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CX-5461 (Pidnarulex) is a potent small-molecule rRNA synthesis inhibitor with an IC50 of 0.11 μM. CX-5461 selectively blocks RNA PolI transcription,PIC assembly and SL1-rDNA interaction. CX-5461 indicates potent antiproliferative activity in cancer cells and induces autophagy incancer cells. CX-5461 shows potent antitumor activity in A375 and MiaPaca xenografts. CX-5461 (50 mg/kg, p.o.) inhibits the Eμ-Myc tumor cells with 84% repression in Pol I transcription at 1 hr posttreatment in C57BL/6 mice.
Nucleic Acids Res. 2022 Nov 28;gkac1114.
TERRA regulates DNA G-quadruplex formation and ATRX recruitment to chromatin
CX-5461 purchased from AbMole
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Source | J Exp Clin Cancer Res (2018). Figure 4. CX-5461 |
| Method | RT-PCR analysis | |
| Cell Lines | GBM cells | |
| Concentrations | 1 μM | |
| Incubation Time | 48 h | |
| Results | CX-5461 could lead to a significant decrease of hTERT-FL in a dose-dependent manner and had no effect on hTERT-All |
| Molecular Weight | 513.61 |
| Formula | C27H27N7O2S |
| CAS Number | 1138549-36-6 |
| Solubility (25°C) | Water 50 mg/mL (ultrasonic and adjust pH to 2 with HCl) 50 mM sodium phosphate (pH 3.5) : 10 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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