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

UC2288 

Cat. No.: HY-112780
Handling Instructions

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.

For research use only. We do not sell to patients.

UC2288 Chemical Structure

UC2288 Chemical Structure

CAS No. : 1394011-91-6

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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].

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].

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.

1394011-91-6

SMILES

O=C(N[[email protected]]1CC[[email protected]](OC2=NC=C(C(F)(F)F)C=C2)CC1)NC3=CC=C(Cl)C(C(F)(F)F)=C3

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

UC2288UC 2288UC-2288MDM-2/p53RCC786-Op53-mutantp21sorafenibovariancancerHK2AttenuatorInhibitorinhibitorinhibit

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