Chuangxinmycin
Chuangxinmycin is a tryptophanyl-tRNA synthetase inhibitor. Chuangxinmycin blocks protein synthesis by competitively binding to the tryptophan/ATP pocket of bacterial TrpRS, exhibits broad-spectrum antibacterial activity against Gram-positive and Gram-negative bacteria, and shows antimycobacterial activity against susceptible, drug-resistant, and intracellular M. tuberculosis. Chuangxinmycin induces PTC readthrough and restores full-length Collagenase, Type VII (HY-E70005J), and can be used for research on tuberculosis, RDEB, and Escherichia coli/Shigella dysenteriae infections.
For research use only. We do not sell to patients.
- CAS No.: 63339-68-4
- Formula: C12H11NO2S
- Molecular Weight:233.29
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
In Vitro
Chuangxinmycin inhibits aminoacylation by purified recombinant Staphylococcus aureus WRS, with an IC50 of approximately 30 nM[4].
Chuangxinmycin (2 μg/mL; 48 h) sensitivity is increased by CRISPRi knockdown of trpS or trpE in Mycobacterium smegmatis mc2155[5].
Chuangxinmycin (5-20 μg/mL and 20-80 × MIC; one month) selection generates spontaneous Mtb H37Rv and H37Ra mutants with trpE mutations and trpS promoter mutations, but no trpS coding region mutations[5].
Chuangxinmycin (1-100 µg/mL Vitamin B12 (HY-B0315); cultured on ISP2 plates at 28°C for 7 days; cultured in a 42 L bioreactor at 28°C for 100 h) is produced by engineered Streptomyces coelicolor M1452/pL-CxnA1-F and Actinoplanes jinanensis 200056/2027-CxnR in M2 medium, with a yield of up to 301 mg/L[7].
Chuangxinmycin (64-0.125 µg/mL; other bacteria treated at 37°C for 10 h) inhibits Mycobacterium tuberculosis H37Rv with an MIC of 1 µg/mL[7].
Chuangxinmycin (10-50 µM; 24 h) downregulates inflammatory gene signatures in RDEB_L1 and NHK cells but does not modulate translation-related pathways, thereby distinguishing its transcriptomic signature from that of aminoglycosides[2].
Chuangxinmycin (≤ 30 μM) is a potent and selective competitive inhibitor of Staphylococcus aureus tryptophanyl-tRNA synthetase, with Ki = 20 nM, and shows no inhibitory effect on sheep WRS[3].
Chuangxinmycin inhibits WRS in a scintillation proximity assay with an IC50 of 90-200 nM[4].
Chuangxinmycin (0.390625-200 μM; 30-40 min) binds to Mtb TrpRS with a Kd of 3.2 μM and inhibits its catalytic PPi production in the EnzChek phosphate assay[5].
Chuangxinmycin (1.8 M K2HPO4; 1.5% v/v 1,3-propanediol; pH 7.6; 37°C) binds to the substrate-binding pocket of GsTrpRS through a D132 hydrogen bond and hydrophobic contacts with M129, I133, and V141[6].
Chuangxinmycin (150 μM; 25°C) binds to GsTrpRS WT through an enthalpy-driven interaction with a Kd of 3.1 μM, whereas mutations M129A, D132A, I133A, and V141A abolish detectable binding[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human hepatocellular carcinoma Huh7 and Huh7.5 cells and African green monkey kidney Vero E6 cells
-
Concentration:128 or 64 µg/mL initial concentration, threefold serial dilutions for seven dilutions
-
Incubation Time:48 h
-
Result:No obvious cytotoxicity was exhibited, with CC50 values ≥ 64 µg/mL at least, across Huh7, Huh7.5, and Vero cells.
Chemical Information
-
CAS No. 63339-68-4
-
Molecular Weight 233.29
-
Formula C12H11NO2S
-
SMILES
C[C@H]1C2=CNC3=CC=CC(S[C@H]1C(O)=O)=C23
-
Structure Classification
-
Initial Source
Actinoplanes tsinanensis
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Chuangxinmycin Related Classifications
HY-N14092 Related Classifications
Powered by Bioz