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.
Products are for research use only. Not for human use. We do not sell to patients.
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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Citations
1 publicationsPublications from researchers using this productDescription
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.
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: | |
Product Documents
Purity:>99.50%Appearance:A solid
Biological Data
1 / 1
Chemical Properties
CAS No.
56396-35-1
Synonyms
PF-1005023;UK5099;UK 5099;PF1005023;PF 1005023
Chemical Name
(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
Molecular Formula
C18H12N2O2
Molecular Weight
288.3
Solubility
≥ 28.8 mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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