GLPBio

UBCS039

Catalog No.: GC34849Purity:>98.50%
UBCS039 هو أول منشط اصطناعي محدد من Sirtuin 6 (SIRT6) ، يحفز الالتهام الذاتي في الخلايا السرطانية البشرية ، مع EC50 من 38 ميكرومتر

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.


UBCS039
Cas No.: 358721-70-7
10mM (in 1mL DMSO)In Stock
$75.00
1
1mgIn Stock
$30.00
1
5mgIn Stock
$68.00
1
10mgIn Stock
$92.00
1
25mgIn Stock
$150.00
1
50mgIn Stock
$213.00
1
100mgIn Stock
$297.00
1
200mgIn Stock
$412.00
1

المراجع (Citations)

1 publicationsمنشورات الباحثين الذين استخدموا هذا المنتج

الوصف (Description)

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.

البروتوكول (Protocol)

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:
[1]. Jiao, Fangzhou, et al. "SIRT6 activator UBCS039 inhibits thioacetamide-induced hepatic injury in vitro and in vivo." Frontiers in Pharmacology 13 (2022): 837544.
[2]. Wang, Yan, et al. "Sirt6 promotes tumor growth and suppresses immune surveillance." Cancer Cell International (2026).

وثائق المنتج (Product Documents)

Purity:>98.50%Appearance:A solid

الخصائص الكيميائية (Chemical Properties)

رقم CAS
358721-70-7
SMILES
N12C(C(C3=CC=CN=C3)NC4=C2C=CC=C4)=CC=C1
الصيغة الجزيئية
C16H13N3
الوزن الجزيئي
247.29
الذوبانية
DMSO : 125 mg/mL (505.48 mM)
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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