2. Apoptosis
  3. MDM-2/p53
  4. UC2288

UC2288 is a novel, cell-permeable, and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM.

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UC2288 Chemical Structure

UC2288 Chemical Structure

CAS No. : 1394011-91-6

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Customer Review

Based on 2 publication(s) in Google Scholar

UC2288 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

UC2288 is a novel, cell-permeable, and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM[1].

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.

UC2288 Related Antibodies

Western Blot Analysis[1]

Cell Line: HK2 (normal kidney), 786-O (RCC), Caki-1 (RCC), ACHN (RCC) and HEY (ovarian cancer) cells
Concentration: 0 μM; 1 μM; 3 μM; 10 μM
Incubation Time: 24 hours
Result: Decreased p21 protein expression.

RT-PCR[1]

Cell Line: p53-mutant RCC cell line 786-O
Concentration: 10 μM
Incubation Time: 24 hours
Result: Decreased p21 mRNA independent of p53 expression.
In Vivo

UC2888 (oral gavage; 15 mg/kg; 3 times a week; 4 weeks) co-treatment with imetelstat significantly suppresses tumor growth?and does not effect mice weight[2].
UC2288 (intraperitoneal?injection; 10 mg/kg; 4 times in 7 days) attenuates MPTP-induced behavioral impairment, prevents activation of MAPK pathway in the MPTP-treated mice brain. MPTP treatment raises TNF-α, IL-6 and IL-1β levels in MPTP treated mice brain, but UC2288 signicantly decreases MPTP-induced TNF-α, IL-6 levels, but IL-1β is not decreased in brain[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5x106)[2]
Dosage: 15 mg/kg
Administration: Oral gavage; 3 times a week; 4 weeks; co-treatment with imetelstat
Result: Combined treatment with imetelstat synergistically inhibited tumor growth in mice.
Animal Model: MPTP-induced C57BL6 Parkinson’s disease mice model[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 4 times in 7 days
Result: Ameliorated MPTP induced PD progression through inhibition of neuroinammation.
Molecular Weight

481.82

Formula

C20H18ClF6N3O2
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0755 mL 10.3773 mL 20.7546 mL
5 mM 0.4151 mL 2.0755 mL 4.1509 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.92%

COA (244 KB) HNMR (292 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

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
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
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UC2288 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UC22881394011-91-6UC 2288UC-2288MDM-2/p53RCC786-Op53-mutantp21sorafenibovariancancerHK2AttenuatorInhibitorinhibitorinhibit

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