UK-5099
Catalog No.: GC11865Purity:>99.50%Synonyms: PF-1005023;UK5099;UK 5099;PF1005023;PF 1005023
UK-5099 is a mitochondrial pyruvate carrier (MPC) inhibitor with an IC50 value of 50nM for inhibiting pyruvate-dependent O2 consumption.
المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.
Cas No.: 56396-35-1
10mgIn Stock
$79.00
1
50mgIn Stock
$338.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mg | $79.00 | In Stock | 1 | |
| 50mg | $338.00 | In Stock | 1 |
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المراجع (Citations)
1 publicationsمنشورات الباحثين الذين استخدموا هذا المنتجالوصف (Description)
UK-5099 is a mitochondrial pyruvate carrier (MPC) inhibitor with an IC50 value of 50nM for inhibiting pyruvate-dependent O2 consumption[1]. UK-5099 is an α-cyanocinnamate derivative that blocks pyruvate entry into mitochondria, impairs mitochondrial oxidative phosphorylation and triggers aerobic glycolysis[2]. UK-5099 can increase glutamate oxidation and prevent excitotoxic neuronal death[3].
In vitro, UK-5099 (25, 50µM) treatment of bone marrow-derived macrophages for 30min dose-dependently reduced the formation of the adaptor protein apoptosis-associated speck-like protein containing CARD (ASC)[4]. UK-5099 (40, 80µM) treatment of microglia significantly reduced the nuclear signal intensity of NF-κB and NF-IL6 in cells[5]. UK-5099 (10-150µM) treatment of 832/13 cells dose-dependently inhibited glucose-stimulated insulin secretion in cells[6].
In vivo, UK-5099 (3mg/kg) was intraperitoneally injected into mice bearing non-small cell lung cancer xenografts and synergized with syrosingopine to inhibit tumor growth[7].
References:
[1] Halestrap A P. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors[J]. Biochemical Journal, 1975, 148(1): 85-96.
[2] Zeng Q, Si H, Lv K, et al. Determination and pharmacokinetics study of UK-5099 in mouse plasma by LC–MS/MS[J]. BMC Veterinary Research, 2022, 18(1): 145.
[3] Quansah E, Peelaerts W, Langston J W, et al. Targeting energy metabolism via the mitochondrial pyruvate carrier as a novel approach to attenuate neurodegeneration[J]. Molecular Neurodegeneration, 2018, 13: 1-12.
[4] Ran L, Chen M, Ye J, et al. UK5099 Inhibits the NLRP3 Inflammasome Independently of its Long‐Established Target Mitochondrial Pyruvate Carrier[J]. Advanced Science, 2024, 11(33): 2307224.
[5] Guimarães N C, Alves D S, Vilela W R, et al. Mitochondrial pyruvate carrier as a key regulator of fever and neuroinflammation[J]. Brain, Behavior, and Immunity, 2021, 92: 90-101.
[6] Patterson J N, Cousteils K, Lou J W, et al. Mitochondrial metabolism of pyruvate is essential for regulating glucose-stimulated insulin secretion[J]. Journal of Biological Chemistry, 2014, 289(19): 13335-13346.
[7] Li Y, Song Y, Shi Z, et al. Syrosingopine and UK5099 synergistically suppress non-small cell lung cancer by activating the integrated stress response[J]. Cell Death & Disease, 2024, 15(6): 431.
البروتوكول (Protocol)
| Cell experiment [1]: | |
Cell lines | Bone marrow-derived macrophages (BMDMs) |
Preparation Method | BMDMs isolated from ASC reporter mice (ASCcitrine BMDMs) were plated on chamber slides at 1×106/mL. Cells were primed the following day with LPS for 3h. After washing with PBS, cells were treated with 25µM or 50µM UK-5099 for 30min, followed by stimulation with nigericin for 1h. The cells were then washed with ice-cold PBS three times and fixed for 15min in fixation solution consisting of 4% PFA in PBS. After three times washing with PBST, nuclei were stained with DAPI. Images were captured using a laser-scanning confocal microscopy. |
Reaction Conditions | 25, 50µM; 30min |
Applications | ASC fluorescence was evenly distributed in resting macrophages, and the formation of dense specks was evident after stimulation with LPS plus nigericin. UK-5099 dose-dependently reduced the formation of ASC specks. |
| Animal experiment [2]: | |
Animal models | Balb/c nude mice |
Preparation Method | 5×106 PC-9 cells were subcutaneously inoculated into the Balb/c nude mice. Once the tumor volumes reached 50mm3, the mice were divided into four groups, each consisting of six mice: Control (PBS), Syrosingopine (7.5mg/kg), UK-5099 (3mg/kg), and a combination of Syrosingopine and UK-5099. Treatments, including Syrosingopine, UK-5099, or PBS, were administered to the mice through intraperitoneal injections continuously for 14 days. Throughout this period, observations were diligently made, recording the tumor volume and weight for subsequent analysis. |
Dosage form | 3mg/kg for 14 days; i.p. |
Applications | In vivo inhibition of tumor growth by the combination of Syrosingopine and UK-5099. |
References: | |
وثائق المنتج (Product Documents)
Purity:>99.50%Appearance:A solid
البيانات البيولوجية (Biological Data)
1 / 1
الخصائص الكيميائية (Chemical Properties)
رقم CAS
56396-35-1
المرادفات
PF-1005023;UK5099;UK 5099;PF1005023;PF 1005023
الاسم الكيميائي
(E)-2-cyano-3-(1-phenylindol-3-yl)prop-2-enoic acid
SMILES
C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O
الصيغة الجزيئية
C18H12N2O2
الوزن الجزيئي
288.3
الذوبانية
≥ 28.8 mg/mL in DMSO
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.
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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