UC2288
Based on 10 publication(s) in Google Scholar
UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM.
For research use only. We do not sell to patients.
- Purity : 99.78%
- CAS No.: 1394011-91-6
- Formula: C20H18ClF6N3O2
- Molecular Weight:481.82
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) UC2288
More- J Biomed Sci. 2026 May 9;33(1):49. [Abstract]
- Adv Sci (Weinh). 2025 Oct 5:e04474. [Abstract]
- Cell Rep Med. 2025 Feb 18;6(2):101964. [Abstract]
- J Control Release. 2026 Jan 10:389:114488. [Abstract]
- Cell Death Dis. 2024 Jun 17;15(6):422. [Abstract]
- J Periodontal Res. 2024 Jun;59(3):599-610. [Abstract]
- J Gastroenterol Hepatol. 2026 Jun 25. [Abstract]
- J Oral Biosci. 2024 Dec;66(4):74-80. [Abstract]
- Res Sq. 2024 Jul 29.
- University of Gothenburg. 2023 Jun 27.
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Cell Imaging/Staining
Biological Activity
Description
In Vitro
UC2288 (0-10 μM; 24 hours) decreases p21 protein level, but has no effects on other proteins[1].UC2288 (0-10 μM; 24 hours) decreases p21 mRNA expression transcriptionally or post-transcriptionally but independently of p53[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HK2 (normal kidney), 786-O (RCC), Caki-1 (RCC), ACHN (RCC) and HEY (ovarian cancer) cells
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Concentration:0 μM; 1 μM; 3 μM; 10 μM
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Incubation Time:24 hours
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Result:Decreased p21 protein expression.
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Cell Line:p53-mutant RCC cell line 786-O
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Decreased p21 mRNA independent of p53 expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5x106)[2]
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Dosage:15 mg/kg
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Administration:Oral gavage; 3 times a week; 4 weeks; co-treatment with imetelstat
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Result:Combined treatment with imetelstat synergistically inhibited tumor growth in mice.
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Animal Model:MPTP-induced C57BL6 Parkinson’s disease mice model[3]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; 4 times in 7 days
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Result:Ameliorated MPTP induced PD progression through inhibition of neuroinammation.
Chemical Information
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CAS No. 1394011-91-6
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Appearance Solid
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Molecular Weight 481.82
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Formula C20H18ClF6N3O2
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Color White to off-white
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SMILES
O=C(N[C@H]1CC[C@H](OC2=NC=C(C(F)(F)F)C=C2)CC1)NC3=CC=C(Cl)C(C(F)(F)F)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (10)
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Journal Impact Factor
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Most Recent
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J Biomed Sci
CASK promotes non-small cell lung cancer growth through coordinated regulation of EGFR expression, trafficking, and p21 expression. [Abstract]2026 May 9;33(1):49. PMID: 42106797 -
Adv Sci (Weinh)
2025 Oct 5:e04474. PMID: 41047496 -
Cell Rep Med
Unraveling AURKB as a potential therapeutic target in pulmonary hypertension using integrated transcriptomic analysis and pre-clinical studies. [Abstract]2025 Feb 18;6(2):101964. PMID: 39933527
UC2288 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Feb 18;6(2):101964. [Abstract]
An increase in p21-positive PASMCs was observed with Barasertib treatment, which was attenuated by co-treatment with UC2288. In addition, cleaved caspase-3 staining revealed a significant increase in PASMC apoptosis after combination therapy.
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J Control Release
Bioswitchable intracellular delivery of small activating RNA by tetrahedral framework nucleic acid: Application to p21-mediated anti-tumor therapy. [Abstract]2026 Jan 10:389:114488. PMID: 41330514 -
Cell Death Dis
TGF-β1 facilitates gallbladder carcinoma metastasis by regulating FOXA1 translation efficiency through m6A modification. [Abstract]2024 Jun 17;15(6):422. PMID: 38886389 -
J Periodontal Res
ZNF862 induces cytostasis and apoptosis via the p21-RB1 and Bcl-xL-Caspase 3 signaling pathways in human gingival fibroblasts. [Abstract]2024 Jun;59(3):599-610. PMID: 38482719 -
J Gastroenterol Hepatol
Coal Dust-Mimetic Carbon Nanoparticles Induce Colonic Epithelial Cell Senescence via p16/p21 Dual Pathways and Promote Colonic Inflammatory Response. [Abstract]2026 Jun 25. PMID: 42350080 -
J Oral Biosci
Antihypertensive agent losartan promotes tongue squamous cell carcinoma cell proliferation via EGFR/ERK1/2/cyclin D1 signaling axis. [Abstract]2024 Dec;66(4):74-80. PMID: 39245205 -
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Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (103.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 12.5 mg/mL (25.94 mM; Need ultrasonic)
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. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Protocol for Cell Counting and Cell Density Analysis
Cell counting and cell-density analysis estimate the number of cells in a known volume or field area. Manual hemocytometer counting uses a chamber of defined geometry to convert counted cells into cells/mL, while automated counters and image-analysis workflows detect cell objects from optical, brightfield, fluorescence, impedance, or digital-image features. Trypan blue viability counting is based on dye exclusion: viable cells with intact membranes exclude dye, while non-viable cells with compromised membranes stain blue. The readout is total cell density, viable-cell density, dead-cell density, and percent viability. Cell density can also be estimated from microscopy images by counting objects per image area, from flow cytometry using calibrated volume or reference particles, or from in situ microscopy in bioreactors after calibration against reference methods such as hemocytometer or flow cytometry.
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Somatic Cell Culture
A method of simulating the in vivo environment in vitro to maintain the cell growth, differentation and main functions.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
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Cell Counting-Based Growth Curve Assay
Cell counting-based growth curve assays quantify cell proliferation by directly measuring changes in viable cell number over time using manual or automated counting methods such as hemocytometer-based counting or instrument-assisted cell enumeration, enabling construction of growth curves that reflect population expansion dynamics in response to culture conditions. A widely used approach is trypan blue exclusion with hemocytometer counting, where membrane-compromised (non-viable) cells take up the dye, allowing discrimination between viable and non-viable cells while simultaneously enabling total cell number quantification. Repeated sampling across time points allows estimation of proliferation rate, growth phases, and comparative growth kinetics between experimental conditions.
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MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (276 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
[1]. Hiromi I Wettersten, et al. A Novel p21 Attenuator Which Is Structurally Related to Sorafenib. Cancer Biol Ther. 2013 Mar;14(3):278-85. [Content Brief]
[2]. Romi Gupta, et al. Synergistic tumor suppression by combined inhibition of telomerase and CDKN1A. Proc Natl Acad Sci U S A. 2014 Jul 29;111(30):E3062-71. [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. 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 |
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| Ethanol / DMSO | 1 mM | 2.0755 mL | 10.3773 mL | 20.7546 mL | 51.8866 mL |
| 5 mM | 0.4151 mL | 2.0755 mL | 4.1509 mL | 10.3773 mL | |
| 10 mM | 0.2075 mL | 1.0377 mL | 2.0755 mL | 5.1887 mL | |
| 15 mM | 0.1384 mL | 0.6918 mL | 1.3836 mL | 3.4591 mL | |
| 20 mM | 0.1038 mL | 0.5189 mL | 1.0377 mL | 2.5943 mL | |
| 25 mM | 0.0830 mL | 0.4151 mL | 0.8302 mL | 2.0755 mL | |
| DMSO | 30 mM | 0.0692 mL | 0.3459 mL | 0.6918 mL | 1.7296 mL |
| 40 mM | 0.0519 mL | 0.2594 mL | 0.5189 mL | 1.2972 mL | |
| 50 mM | 0.0415 mL | 0.2075 mL | 0.4151 mL | 1.0377 mL | |
| 60 mM | 0.0346 mL | 0.1730 mL | 0.3459 mL | 0.8648 mL | |
| 80 mM | 0.0259 mL | 0.1297 mL | 0.2594 mL | 0.6486 mL | |
| 100 mM | 0.0208 mL | 0.1038 mL | 0.2075 mL | 0.5189 mL |