CX-5461

Catalog No. A11065

CX-5461是RNA聚合酶I（Pol I）的一流的非遗传毒性小分子靶向抑制剂，可激活p53途径而不会引起DNA损伤。

Product Citations

Taro Mannena, .et al. Distinct RNA polymerase transcripts direct the assembly of phase-separated DBC1 nuclear bodies in different cell lines, Mol Biol Cell, 2021, 32:ar33, 1?C11 PMID: 34495685
Shuichiro Okamoto, .et al. The rRNA synthesis inhibitor CX-5461 may induce autophagy that inhibits anticancer drug-induced cell damage to leukemia cells, Biosci Biotechnol Biochem, 2020, Aug 15;1-8 PMID: 32799625
Ahmed Abdullah Ahmed, .et al. A G-quadruplex-binding compound shows potent activity in human gemcitabine-resistant pancreatic cancer cells, Sci Rep, 2020, 10: 12192 PMID: 32699225
Abed Saady, .et al. Applying styryl quinolinium fluorescent probes for imaging of ribosomal RNA in living cells, Dyes Pigm, 2020, 174: 107986
Jackobel AJ, .et al. DNA binding preferences of S. cerevisiae RNA polymerase I Core Factor reveal a preference for the GC-minor groove and a conserved binding mechanism, Biochim Biophys Acta Gene Regul Mech, 2019, Aug 2:194408 PMID: 31382053
Hiroaki Suzuki, .et al. The proline-arginine repeat protein linked to C9-ALS/FTD causes neuronal toxicity by inhibiting the DEAD-box RNA helicase-mediated ribosome biogenesi, Cell Death Dis, 2018, Oct; 9(10): 975 PMID: 30250194
Anastasia Gelgor, .et al. Nucleolar stress enhances lytic reactivation of the Kaposi??s sarcoma-associated herpesvirus, Oncotarget, 2018, Mar 2; 9(17): 13822-13833 PMID: 29568397
Wang ZF, .et al. The Hairpin Form of r(G4C2)exp in c9ALS/FTD Is Repeat-Associated Non-ATG Translated and a Target for Bioactive Small Molecules, Cell Chem Biol, 2018, Nov 29. pii: S2451-9456(18)30378-7 PMID: 30503283
Yuko Fujiwara, .et al. A Nucleolar Stress-Specific p53-miR-101 Molecular Circuit Functions as an Intrinsic Tumor-Suppressor Network, EBioMedicine, 2018, Jul; 33: 33-48 PMID: 30049386
Maïmouna Coura Kone, .et al. Three-Dimensional Distribution of UBF and Nopp140 in Relationship to Ribosomal DNA Transcription During Mouse Preimplantation Development, Biol Reprod, 2016, Apr;94(4):95, 1-12 PMID: 26984997

Technical details

Catalog Num	A11065
M. Wt	513.6
Formula	C27H27N7O2S
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1138549-36-6
Synonyms	CX5461
SMILES	CC1=CN=C(C=N1)CNC(=O)C2=C3N(C4=CC=CC=C4S3)C5=C(C2=O)C=CC(=N5)N6CCCN(CC6)C

Biological Activity

CX-5461是RNA聚合酶I（Pol I）的一流的非遗传毒性小分子靶向抑制剂，可激活p53途径而不会引起DNA损伤。

Targets

A375	MIA PaCa-2	Pol I-driven transcription of rRNA (HCT-116, A375, MIA PaCa-2 cells)	HCT-116
58 nM(ED50)	74 nM(ED50)	142 nM	167 nM(ED50)

Solubility *

In vitro	DMSO	<1 mg/mL
	Water	Insoluble
	Ethanol	DMF: Warmed: 3 mg/mL (5.84 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	19.47 mL	97.35 mL	194.7 mL
0.5 mM	3.89 mL	19.47 mL	38.94 mL
1 mM	1.95 mL	9.74 mL	19.47 mL
5 mM	0.39 mL	1.95 mL	3.89 mL

*The above data is based on the productmolecular weight 513.6. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.