UBCS039 |
Catalog No.GC34849
One-Click Copy Product Info
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UBCS039 is a synthetic specific activator of SIRT6, with EC50 value of 38μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 358721-70-7
Sample solution is provided at 25 µL, 10mM.
UBCS039 is a synthetic specific activator of SIRT6, with EC50 value of 38μM[1]. UBCS039 is often used in studies of SIRT6-mediated autophagy, anti-inflammatory effects, antioxidant stress, lipid metabolism, macrophage polarization, renal and hepatic injury, and thrombosis[1].
In vitro, UBCS039 (75-100μM; 24-72h) treatment induced H3K9 deacetylation, promoted the increase of LC3B-II, the formation of GFP-LC3 puncta. UBCS039 (100μM; 72h) treatment induced ROS-AMPK/ULK1/mTOR-related autophagy and autophagy-related cell death and apoptosis in H1299 and HeLa cells[2]. UBCS039 (40μM; 2h) pretreatment inhibited lipopolysaccharide (10μg/ml; 24h)-induced inflammatory responses in RAW264.7 macrophages[3]. UBCS039 (40μM; 24h) inhibited the oxidative stress in thioacetamide(TAA)-induced hepatocyte injury in LO2 cells[3]. UBCS039 (100μM; 24h) improved the senescence phenotype induced by D-gal, increased cell viability and TERT expression, and reduced cell apoptosis, ROS, HK2 and SA-β-gal levels in H9c2 cardiac muscle cells[4].
In vivo, UBCS039 (10mg/kg; i.p.; once every 3 days for a total of five injections) promoted the growth of various tumor xenografts, and elevated levels of GM-CSF, IL-10, and ADO, decreased IFN-γ, as well as increased indicators related to PD-L1, PD-1, and M2 macrophages/TAM[5]. UBCS039 (30mg/kg; i.p.; once) reduced lipid accumulation in the renal tissues and apoptosis of renal tubular epithelial cells in LPS-induced acute kidney injury (AKI) mice[6].
References:
[1]. You, Weijie, et al. "Structural basis of sirtuin 6 activation by synthetic small molecules." Angewandte Chemie International Edition 56.4 (2017): 1007-1011.
[2]. Iachettini, Sara, et al. "Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells." Cell death & disease 9.10 (2018): 996.
[3]. Jiao, Fangzhou, et al. "SIRT6 activator UBCS039 inhibits thioacetamide-induced hepatic injury in vitro and in vivo." Frontiers in Pharmacology 13 (2022): 837544.
[4]. Zhou, Hongji, et al. "Downregulation of Sirt6 by CD38 promotes cell senescence and aging." Aging (albany NY) 14.23 (2022): 9730.
[5]. Wang, Yan, et al. "Sirt6 promotes tumor growth and suppresses immune surveillance." Cancer Cell International (2026).
[6]. Wang, Dan, et al. "SIRT6 mitigates acute kidney injury by enhancing lipid metabolism and reducing tubular epithelial cell apoptosis via suppression of the ACMSD signaling pathway." Cellular Signalling 131 (2025): 111757.
| Cell experiment [1]: | |
Cell lines | RAW264.7 cells |
Preparation Method | The cells were cultured in 96-well plates at a density of 1×104 cells/well, and then the cells were exposed to different concentrations of UBCS039 for 24h. After treatment, the culture medium was replaced with 10μl CCK-8 solution and 90μl medium for 1h at 37°C. |
Reaction Conditions | 0-200μM; 24h |
Applications | High doses of UBCS039 (50μM, 100μM, and 200μM) were cytotoxic to macrophages, with a cell viability lower than 90%. |
| Animal experiment [2]: | |
Animal models | Sixty five-week-old healthy female BALB/c nude mice (BALB/c FOXN1-/-) |
Preparation Method | Mice were randomly assigned to groups. Every three days, each group was given intraperitoneal UBCS039, PBS, or DMSO injections at a 10mg/kg concentration, for a total of five injections. Each group included twenty mice. Cultured HeLa, LM3, Hcc827 or MDA-MB-231 cells were collected and resuspended in PBS 1 day after the final UBCS039 injection into nude mice. Mice pretreated with UBCS039 received a subcutaneous injection of 1 × 107 cells/ml into the right axillary area. |
Dosage form | 10mg/kg; i.p.; administered once every 3 days for 5 times |
Applications | UBCS039 promoted the growth of various tumor xenografts, and elevated levels of GM-CSF, IL-10, and ADO, decreased IFN-γ, as well as increased indicators related to PD-L1, PD-1, and M2 macrophages/TAM. |
References: | |
| Cas No. | 358721-70-7 | SDF | |
| Canonical SMILES | N12C(C(C3=CC=CN=C3)NC4=C2C=CC=C4)=CC=C1 | ||
| Formula | C16H13N3 | M.Wt | 247.29 |
| Solubility | DMSO : 125 mg/mL (505.48 mM) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0438 mL | 20.2192 mL | 40.4384 mL |
| 5 mM | 808.8 μL | 4.0438 mL | 8.0877 mL |
| 10 mM | 404.4 μL | 2.0219 mL | 4.0438 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)