MS-347a
MS-347a is an inhibitor of myosin light chain kinase (MLCK) and protein kinase C (PKC), with IC50 values of 9.2 μM, 31 μM and 16 μM against calmodulin-dependent MLCK, calmodulin-independent MLCK and PKC, respectively. MS-347a binds to the catalytic domain of MLCK and blocks both calmodulin-dependent and calmodulin-independent MLCK activity. MS-347a inhibits the growth of drug-sensitive fission yeast and multiple ascomycete phytopathogenic fungi. MS-347a exhibits fungicidal activity against a variety of phytopathogenic fungi and protective activity against Magnaporthe oryzae in rice seedlings. MS-347a shows antibacterial activity against specific Gram-positive bacteria and Proteus vulgaris. MS-347a can be used in studies related to rice blast, bacterial infections and phytopathogenic fungal diseases.
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- CAS No.: 144678-18-2
- 화학식: C16H12O7
- 분자량:316.26
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PKC 16 μM (IC50) |
MLCK 9.2 μM (IC50, Calmodulin-dependent MLCK activity) |
MLCK 31 μM (IC50, Calmodulin-independent MLCK activity) |
MS-347a (10-40 min) potently inhibits calmodulin-dependent chicken gizzard myosin light chain kinase (MLCK) with an IC50 value of 9.2 μM, and this inhibitory effect is time-dependent, reaching a peak after pre-incubation at a concentration of 15 μM for 20 minutes[1].
MS-347a inhibits calmodulin-independent trypsin-digested chicken gizzard myosin light chain kinase (MLCK) with an IC50 of 31 μM[1].
MS-347a inhibits protein kinase C in rat brain with an IC50 of 16 μM; at concentrations up to 150 μM, it does not inhibit calmodulin-dependent cyclic nucleotide phosphodiesterase, cAMP-dependent protein kinase, or cGMP-dependent protein kinase[1].
MS-347a (0.4-100 μg/mL) exhibits antibacterial activity against Gram-positive bacteria and *Proteus vulgaris* ATCC 6897, with MIC values ranging from 0.4 to 3.0 μg/mL. However, at the highest concentration of 100 μg/mL, it shows no activity against Gram-negative bacteria (except *Proteus vulgaris*) and *Candida albicans*[1].
MS-347a (0.03-10 µg/disk; 3 days) exhibits broad-spectrum antifungal activity against Pyricularia oryzae APU15-60A (QoIS), Pyricularia oryzae APU15-63A (QoIR), Botrytis cinerea MAFF-306820, Leptosphaeria maculans MAFF-726728, and Colletotrichum gloeosporioides MAFF-237219. Among these pathogens, the largest inhibition zone, reaching 24.19 mm, is observed against Pyricularia oryzae APU15-60A (QoIS) at the dose of 10 µg/disk[3].
MS-347a (1-30 μg/disk; 3 days) exhibits potent antifungal activity against Saccharomyces cerevisiae BY4741 12gene-0HSR-iERG6, and its activity in YPG medium (inhibition zone diameter of 15.7 mm at 30 μg/disk) is higher than that in YPD medium (inhibition zone diameter of 11 mm at 30 μg/disk)[2].
MS-347a (0.01-10 μg/disk; 3 days) exhibits broad-spectrum antifungal activity against plant pathogenic fungi belonging to Ascomycota, and is effective against both QoI-sensitive and QoI-resistant Pyricularia oryzae strains. Among these, it shows the strongest activity against the QoI-sensitive Pyricularia oryzae strain APU15-60A, with an inhibition zone diameter of 25.91 mm at 10 μg/disk[2].
MS-347a (up to 128 μg/mL) selectively inhibits the growth of drug-hypersensitive fission yeast (S. pombe 7Δ) with an MIC of 1 μg/mL; it exhibits a selectivity up to 32-fold over multidrug-sensitive budding yeast (S. cerevisiae 12geneΔ0HSR-iERG6), and shows no activity against wild-type fission yeast, 2Δ fission yeast, or wild-type budding yeast at concentrations up to 128 μg/mL[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 144678-18-2
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분자량 316.26
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화학식 C16H12O7
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SMILES
O=C(C12OC1C=CC(OC3=CC(CO)=CC(O)=C34)=C2C4=O)OC
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Structure Classification
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Initial Source
Aspergillus sp.
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Nakanishi S, et al. MS-347a, a new inhibitor of myosin light chain kinase from Aspergillus sp. KY52178. The Journal of antibiotics. 1993 Dec;46(12):1775-81. [Content Brief]
[2]. Honma S, et al. Re-discovery of MS-347a as a Fungicide Candidate through a New Drug Discovery Platform with a Multidrug-Sensitive Saccharomyces cerevisiae Screening System and the Introduction of a Global Secondary Metabolism Regulator, laeA Gene. Biosci Biotechnol Biochem. 2024;88:824-829. [Content Brief]
[3]. Kimishima A, et al. Synthesis and biological evaluation of MS-347a derivatives against plant pathogenic fungi based on a strategy of gene introduction. Journal of pesticide science. 2024 Nov 20;49(4):224-231. [Content Brief]
[4]. Kimishima A, et al. Construction of a New Drug and Agrochemical Candidates Screening Platform Utilizing Drug-Hypersensitive Fission Yeast to Discover Overlooked Natural Products. Journal of natural products. 2025 Sep 26;88(9):2090-2096. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS-347a Related Classifications
HY-N19735 Related Classifications
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