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UC2288 is a novel p21 attenuator with cellular permeability and oral activity (relatively selective activity for P21), based on the structural synthesis of sorafenib. UC2288 down-regulated the expression of P21 mRNA and reduced the level of P21 protein independently of p53, and had little effect on the stability of P21 protein. UC2288 did not inhibit VEGFR2 and Raf kinases, even at 10 μM.
| Molecular Weight | 481.82 |
| Formula | C20H18ClF6N3O2 |
| CAS Number | 1394011-91-6 |
| Solubility (25°C) | DMSO 48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Mdm2 Products |
|---|
| Nutlin-3
Nutlin-3 is a selective MDM2 (mouse double minute 2) antagonist with IC50 of 90 nM. Nutlin-3 induces apoptosis in cancer cells. Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM in cells with wild-type p53 such as HCT116, RKO and SJSA-1. |
| NSC 66811
NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM, which disrupts MDM2-p53 interaction and activates p53 function. |
| Nutlin-3a
Nutlin-3a, the active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits the p53/MDM2 interaction with IC50 of 90 nM. |
| Nutlin-3b
Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite enantiomer Nutlin-3a. |
| SL-01
SL-01 is a p53-Mdm2 interaction inhibitor with IC50 of 3.18 μM. |
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