in models of cerebral ischaemia, traumatic brain injury, and Huntington's and Parkinson's disease. The neuroprotective action of minocycline may include its inhibitory effect on 5-lipoxygenase, an inflammatory enzyme associated with brain aging. [3]

Protocol

Solubility (25°C)

In vitro Water 1 mg/mL warmed (2.02 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 493.94
Formula

C23H27N3O7.HCl

CAS No. 13614-98-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03291158 Not yet recruiting Drug: Minocycline Normal Healthy Volunteers Rempex Pharmaceuticals (a wholly owned subsidiary of The Medicines Company)|Universitätsklinikum Köln|Innovative Medicines Initiative April 2018 Phase 1
NCT03160040 Completed Drug: Minocycline IV Gram-Negative Bacterial Infections Rempex (a wholly owned subsidiary of Melinta Therapeutics Inc.)|Melinta Therapeutics Inc. October 11 2017 --
NCT02808052 Terminated Drug: Minocin (minocycline) for Injection Renal Insufficiency Acute|Renal Insufficiency Chronic|Healthy Subjects Rempex (a wholly owned subsidiary of Melinta Therapeutics Inc.)|Universitätsklinikum Köln|Innovative Medicines Initiative|Melinta Therapeutics Inc. May 29 2017 Phase 1
NCT02802631 Completed Drug: Minocin (minocycline) for Injection|Other: Placebo Normal Healthy Volunteers Rempex (a wholly owned subsidiary of Melinta Therapeutics Inc.)|Universitätsklinikum Köln|Innovative Medicines Initiative|Melinta Therapeutics Inc. April 20 2017 Phase 1
NCT03117530 Recruiting Drug: Minocycline Autism Spectrum Disorder University of California Los Angeles April 11 2017 Phase 1
NCT02695446 Completed Drug: Minocycline Acne BioPharmX Inc. March 2016 Phase 4

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID