tunicamycin

Tunicamycin is a mixture of antibiotics that inhibit N-linked glycosylation by blocking GlcNAc phosphotransferase (GPT). Tunicamycin has antitumor activity, as well as anti-bacterial, anti-fungal, and anti-viral activity.

Tunicamycin 15:1 is a mixture of tunicamycin structural isomers that contains a 15-carbon N-acyl chain with variable branching patterns.References Tunicamycin 15:1 is a mixture of tunicamycin structural isomers that contains a 15-carbon N-acyl chain with variable branching patterns. References

Tunicamycin VIII is a useful organic compound for research related to life sciences. The catalog number is T124297 and the CAS number is 73942-07-1.

Tunicamycin X is a useful organic compound for research related to life sciences. The catalog number is T124448 and the CAS number is 66081-38-7.

Tunicamycin VII is a useful organic compound for research related to life sciences. The catalog number is T124449 and the CAS number is 66081-36-5.

Tunicamycin 14:1 is a mixture of tunicamycin structural isomers that contain a 14-carbon N-acyl chain with variable branching patterns. The N-acyl chain incorporated into tunicamycins, like tunicamycin 14:1, is derived from the same pool of cellular branched-chain fatty acids (BCFAs) in Streptomyces and directly impacts the biological activity of each individual tunicamycin variant.1,2,3Purified tunicamycin 14:1 with the iso branching configuration inhibits bacterial phospho-MurNAc-pentapeptide transferase (MraY) with an IC50 value of 0.31 μM.2

Tunicamycin 15:1 is a mixture of tunicamycin structural isomers that contain a 15-carbon N-acyl chain with variable branching patterns. The N-acyl chain incorporated into tunicamycins, like tunicamycin 15:1, is derived from the same pool of cellular branched-chain fatty acids (BCFAs) inStreptomycesand directly impacts the biological activity of each individual tunicamycin variant.1,2,3Purified tunicamycin 15:1 withiso,anteiso, or a mixture ofisoandanteisobranching configurations inhibit bacterial phospho-MurNAc-pentapeptide transferase (MraY) with IC50values of 0.05, 0.36, and 0.09 μM, respectively.2 1.Price, N.P.J., Jackson, M.A., Hartman, T.M., et al.Branched chain lipid metabolism as a determinant of the N-Acyl variation of Streptomyces natural productsACS Chem. Biol.16(1)116-124(2021) 2.Hering, J., Dunevall, E., Snijder, A., et al.Exploring the active site of the antibacterial target MraY by modified tunicamycinsACS Chem Biol.15(11)2885-2895(2020) 3.Duksin, D., and Mahoney, W.C.Relationship of the structure and biological activity of the natural homologues of tunicamycinJ. Biol. Chem.257(6)3105-3109(1982)

Tunicamycin 17:1 is a mixture of tunicamycin structural isomers that contain a 17-carbon N-acyl chain with variable branching patterns. The N-acyl chain incorporated into tunicamycins, like tunicamycin 17:1, is derived from the same pool of cellular branched-chain fatty acids (BCFAs) inStreptomycesand directly impacts the biological activity of each individual tunicamycin variant.1,2,3Purified tunicamycin 17:1 withisooranteisobranching configurations inhibits bacterial phospho-MurNAc-pentapeptide transferase (MraY) with IC50values of 0.12 and 0.9 μM, respectively.2 1.Price, N.P.J., Jackson, M.A., Hartman, T.M., et al.Branched chain lipid metabolism as a determinant of the N-Acyl variation of Streptomyces natural productsACS Chem. Biol.16(1)116-124(2021) 2.Hering, J., Dunevall, E., Snijder, A., et al.Exploring the active site of the antibacterial target MraY by modified tunicamycinsACS Chem Biol.15(11)2885-2895(2020) 3.Duksin, D., and Mahoney, W.C.Relationship of the structure and biological activity of the natural homologues of tunicamycinJ. Biol. Chem.257(6)3105-3109(1982)

PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. PKR-IN-C16 protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.

Endoplasmic reticulum (ER) stress, caused by accumulation of misfolded proteins and a disruption of calcium homeostasis, has been linked to several neuronal diseases including, Parkinson's, Alzheimer's, and prion diseases. A screen for protective activity against ER stress-dependent cell death identified termitomycamides, extracts from the fruiting bodies of T. titanicus, a notably large edible mushroom that is cultivated symbiotically in the nests of termites Termitomycamide B is a fatty acid isolated from T. titanicus that at a dose of 0.1 μg/ml protects against ER stress-dependent cell death in Neuro2a cells induced by tunicamycin.

TunR1 is an antibiotic and derivative of tunicamycin .1It is active againstB. subtilis(MIC = 0.3 μg/ml) and increases the efficacy of the β-lactam antibiotics oxacillin , methicillin , and penicillin G againstB. subtiliswhen used at a concentration of 0.4 μg/ml. TunR1 (5 μg/ml) is cytotoxic to MDA-MB-231 breast cancer cells and non-cancerous CHO cells. Unlike tunicamycin, TunR1 does not inhibit glycosylation in a protein N-glycosylation assay. 1.Price, N.P., Hartman, T.M., Li, J., et al.Modified tunicamycins with reduced eukaryotic toxicity that enhance the antibacterial activity of β-lactamsJ. Antibiot. (Tokyo)70(11)1070-1077(2017)

TunR2 is an antibiotic and derivative of tunicamycin .1It is active againstB. subtilis(MIC = 0.3 μg/ml) and increases the efficacy of the β-lactam antibiotics oxacillin , methicillin , and penicillin G againstB. subtiliswhen used at a concentration of 0.4 μg/ml. Unlike tunicamycin, TunR2 is non-toxic toS. cerevisiae(MIC = >10 μg/ml) and does not inhibit glycosylation in a protein N-glycosylation assay. TunR2 also has reduced antiproliferative activity against MDA-MB-231 and CHO cells compared with tunicamycin. 1.Price, N.P., Hartman, T.M., Li, J., et al.Modified tunicamycins with reduced eukaryotic toxicity that enhance the antibacterial activity of β-lactamsJ. Antibiot. (Tokyo)70(11)1070-1077(2017)

KUS121 is a valosin-containing protein modulator that inhibits VCP ATPase activity with an IC50 of 330 nM, suppresses tunicamycin-induced ATP depletion, cell death, and CHOP upregulation in HeLa cells, protects primary cortical neurons from oxygen-glucose deprivation injury in vitro, reduces infarct volume and improves motor performance in mouse models of focal cerebral ischemia, and preserves retinal structure and visual function in rd10 retinitis pigmentosa models, supporting its investigation in neuroprotection and ischemic disease research.