Novobiocin sodium
Based on 14 publication(s) in Google Scholar
Novobiocin (Albamycin; Cathomycin) sodium is an orally active antibiotic and Hsp-90 antagonist that also inhibits the Polθ helicase/ATPase domain with IC50 values of 24 μM and 15-17 μM, respectively. Novobiocin sodium binds to Hsp90, GyrB, and POLθ, inhibiting their ATPase activity and ssDNA binding. Novobiocin sodium inhibits molecular chaperone function and DNA repair, and induces apoptosis and genomic instability. Novobiocin sodium exhibits bactericidal and antiparasitic activities. Novobiocin sodium inhibits tumor growth in vivo. Novobiocin sodium is used for research on equine piroplasmosis, ovarian cancer, breast cancer, anthrax, and melioidosis.
For research use only. We do not sell to patients.
- Purity : 99.07%
- CAS No.: 1476-53-5
- Formula: C31H35N2NaO11
- Molecular Weight:634.61
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Novobiocin sodium
More- Nat Methods. 2023 Sep;20(9):1388-1399. [Abstract]
- Blood. 2018 Jul 19;132(3):307-320. [Abstract]
- Adv Sci (Weinh). 2022 Dec;9(34):e2203088. [Abstract]
- Cell Rep Med. 2024 Jun 18;5(6):101592. [Abstract]
- Mol Ther. 2026 Jul 20:S1525-0016(26)00602-7.
- Mol Cancer Ther. 2026 Jul 15:10.1158/1535-7163.MCT-26-0182.
- Int J Mol Sci. 2019 Mar 5;20(5):1125. [Abstract]
- PLoS Pathog. 2026 Jan 26;22(1):e1013903. [Abstract]
- Mol Pharm. 2022 Nov 7;19(11):4320-4332. [Abstract]
- Cancer Res Commun. 2024 Apr 9;4(4):1024-1040. [Abstract]
- J Med Virol. 2025 Oct;97(10):e70655. [Abstract]
- Surgery. 2024 Nov;176(5):1380-1387. [Abstract]
- Vet Microbiol. 2026 May:316:110992. [Abstract]
- bioRxiv. 2025 Sep 15.
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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WB
All Antibiotic Isoforms
MoreAll DNA/RNA Synthesis Isoforms
MoreAll Parasite Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
β-lactam |
HSP90 |
In Vitro
Novobiocin (1-2000 μM; 24 h) sodium shows low cytotoxicity against horse PBMCs, with a CC50 of 11.63 mM and an SSI of 70.47, indicating its safety for mammalian cells[1].
Novobiocin sodium exhibits low in vitro effective concentrations against both Bacillus anthracis and Burkholderia pseudomallei[5].
Novobiocin sodium shows increased resistance in POLQ-deficient U2OS cells[3].
Novobiocin sodium acts synergistically with Rucaparib (HY-10617A) to reduce the survival rate of BRCA1-/- RPE1 cells and decrease the IC50 of Rucaparib[3].
Novobiocin sodium synergizes with Olaparib in HR-deficient TOV21G + EV cells, reducing the IC50 of Olaparib by more than 40-fold[3].
Novobiocin sodium is cytotoxic to multiple PARPi-resistant clones derived from RPE1-BRCA1-/- cells[3].
Novobiocin sodium inhibits MMEJ repair but not HR repair in U2OS cells[3].
Novobiocin sodium increases IR-induced RAD51 and γH2AX foci formation in U2OS cells[3].
Novobiocin sodium induces chromosomal aberrations and radial chromosomes in BRCA1-/- RPE1 cells[3].
Novobiocin (120 nM-1 mM; 1 h pre-incubation, 2 h reaction) sodium is a non-ATP-competitive inhibitor of Polθ-ATPase activity[4].
Novobiocin (4 mM; 30 min) sodium binds to the allosteric site of the Polθ-ATPase domain, affecting ATP hydrolysis and stabilizing the core of this domain[4].
Novobiocin sodium blocks the binding of Polθ to ssDNA in vitro[4].
Novobiocin (500 μM; 30 min) sodium stabilizes the Polθ-ATPase domain[4].
Novobiocin (500 μM; 1 h) sodium promotes tetramerization of the Polθ-ATPase domain[4].
Novobiocin (50-200 μM; 24 h) sodium blocks the binding of intracellular Polθ to ssDNA in a dose-dependent manner[4].
Novobiocin (200 μM; 2 h) sodium treatment leads to the accumulation of ssDNA gaps in RPE1 TP53-/- BRCA1-/- cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Theileria equi and Babesia caballi parasitized horse red blood cells (RBCs)
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Concentration:1, 5, 10, 20, 50, 100, 200 μM (T. equi); 10, 20, 50, 100, 200 μM (B. caballi)
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Incubation Time:96 h
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Result:Inhibited the in vitro growth of Theileria equi with an IC50 of 165 μM.
Inhibited the in vitro growth of Babesia caballi with an IC50 of 84.85 μM.
Showed significant growth inhibition of T. equi at 100 μM and 200 μM at 24 h and 48 h.
Showed significant growth inhibition of T. equi at ≥20 μM at 72 h and 96 h.
Showed significant growth inhibition of B. caballi at 100 and 200 μM at 24, 48, 72, and 96 h.
Caused parasite death at 100 μM and 200 μM after 96 h.
Failed to inhibit growth at 1-50 μM (T. equi) and 10-50 μM (B. caballi) in viability studies.
Induced dot-shaped/distorted nuclear material at 100 and 200 μM after 96 h.
Showed no recrudescence at 100 and 200 μM in viability testing.
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Cell Line:Equine peripheral blood mononuclear cells (PBMCs)
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Concentration:1, 5, 10, 25, 50, 100, 1000, 2000 μM
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Incubation Time:24 h
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Result:Showed less than 10% cytotoxicity at 1000 μM.
Exhibited a CC50 of 11.63 mM.
Demonstrated a specific selective index (SSI) of 70.47.
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Cell Line:U2OS POLQ knockout cells expressing Myc-tagged Polθ
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Concentration:50 μM, 100 μM, 200 μM
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Incubation Time:24 h
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Result:Reduced Polθ recruitment to ssDNA in cells in a dose-dependent manner.
Blocked 96% of Polθ from being recruited to damage sites at the highest dose of 200 μM.
In Vivo
Novobiocin (100 mg/kg; i.p.; twice daily; 4 weeks) sodium specifically inhibits the growth of FANCF-deficient HR-defective tumors in vivo [3].
Novobiocin (75 mg/kg; i.p.; twice daily; 4 weeks) sodium alone induces tumor regression and, in combination with Olaparib (HY-10162), achieves tumor regression in the HR-deficient DF83 PDX model[3].
Novobiocin (75 mg/kg; i.p.; twice daily; 4 weeks) sodium significantly inhibits tumor growth in the PARPi-resistant DF59 PDX model[3].
Novobiocin (75 mg/kg; i.p.; twice daily; 4 weeks) sodium does not inhibit tumor growth in the DF149 PDX model with normal HR function, which is associated with low POLθ expression[3].
Novobiocin (2.5 mg; i.p.; 2-5 doses) sodium significantly prolongs time to death but does not significantly improve overall survival in the highly lethal inhalational anthrax model in A/J mice[5].
Novobiocin (2.5 mg; i.p.; 4 doses; 7 days) sodium provides 70% protection against lethal aerosolized B. pseudomallei infection in BALB/c mice, and bacterial burden is typically undetectable in the tissues of surviving mice[5].
Novobiocin (2.5 mg; i.p.; 3 doses) sodium significantly synergizes with live attenuated vaccine, improving survival and prolonging time to death in a lethal aerosol B. pseudomallei model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (strain not specified)[1]
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Dosage:5, 10, 20, 50, and 100 mg/kg
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Administration:i.p.; single dose
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Result:Induced a significant rise in serum glutamic oxaloacetic transaminase (SGOT) and serum glutamic pyruvic transaminase (SGPT) in mice at 100 mg/kg at 24 h, which decreased to non-significant levels thereafter.
Showed non-significant differences in kidney biochemical markers (creatinine, blood urea nitrogen) and other parameters (bilirubin and total protein) at different time intervals.
Exhibited minimal diffuse cytoplasmic rarefaction and vacuolation in hepatocytes at 100 mg/kg.
Showed no adverse histopathological changes in any organ at other doses.
Identified 50 mg/kg as the No Observed Adverse Effect Level (NOAEL).
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Animal Model:FVB/129P2 (female, at least 6 weeks old, K14-Cre-Brca1^f/f;Trp53^f/f GEMM tumor transplanted into mammary fat pad)[3]
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Dosage:100 mg/kg
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Administration:i.p.; twice a day; 35 days
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Result:Significantly suppressed tumor growth after 7 days of treatment and beyond.
Prolonged overall survival by 3-fold compared to vehicle, with median survival times of 29 and 10 days for treated and vehicle groups, respectively.
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Animal Model:NU(NCr)-Foxn1^nu athymic nude (female)[3]
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Dosage:100 mg/kg
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Administration:i.p.; twice a day; 4 weeks
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Result:Specifically impaired the growth of FANCF-deficient tumors, with no effect on FANCF-complemented tumors.
Strongly induced RAD51 foci in the treated tumors.
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Animal Model:NSG (female, 8 weeks old)[3]
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Dosage:75 mg/kg
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Administration:i.p.; twice daily; 4 weeks
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Result:Led to tumor regression as a single agent, while tumors in vehicle-treated mice showed exponential growth.
Achieved complete tumor regression in combination with olaparib, with few tumor cells detectable via BLI on day 28.\nSubstantially reduced tumor growth as monotherapy.
In combination with olaparib, further inhibited tumor growth with regression in the first two weeks.
Exhibited higher levels of phospho-RPA32 compared to vehicle-treated samples.
Exhibited a strong increase in RAD51 staining when treated alone or in combination with olaparib.\nDid not inhibit tumor growth in the HR-proficient DF149 PDX model.
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Animal Model:BALB/c mice[5]
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Dosage:1.25 mg; 2.5 mg
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Administration:i.p.; 1, 2, or 3 doses
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Result:Administered 1.25 mg or 2.5 mg in 1, 2, or 3 doses, achieving 70-90% protection except for a single 1.25 mg dose.
Administered 1.25 mg in 3 doses, achieving 90% protection.
Extended time-to-mortality in all treatment groups compared to PBS control.
Resulted in no detectable bacterial burden in spleens of most survivors.
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Animal Model:A/J mice[5]
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Dosage:2.5 mg
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Administration:i.p.; 2, 3, 4, or 5 doses
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Result:Administered 2.5 mg in 2 doses, resulting in a time-to-mortality of 5.8 days.
Administered 2.5 mg in 3 doses, resulting in a time-to-mortality of 6.7 days.
Administered 2.5 mg in 5 doses, resulting in a time-to-mortality of 6.9 days.
Administered 2.5 mg in 4 doses over 7 days, resulting in a time-to-mortality of 8.3 days.
Did not significantly improve overall survival rates by day 21.
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Animal Model:BALB/c mice[5]
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Dosage:2.5 mg
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Administration:i.p.; 2, 3, 4, or 5 doses
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Result:Administered 2.5 mg in 4 doses over 7 days, protecting 70% of mice.
Administered 2.5 mg in 5 doses over 3 days, protecting 60% of mice.
Administered 2.5 mg in 2 doses, protecting 22% of mice.
Administered 2.5 mg in 3 doses, protecting 20% of mice.
Resulted in no detectable bacteria in lung or spleen tissues of any survivors, except for one mouse in the 3-dose group with a bacterial burden of approximately 1.2 × 10^8 CFU/g in the spleen.
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Animal Model:BALB/c mice (vaccinated)[5]
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Dosage:2.5 mg
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Administration:i.p.; 3 doses
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Result:Achieved 80% survival at day 21.
Resulted in a geometric mean time-to-mortality of 35.1 days.
Yielded a synergy score of 3.15.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Patient-Derived Orthotopic Xenograft (PDOX)
- Subcutaneous Cell-Line-Derived Xenograft
- Breast Cancer Modeling
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 1476-53-5
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Appearance Solid
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Molecular Weight 634.61
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Formula C31H35N2NaO11
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Color White to off-white
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SMILES
CC1=C(OC2=O)C(C(O)=C2NC(C3=CC(C/C=C(C)/C)=C(O[Na])C=C3)=O)=CC=C1O[C@H](OC(C)(C)[C@H](OC)[C@H]4OC(N)=O)[C@@H]4O
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Synonyms
Albamycin sodium; Cathomycin sodium
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Initial Source
Streptomyces niveus
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Methods
2023 Sep;20(9):1388-1399. PMID: 37474806
Novobiocin sodium purchased from MedChemExpress. Usage Cited in: Nat Methods. 2023 Sep;20(9):1388-1399. [Abstract]
Editing efficiencies of the VCAN target using Cas9D10A double nicking in H9 hESCs carrying the K3753R mutation and additional small molecules to inhibit the MMEJ repair proteins Polϴ, PARP or Ligase I/III: Novobiocin.
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Blood
Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response. [Abstract]2018 Jul 19;132(3):307-320. PMID: 29724897
Novobiocin sodium purchased from MedChemExpress. Usage Cited in: Blood. 2018 Jul 19;132(3):307-320. [Abstract]
K562, KCL22 and HL60 are treated with the indicated (cytotoxic) concentration of Amidopyrine (AX), Novobiocin (NB) and AUY922 for 48h and later protein lysates are subjected to immunoblot analysis.
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Adv Sci (Weinh)
SRSF5-Mediated Alternative Splicing of M Gene is Essential for Influenza A Virus Replication: A Host-Directed Target Against Influenza Virus. [Abstract]2022 Dec;9(34):e2203088. PMID: 36257906 -
Cell Rep Med
A CD36-dependent non-canonical lipid metabolism program promotes immune escape and resistance to hypomethylating agent therapy in AML. [Abstract]2024 Jun 18;5(6):101592. PMID: 38843841 -
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Int J Mol Sci
Cisplatin Synergistically Enhances Antitumor Potency of Conditionally Replicating Adenovirus via p53 Dependent or Independent Pathways in Human Lung Carcinoma. [Abstract]2019 Mar 5;20(5):1125. PMID: 30841620
Novobiocin sodium purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2019 Mar 5;20(5):1125. [Abstract]
Cell viability assay to analyze the impact of Probenecid and Novobiocin treatments on resistance.
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PLoS Pathog
Anti-orthopoxvirus drugs inhibit lumpy skin disease virus replication by targeting viral DNA polymerase. [Abstract]2026 Jan 26;22(1):e1013903. PMID: 41587213 -
Mol Pharm
2022 Nov 7;19(11):4320-4332. PMID: 36269563 -
Cancer Res Commun
Inhibition of NEK2 Promotes Chemosensitivity and Reduces KSHV-positive Primary Effusion Lymphoma Burden. [Abstract]2024 Apr 9;4(4):1024-1040. PMID: 38592451 -
J Med Virol
Drug Repurposing: In Vitro Evaluation of Simeprevir as a Novel Antiviral Drug Against Severe Fever With Thrombocytopenia Syndrome Virus. [Abstract]2025 Oct;97(10):e70655. PMID: 41117261
Novobiocin sodium purchased from MedChemExpress. Usage Cited in: J Med Virol. 2025 Oct;97(10):e70655. [Abstract]
Novobiocin also reduced NP expression at 25 μM, with mean fluorescence intensities significantly lower than those of the untreated control.
Novobiocin sodium purchased from MedChemExpress. Usage Cited in: J Med Virol. 2025 Oct;97(10):e70655. [Abstract]
Cytoxicity and inhibition of Novobiocin, EC50 = 25.12 μM.
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Surgery
Overexpression of human DNA polymerase theta is a biomarker of aggressive and DNA repair-deficient papillary thyroid cancers. [Abstract]2024 Nov;176(5):1380-1387. PMID: 38897886 -
Vet Microbiol
The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]2026 May:316:110992. PMID: 41865607 -
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (157.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (78.79 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (157.58 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Purity & Documentation
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Data Sheet (296 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[3]. Zhou J, et al. A first-in-class Polymerase Theta Inhibitor selectively targets Homologous-Recombination-Deficient Tumors. Nature cancer. 2021 Jun;2(6):598-610. [Content Brief]
[6]. Marcu MG, et al. The heat shock protein 90 antagonist novobiocin interacts with a previously unrecognized ATP-binding domain in the carboxyl terminus of the chaperone. J Biol Chem. 2000 Nov 24;275(47):37181-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.5758 mL | 7.8789 mL | 15.7577 mL | 39.3943 mL |
| 5 mM | 0.3152 mL | 1.5758 mL | 3.1515 mL | 7.8789 mL | |
| 10 mM | 0.1576 mL | 0.7879 mL | 1.5758 mL | 3.9394 mL | |
| 15 mM | 0.1051 mL | 0.5253 mL | 1.0505 mL | 2.6263 mL | |
| 20 mM | 0.0788 mL | 0.3939 mL | 0.7879 mL | 1.9697 mL | |
| 25 mM | 0.0630 mL | 0.3152 mL | 0.6303 mL | 1.5758 mL | |
| 30 mM | 0.0525 mL | 0.2626 mL | 0.5253 mL | 1.3131 mL | |
| 40 mM | 0.0394 mL | 0.1970 mL | 0.3939 mL | 0.9849 mL | |
| 50 mM | 0.0315 mL | 0.1576 mL | 0.3152 mL | 0.7879 mL | |
| 60 mM | 0.0263 mL | 0.1313 mL | 0.2626 mL | 0.6566 mL | |
| DMSO | 80 mM | 0.0197 mL | 0.0985 mL | 0.1970 mL | 0.4924 mL |
| 100 mM | 0.0158 mL | 0.0788 mL | 0.1576 mL | 0.3939 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Keywords
- Novobiocin
- 1476-53-5
- Albamycin
- Cathomycin
- Antibiotic
- DNA/RNA Synthesis
- HSP
- Apoptosis
- Bacterial
- Parasite
- Theileria equi
- POLθ ATPase domain
- Hsp-90 inhibitor
- U2OS cells
- BRCA1-/- RPE1 cells
- microhomology-mediated end joining repair
- N. gonorrhoeae
- Babesia caballi
- Bacillus anthracis
- Burkholderia pseudomallei
- Inhibitor
- inhibitor
- inhibit