5.30353
Regacin
Synonym(s):
Regacin, 5-((4-Chlorobenzyl)sulfanyl)-1,3,4-thiadiazol-2-amine, Virulence Regulator RegA Inhibitor, NSC-523933
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About This Item
Empirical Formula (Hill Notation):
C9H8ClN3S2
CAS Number:
Molecular Weight:
257.76
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
assay
≥95% (HPLC)
Quality Level
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
InChI
1S/C9H8ClN3S2/c10-7-3-1-6(2-4-7)5-14-9-13-12-8(11)15-9/h1-4H,5H2,(H2,11,12)
InChI key
SPABJFQNGHSGMG-UHFFFAOYSA-N
General description
An orally bioavailable, non-toxic, thio-thiadiazolamine compound that specifically inhibits the DNA-binding capacity of virulence regulator, RegA (IC50 = 1.7 µM in E. coli strain MC4100 (kfc-lacZ, pACYC184-regA), by interacting with amino acid residues within a conserved region of the DNA-binding domain, but without affecting RegA dimerization. Interacts with the double helix-turn-helix (HTH) domain that results in a loss of binding affinity of RegA for its DNA targets. This interaction appears to involve W188 and R223 residues that are conserved in several RegA homologs including ToxT, AggR, RegR, and Rns. Shown to be highly effective in reducing Citrobacter rodentium colonization when administered perorally to mice (~50 mg/kg) either 15 minutes before or 12 hours after bacterial inoculation. Reduces the ability of Rns and RegR to activate the transcription of their target promoters, but does not affect the activity of AggR and ToxT.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
RegA
RegA
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Yang, J., et al. 2013. J. Biol. Chem.288, 31115.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
新产品
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Ji Yang et al.
The Journal of biological chemistry, 288(43), 31115-31126 (2013-09-11)
The misuse of antibiotics during past decades has led to pervasive antibiotic resistance in bacteria. Hence, there is an urgent need for the development of new and alternative approaches to combat bacterial infections. In most bacterial pathogens the expression of
Global Trade Item Number
| SKU | GTIN |
|---|---|
| 5303530001 | 04055977260755 |