Coumermycin A1 |
|
Catalog No.GC62908
|
La cuumermicina A1 es un activador de la seÑal JAK2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 4434-05-3
Sample solution is provided at 25 µL, 10mM.
Coumermycin A1 is an aminocoumarin antibiotic produced by Streptomyces and acts as a DNA gyrase inhibitor. Coumermycin A1 can be used in research related to antibacterial, antiviral, and antitumor activities, as well as serving as a molecular biology tool[1-4].
In vitro, SupT1, Jurkat, HeLa, 293T, HT1080, mTOP cells, and human peripheral blood mononuclear cells were pretreated with Coumermycin A1 (50–2000nM) for 6 hours, followed by infection with HIV-1 virus (m.o.i. = 0.02–0.08) for 24 hours. Coumermycin A1 significantly inhibited HIV-1 integration and gene expression[5]. PC12 cells were pretreated with Coumermycin A1 (100nM) and butyrate (10μM) for 24 hours, followed by stimulation with N-Methyl-4-Phenylpyridinium Iodide (MPP⁺; 500µM) for 24 hours. Coumermycin A1 reversed the butyrate-mediated inhibition of JAK2/STAT3 phosphorylation and attenuated the inhibitory effects of butyrate on MPP⁺-triggered apoptosis, oxidative stress, and inflammatory responses[6].
In vivo, Coumermycin A1 (100µg/kg; single administration) was intraperitoneally injected into DNFB-induced atopic dermatitis (AD) model NC/Nga mice. Coumermycin A1 activated the JAK2/STAT3 pathway and counteracted the therapeutic effect of Naringenin on AD mice[7]. Before sevoflurane exposure, C57BL/6 wild-type mice were treated with Coumermycin A1 (100μg/kg; single intraperitoneal injection) and pAAV-hsyn-miR135b-5p-mCherry-3xFLAG-WPRE (1.2×1013VG/mL; 0.5μl; single targeted injection into the hippocampal CA1 region). Coumermycin A1 abolished the protective effect of miR-135b-5p against sevoflurane-induced cognitive dysfunction[8].
References:
[1] Ryan MJ. Coumermycin A1: A preferential inhibitor of replicative DNA synthesis in Escherichia coli. I. In vivo characterization. Biochemistry. 1976 Aug 24;15(17):3769-77.
[2] Newmark HL, Berger J, Carstensen JT. Coumermycin A1-Biopharmaceutical studies. II. J Pharm Sci. 1970 Sep;59(9):1249-51.
[3] Smee DF. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24.
[4] Spivack JG, O'Boyle DR 2nd, Fraser NW. Novobiocin and coumermycin A1 inhibit viral replication and the reactivation of herpes simplex virus type 1 from the trigeminal ganglia of latently infected mice. J Virol. 1987 Oct;61(10):3288-91.
[5] Vozzolo L, Loh B, Gane PJ, et al. Gyrase B inhibitor impairs HIV-1 replication by targeting Hsp90 and the capsid protein. J Biol Chem. 2010 Dec 10;285(50):39314-28.
[6] Ji LL, Huang TT, Mao LL, et al. The gut microbiota metabolite butyrate mitigates MPTP/MPP+ -induced Parkinson's disease by inhibiting the JAK2/STAT3 signaling pathway. Kaohsiung J Med Sci. 2023 Oct;39(10):1002-1010.
[7] Tian L, Wang M, Wang Y, et al. Naringenin ameliorates atopic dermatitis by inhibiting inflammation and enhancing immunity through the JAK2/STAT3 pathway. Genes Genomics. 2024 Mar;46(3):333-340.
[8] Guo FH, Xie T, Kang JM, et al. MiR-135b-5p relieves sevoflurane-induced postoperative cognitive dysfunction by inhibiting JAK2-STAT3-mediated hepcidin upregulation. Brain Res Bull. 2026 Apr;237:111785.
| Cell experiment [1]: | |
Cell lines | HeLa cells (human epithelial immortal cell line), 293T cells (human embryonic kidney epithelial), HT1080 cells (human fibrosarcoma), SupT1 cells (human CD4+ lymphoblastic leukemia), Jurkat cells (human CD4+ acute lymphoblastic leukemia), and mTOP cells (mouse fibroblasts) |
Preparation Method | Cells were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal calf serum (FCS) at 37°C in 5% CO2. Cells were incubated with Coumermycin A1 for 6 hours, then infected with VSV-G pseudotyped HIV-1 vector or HIV-1 LAI△env virus. |
Reaction Conditions | 1µM; 6h |
Applications | Coumermycin A1 inhibited HIV-1 integration and gene expression from acutely infected cells. Coumermycin A1 targeted Hsp90 and the capsid protein, and inhibited Hsp90 dimer formation. |
| Animal experiment [2]: | |
Animal models | the AD-like skin lesions NC/Nga mice |
Preparation Method | A severe AD model were intraperitoneally injected once with 50mg/kg or 100mg/kg Naringenin on the 7th and 13th day of DNFB induction. Mice were intraperitoneally administered with 100µg/kg Coumermycin A1 after Naringenin treatment. |
Dosage form | 100µg/kg; i.p.; single injection |
Applications | Coumermycin A1 activated the JAK2/STAT3 pathway, partially offsetting the therapeutic effects of Naringenin on AD mice. |
References: | |
| Cas No. | 4434-05-3 | SDF | |
| Formula | C55H59N5O20 | M.Wt | 1110.08 |
| Solubility | DMSO : 50 mg/mL (45.04 mM; Need ultrasonic and warming) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 900.8 μL | 4.5042 mL | 9.0084 mL |
| 5 mM | 180.2 μL | 900.8 μL | 1.8017 mL |
| 10 mM | 90.1 μL | 450.4 μL | 900.8 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)