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Chemical Structure| 1394011-91-6 Chemical Structure| 1394011-91-6

Structure of UC2288
CAS No.: 1394011-91-6

Chemical Structure| 1394011-91-6

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UC2288 is a novel p21-attenuating reagent with cell permeability and oral activity (having relatively selective activity against p21), synthesized based on the structure of sorafenib. UC2288 downregulates the expression of p21 mRNA without relying on p53, reducing the level of p21 protein, with minimal impact on the stability of the p21 protein.

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Product Details of UC2288

CAS No. :1394011-91-6
Formula : C20H18ClF6N3O2
M.W : 481.82
SMILES Code : 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
MDL No. :MFCD28139634
InChI Key :ISPSOOYSNVVMMB-UHFFFAOYSA-N
Pubchem ID :60196635

Safety of UC2288

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319
Precautionary Statements:P264-P280-P302+P352-P305+P351+P338-P332+P313-P337+P313-P362

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SH-SY5Y cells 10 µM 2 hours, 4 hours and 6 hours Investigate the effect of UC2288 on p21 mRNA and protein levels. Results showed an increase in p21 mRNA levels at 4 hours but no change in the fraction of p21 or p-p21 positive cells. Front Oncol. 2022 Sep 6;12:906194
Kelly cells 10 µM 2 hours, 4 hours and 6 hours Investigate the effect of UC2288 on p21 mRNA and protein levels. Results showed a decrease in p21 mRNA levels after 2 hours followed by an increase at 4 and 6 hours. Western blot showed reduced p-p21 expression at all time points. Front Oncol. 2022 Sep 6;12:906194
BCBL1 cells 5 µM 24 and 48 hours To evaluate the effect of UC2288 on PEL cell survival, results showed that UC2288 alone induced cytotoxic effects and further reduced cell survival when combined with Lovastatin. IUBMB Life. 2021 Jul;73(7):968-977
BC3 cells 5 µM 24 and 48 hours To evaluate the effect of UC2288 on PEL cell survival, results showed that UC2288 alone induced cytotoxic effects and further reduced cell survival when combined with Lovastatin. IUBMB Life. 2021 Jul;73(7):968-977
MIN6 cells 2.5 µM 24 hours To investigate the effect of UC2288 on apoptosis in MIN6 cells under DNA damage conditions. Results showed that UC2288 inhibited p21 function and significantly increased the frequency of apoptosis in MIN6 cells under DNA damage conditions. Sci Rep. 2019 Dec 18;9(1):19341
BE(2)-C cells 10 µM 24 hours Investigate the effect of UC2288 on p21 and p-p21 expression. Western blot showed increased p21 expression and decreased p-p21 expression. Front Oncol. 2022 Sep 6;12:906194
Normal kidney proximal tubule epithelial cell line HK2 10 µM 24 hours UC2288 markedly decreased p21 protein levels. Cancer Biol Ther. 2013 Mar;14(3):278-85
Ovarian cancer cell line Hey 10 µM 24 hours UC2288 markedly decreased p21 protein levels. Cancer Biol Ther. 2013 Mar;14(3):278-85
Renal cell carcinoma cell line ACHN 10 µM 24 hours UC2288 markedly decreased p21 protein levels. Cancer Biol Ther. 2013 Mar;14(3):278-85
Renal cell carcinoma cell line Caki-1 10 µM 24 hours UC2288 markedly decreased p21 protein levels. Cancer Biol Ther. 2013 Mar;14(3):278-85
Renal cell carcinoma cell line 786-O 10 µM 24 hours UC2288 decreased p21 protein levels independently of p53 activity, via transcriptional or post-transcriptional regulation. Cancer Biol Ther. 2013 Mar;14(3):278-85
5-8F 4 µM, 6 µM, 8 µM, 12 µM 24 hours, 48 hours To evaluate the inhibitory effect of UC2288 on the proliferation of 5-8F cells, the results showed that UC2288 significantly inhibited cell proliferation in a dose- and time-dependent manner, and the effect was better than that of cisplatin. J Cancer. 2021 Jan 1;12(4):988-995
CNE-2 4 µM, 6 µM, 8 µM, 12 µM 24 hours, 48 hours To evaluate the inhibitory effect of UC2288 on the proliferation of CNE-2 cells, the results showed that UC2288 significantly inhibited cell proliferation in a dose- and time-dependent manner. J Cancer. 2021 Jan 1;12(4):988-995
Amnion Epithelial Cells (AECs) 20 µM 48 hours UC2288, as a p21 inhibitor, was used to block Dex-induced senescence in amnion epithelial cells. Results showed that UC2288 significantly reduced Dex-induced cellular senescence. Biol Reprod. 2019 Jun 1;100(6):1605-1616
Human erythroid progenitors 1 µM 6 days Partially rescued DNMT1 deficiency-induced cell cycle arrest by inhibiting p21 expression. Cell Death Differ. 2024 Aug;31(8):999-1012

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Db/db mice In vitro treatment 2.5 µM 24 hours To investigate the effect of UC2288 on apoptosis in β-cells of db/db mice under DNA damage conditions. Results showed that UC2288 inhibited p21 function and significantly increased the frequency of apoptosis in β-cells under DNA damage conditions. Sci Rep. 2019 Dec 18;9(1):19341

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.38mL

2.08mL

1.04mL

20.75mL

4.15mL

2.08mL

 

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